HomeAll New Products Listed Chronologically

All New Products Listed Chronologically

Catalog No. Product Name Information Isotype
E4942 Talazoparib tosylate Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1. Dec 26 2024
E1882 THZ1 THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression. Dec 26 2024
E4790 H-89 H-89 is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase, and others kinases. Dec 26 2024
E4787 Etomoxir Etomoxir ((R)-(+)-Etomoxir) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig. Dec 26 2024
E4788 Nigericin Nigericin is an antibiotic derived from Streptomyces hygroscopicus that act as a K+/H+ ionophore, promoting K+/H+ exchange across mitochondrial membranes. Nigericin shows promising anti-cancer activities through decreasing intracellular pH (pHi), and inactivation of Wnt/β-catenin signals. Nigericin induces pyroptosis through caspase 1/GSDMD in TNBC. Dec 26 2024
E1251 Oligomycin Oligomycin, an antifungal antibiotic, is an inhibitor of H+-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells. Dec 26 2024
S7925 Deferoxamine Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19. Dec 26 2024
P1247 Exendin-4 Exendin-4 (Exenatide), a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM. Dec 26 2024
E1230 Vaborbactam Vaborbactam (RPX7009) is a cyclic boronic acid pharmacophore β-lactamase inhibitor. Dec 26 2024
E1473 BODIPY 581/591 C11 BODIPY 581/591 C11 is a BODIPY borofluoroprene derivative with good light stability and low fluorescence artifacts. BODIPY 581/591 C11 can be used for study lipid peroxidation and antioxidant properties in living cells, or detect ferroptosis by reaction with hydroxyl radicals. BODIPY 581/591 C11 is emitted at 591 nm (reduced prototype), or redshifted to 510 nm (oxidized type). The excitation wavelengths were 581 nm (reduced prototype) and 500 nm (oxidized type). Dec 26 2024
E4789 Bleomycin hydrochloride Bleomycin hydrochloride is a DNA synthesis inhibitor. Bleomycin hydrochloride is a DNA damaging agent. Bleomycin hydrochloride is an antitumor antibiotic. Dec 26 2024
E1835 diABZI STING agonist-1 trihydrochloride diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively. Dec 26 2024
E4794 GSK-J4 GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1. GSK-J4 induces endoplasmic reticulum stress-related apoptosis. Dec 26 2024
P1235 Raleukin Raleukin (AMG-719) is a recombinant, nonglycosylated human interleukin-1 receptor (IL-1R) antagonist. Raleukin (AMG-719) is the first biological agent to block the pro-inflammatory effects. Dec 26 2024
E4795 Bobcat339 Bobcat339 is a potent and selective cytosine-based inhibitor of TET enzyme, with IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription. Dec 26 2024
E4796 SRT 1720 SRT 1720 is a selective activator of human SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities for SIRT2 and SIRT3 with EC1.5s of 37 μM and > 300 μM, respectively. Dec 26 2024
E1850 Aldoxorubicin Aldoxorubicin (INNO-206) is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models. Dec 26 2024
E4996 Puromycin Puromycin dihydrochloride is the dihydrochloride salt of puromycin. Puromycin is an aminoglycoside antibiotic that inhibits protein synthesis. Dec 26 2024
E4797 Fluo-4 AM Fluo-4 AM is a cell-permeable Ca2+ indicator. Dec 26 2024
P1244 PLGA (50:50) PLGA (50:50) (poly(lactic-co-glycolic acid) (50:50)) is a copolymer of poly lactic acid (PLA) and poly glycolic acid (PGA) which can be used to fabricate devices for drug delivery and tissue engineering applications. Dec 26 2024
E1838 Acridine Orange hydrochloride Acridine Orange hydrochloride is a cell-penetrable nucleic acid-selective fluorescent dye. Acridine Orange hydrochloride produces orange fluorescence when it binds to ssDNA or RNA, and green fluorescence when it binds to dsDNA (Ex: 488 nM; Em: green fluorescence at 530 nm, orange fluorescence at 640 nm). Dec 26 2024
E4799 BIX-01294 BIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells. Dec 26 2024
S7879 Tin protoporphyrin IX dichloride Tin protoporphyrin IX dichloride (SnPPIX) is a potent Heme oxygenase-1 (HO-1) inhibitor. Tin protoporphyrin IX dichloride sensitizes pancreatic ductal adenocarcinoma (PDAC) tumors to chemotherapy in mice model. Dec 26 2024
E4982 Ouabain Octahydrate Ouabain Octahydrate is an inhibitor of Na+/K+-ATPase, used for the treatment of congestive heart failure. Dec 26 2024
E4776 Rhod-2 AM Rhod-2 is a high-affinity visible light excitation wavelength Ca2+ fluorescent probe, Rhod-2, AM is an acetyl methyl ester derivative of Rhod-2, which has cell membrane permeability and can easily enter cells with simple culture. Once it enters the cell, it is sheared by its lactesterase to produce Rhod-2 without membrane permeability, which remains in the cell to perform the corresponding physiological functions. Maximum excitation/emission wavelength: 549/578 nm. Dec 26 2024
E4992 Afuresertib hydrochloride Afuresertib hydrochloride (GSK 2110183 hydrochloride) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively. Dec 26 2024
S9834 CA-074 CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM. Dec 26 2024
S3277 Monensin Monensin (Monensin A), an orally active antibiotic, is an ionophore that mediates Na+/H+ exchange. Monensin is a potent Wnt signaling inhibitor. Monensin causes a marked enlargement of the multivesicular bodies (MVBs) and regulates exosome secretion. Monensin can be used for bacterial, fungal, and parasitic infections research, and shows anticancer effects. Dec 26 2024
S7407 NFAT Inhibitor-1 NFAT Inhibitor (VIVIT peptide) is a cell-permeable peptide inhibitor of nuclear factor of activated Tcells (NFAT) that selectively inhibits calcineurin-mediated dephosphorylation of NFAT. Dec 26 2024
E5820 AKT Kinase Inhibitor AKT Kinase Inhibitor is an Akt kinase inhibitor with anti-tumor activity. Dec 26 2024
E4981 Fluvastatin Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway. Dec 26 2024
E2845 Maribavir Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC50 of 3 nM. Maribavir has potent antiviral activity against HCMV and Epstein-Barr virus (EBV). Dec 26 2024
E8213 Tanzisertib Tanzisertib (CC-930) is a potent JNK1/2/3 inhibitor with IC50s of 61/7/6 nM, respectively. Dec 26 2024
E1415 C16-PAF C16-PAF (PAF (C16)), a phospholipid mediator, is a platelet-activating factor and ligand for PAF G-protein-coupled receptor (PAFR). C16-PAF exhibits anti-apoptotic effect and inhibits caspase-dependent death by activating the PAFR. C16-PAF is a potent MAPK and MEK/ERK activator. C16-PAF induces increased vascular permeability. Dec 26 2024
E4894 Fasudil Fasudil (HA-1077; AT877) is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil is also a potent Ca2+ channel antagonist and vasodilator. Dec 26 2024
E1792 Cefiderocol Cefiderocol (S-649266) is a siderophore cephalosporin which has a potent activity against a broad range of aerobic Gram-negative bacterial species with MIC50s of 2 μg/mL or less. Dec 26 2024
E5810 Ro 67-7476 Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM. Ro 67-7476 is a potent P-ERK1/2 agonist?and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM). Dec 26 2024
S7385 Calyculin A Calyculin A ((-)-Calyculin A) is a potent and cell-permeable protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A) inhibitor with IC50s of 2 nM and 0.5-1 nM, respectively. Dec 26 2024
E8214 cGAMP cGAMP (Cyclic GMP-AMPP) functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators. Dec 26 2024
E4698 Temoporfin Temoporfin (m-THPC), a reduced porphyrin, is a potent second-generation photosensitizer. Temoporfin can be used in the research of photodynamic therapy (PDT) for head and neck cancers. Dec 26 2024
E5770 DIDS sodium salt DIDS sodium salt (MDL101114ZA) is a dual inhibitor of ABCA1 and VDAC1. DIDS also inhibits RAD51, inhibiting RAD51-mediated homologous pairing and strand exchange reactions. DIDS inhibits anion exchange and binding to red blood cell membranes, inhibits the activation of caspase-3 and -9, and can be used in cancer research. Dec 26 2024
S7887 Concanamycin A Concanamycin A (Folimycin; Antibiotic X 4357B) is a macrolide antibiotic, a vacuolar type H+-ATPase (V-ATPase) inhibitor. Concanamycin A is also an inhibitor of lysosomal acidification, can be used to T cell-mediated inflammation research-. Dec 26 2024
S8121 LY341495 LY341495 is a metabotropic glutamate receptor (mGluR) antagonist with IC50s of 21 nM, 14 nM, 7.8 μM, 8.2 μM, 170 nM, 990 nM, 22 μM for mGlu2, mGlu3, mGlu1a, mGlu5a, mGlu8, mGlu7, and mGlu4 receptors, respectively. Dec 26 2024
E1227 CAY10566 CAY10566 is a potent, orally bioavailable and selective stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. CAY10566 also shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM). Dec 26 2024
E1060 AVE 0991 AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC50 of 21 nM. Dec 26 2024
E5827 Propranolol Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy. Dec 26 2024
E1999 Sphingosine-1-phosphate Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca2+ as an extracellular ligand for G protein-coupled receptors. Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids. Dec 26 2024
E1756 KJ Pyr 9 KJ Pyr 9 is an inhibitor of MYC with a Kd of 6.5 nM in in vitro assay. Dec 26 2024
E1380 Tonabersat Tonabersat (SB-220453) is a gap-junction modulator. Tonabersat prevents inflammatory damage in the central nervous system. Dec 26 2024
E1387 Butyrolactone 3 Butyrolactone 3 (MB-3) is a specifical small-molecule inhibitor of the histone acetyltransferase Gcn5 (IC50=100 μM), which has a high affinity to the Gcn5 enzyme comparable to that of its natural substrate, histone H3. Butyrolactone 3 shows weak inhibitory on CBP (IC50=0.5 mM). Butyrolactone 3 can be used in studies of cancer, metabolic, autoimmune and neurological diseases. Dec 26 2024
S8204 Phalloidin Phalloidin is a mushroom-derived toxin which can be used to label F-actin of the cytoskeleton with fluorochrome . Dec 26 2024
E1873 CY5 CY5 is a CY dye. CY, short for Cyanine, is a compound consisting of two nitrogen atoms connected by an odd number of methyl units. Cyanine compounds have the characteristics of long wavelength, adjustable absorption and emission, high extinction coefficient, good water solubility and relatively simple synthesis. CY dyes are of en used for the labeling of proteins, antibodies and small molecular compounds. For the labeling of protein antibodies, the combination can be completed through a simple mixing reaction. Below, we introduce the labeling method of protein antibody labeling, which has certain reference significance. Dec 26 2024
S8216 Latrunculin A Latrunculin A (LAT-A), found in the red sea sponge Latrunculia magnifica, is a G-actin polymerization inhibitor. Latrunculin A binds to actin monomers and inhibits polymerization of actin with Kds of 0.1, 0.4, 4.7 μM and 0.19 μM for ATP-actin, ADP-Pi-actin, ADP-actin and G-actin, respectively. Latrunculin A has effective anti-metastatic properties for cancer research. Latrunculin A blocks cell migration. Dec 26 2024
E1626 BMS-509744 BMS-509744 is a potent, selective and ATP competitive Itk inhibitor with an IC50 of 19 nM. Dec 26 2024
E6039 Imiquimod hydrochloride Imiquimod hydrochloride (R 837 hydrochloride), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod hydrochloride exhibits antiviral and antitumor effects in vivo. Imiquimod hydrochloride can be used for the research of external genital, perianal warts, cancer and COVID-19. Dec 26 2024
E5807 Eflornithine Eflornithine is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women. Dec 26 2024
S8252 Okadaic acid Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid increases of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter. Okadaic acid induces tau phosphorylation. Dec 26 2024
E4707 Aldosterone Aldosterone is the primary mineralocorticoid. Aldosterone is a steroid hormone, and it is synthesized and secreted in response to renin-angiotensin system activation (RAS) or high dietary potassium by the zona glomerulosa (ZG) of the adrenal cortex. Aldosterone activity is dependent by the binding and activation of the cytoplasmic/nuclear mineralocorticoid receptor (MR) at cellular level. Dec 26 2024
E4743 NITD008 NITD008 is a potent and selective flaviviruse inhibitor which can inhibit Dengue Virus Type 2 (DENV-2) with an EC50 of 0.64 μM. NITD008 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 26 2024
E8146 Citric acid trisodium Citric acid trisodium is a natural preservative and food tartness enhancer. Citric acid trisodium induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid trisodium cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid trisodium causes renal toxicity in mice. Dec 26 2024
E8147 PI-103 Hydrochloride PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy. Dec 26 2024
E8148 BAPTA BAPTA is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA is widely used as an intracellular buffer for investigating the effects of Ca2+ release from intracellular stores or influx via Ca2+-permeable channels in the plasma membrane. BAPTA can also inhibit phospholipase C activity independently of their role as Ca2+ chelators. Dec 26 2024
E8149 Bovine Serum Albumin Bovine Serum Albumin (BSA) is a 583-residue protein consisting of three homologous all-α domains, organized in a heart-shaped structure. BSA is a globular protein that is used in numerous biochemical applications. Dec 26 2024
E8150 Amiloride Amiloride (MK-870) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride is a blocker of polycystin-2 (PC2; TRPP2) channel. Dec 26 2024
E8151 Bleomycin Bleomycin is a glycopeptide antibiotic. Bleomycin has potent antitumour activities against a range of lymphomas, head and neck cancers and germ-cell tumours. Bleomycin can be used for the research of cancer and chemotherapy. Dec 26 2024
E8152 Bay 41-4109 BAY 41-4109 is a potent inhibitor of human hepatitis B virus (HBV) with an IC50 of 53 nM. Dec 26 2024
E8153 Filipin complex Filipin complex is a potent polyene macrolide antifungal antibiotic. Filipin complex inserts into membranes and sequester cholesterol into complexes and inhibits PRRSV entry. The Filipin complex consists of about 75.8% Filipin III (HY-N6718), 10.8% Filipin IV, 9.1% Filipin II, and 1.2% Filipin I. Dec 26 2024
E8155 α-MSH α-MSH (α-Melanocyte-Stimulating Hormone), an endogenous neuropeptide, is an endogenous melanocortin receptor 4 (MC4R) agonist with anti-inflammatory and antipyretic activities. α-MSH is a post-translational derivative of pro-opiomelanocortin (POMC). Dec 26 2024
E8156 2’3’-c-di-AM(PS)2 (Rp,Rp) (ammonium salt) 2’3’-c-di-AM(PS)2 (Rp,Rp) ammonium salt (ADU-S100 ammonium salt), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity. Dec 26 2024
E8157 FLAG peptide FLAG peptide is a multifunctional fusion tag for the purification of recombinant proteins. FLAG peptide maintances the natural folding of its fusing proteins. FLAG peptide can be removed by enterokinase, and eluted under non-denaturing conditions. Dec 26 2024
E8158 OTSSP167 hydrochloride OTSSP167 (OTS167) hydrochloride is a highly potent and ATP-competitive MELK inhibitor with IC50 value of 0.41 nM. Dec 26 2024
E8159 CY5-SE Cy5-SE (Cy5 NHS Ester) is a reactive dye for the labeling of amino-groups in peptides, proteins, and oligonucleotides. This dye requires small amount of organic co-solvent (such as DMF or DMSO) to be used in labeling reaction. This reagent is ideal for very cost-efficient labeling of soluble proteins, as well as all kinds of peptides and oligonucleotides. This reagent also works well in organic solvents for small molecule labeling. Excitation (nm):649, Emission (nm): 670. Dec 26 2024
E8160 Cyclo(-RGDfK) Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface. Dec 26 2024
E8161 Fasiglifam Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM. Dec 26 2024
E8162 Nicotinamide riboside Nicotinamide riboside, an orally active NAD+ precursor, increases NAD+ levels and activates SIRT1 and SIRT3. Nicotinamide riboside is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease. Dec 26 2024
E8163 GW3965 GW3965 is a potent, selective liver X receptor (LXR) agonist with EC50s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively. Dec 26 2024
E8164 Daunorubicin Daunorubicin (Daunomycin) is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin inhibits DNA and RNA synthesis. Daunorubicin is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin is also an anthracycline antibiotic. Daunorubicin can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor. Dec 26 2024
E8165 MMAF hydrochloride MMAF (Monomethylauristatin F) hydrochloride is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF hydrochloride is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as Vorsetuzumab mafodotin and SGN-CD19A. Dec 26 2024
E8166 PF429242 dihydrochloride PF429242 dihydrochloride is a reversible and competitive SREBP site 1 protease (S1P) inhibitor with an IC50 of 175 nM. Dec 26 2024
E8167 MRT68921 dihydrochloride MRT68921 dihydrochloride is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively. Dec 26 2024
E8168 Substance P Substance P (Neurokinin P) is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R). Dec 26 2024
E8169 C12-200 C12-200 is a type of ionizable cationic lipid and helper lipid commonly used for mRNA delivery. In the hemophilia B mouse model, mRNA encoding human erythropoietin (EPO) and coagulation factor IX (FIX) can be successfully delivered and expressed using C12-200. C12-200 is utilized in research related to hemophilia B. Dec 26 2024
E8170 SCH 546738 SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments. Dec 26 2024
E8171 NSC 23766 NSC 23766 is a cell-permeable, reversible and specific inhibitor of Rac GTPase, used for cancer treatment. Dec 26 2024
E8172 Pyridostatin Pyridostatin (RR82) is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin targets the proto-oncogene Src. Pyridostatin reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells. Dec 26 2024
E8173 AZD-5991 AZD-5991 is a potent and selective Mcl-1 inhibitor with an IC50 of 0.7 nM in FRET assay and a Kd of 0.17 nM in surface plasmon resonance (SPR) assay. Dec 26 2024
E8174 Streptomycin Streptomycin (Agrept) is an effective antibiotic against M. tuberculosis, is used for the research of tuberculosis (TB). Streptomycin also is a bacteriocidal agent that can be used for the research of a number of bacterial infections. Streptomycin can bind strongly to nucleic acids, interferes and blocks protein synthesis while permitting continued RNA and DNA synthesis. Streptomycin, as a common antibiotic used in culture media, also is a blocker of stretch-activated and mechanosensitive ion channels in neurons and cardiac myocytes . Dec 26 2024
E8175 Hoechst 33342 trihydrochloride Hoechst 33342 trihydrochloride is a marker dye in Hoechst series. Hoechst is A live nuclear marker dye. Hoechst binds to the grooves in the DNA double strand, which tends to be A/ T-rich DNA strand. Although it binds to all nucleic acids, the A/ T-rich double strand DNA significantly enhances fluorescence intensity Therefore,Hoechst dye can be used for living cell labeling. The fluorescence intensity of Hoechst dye increases with the increase of pH of solution. Dec 26 2024
E8176 TMA-DPH TMA-DPH is a hydrophobic fluorescent membrane probe (Ex=355 nm; Em=430 nm). TMA-DPH is able to anchor on the cell surface and localize to different regions of the phospholipid bilayer. By analyzing the fluorescence polarization values of TMA-DPH in the plasma membrane and membrane substructures, the fluidity of the cell membrane can be determined. Dec 26 2024
E8177 5-Ph-IAA 5-Ph-IAA is a derivative of IAA. 5-Ph-IAA, a ligand, establishes the auxin-inducible degron 2 (AID2) system together with an OsTIR1 (F74G) mutant. AID2 induces rapid and efficient depletion of mAID-fused proteins to study protein function in living cells, causing tumor suppression. Dec 26 2024
E8178 Quisinostat Quisinostat (JNJ-26481585) is a potent, second-generation and orally active pan-HDAC inhibitor (HDACi), with IC50 values ranging from 0.11 nM to 0.64 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11. Quisinostat has a broad spectrum antitumoral activity. Quisinostat can induce autophagy in neuroblastoma cells. Dec 26 2024
E8179 2’3’-c-di-AM(PS)2 (Rp,Rp) (disodium salt) 2’3’-c-di-AM(PS)2 (Rp,Rp) disodium salt (ADU-S100 disodium salt) is an activator of stimulator of interferon genes (STING). Dec 26 2024
E8180 Zosuquidar Zosuquidar (LY335979) is a P-glycoprotein (P-gp) inhibitor (Ki=59 nM). Zosuquidar shows anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research. Dec 26 2024
E8181 Glucagon (1-29), bovine, human Glucagon (1-29), bovine, human, porcine is a peptide hormone, produced by pancreatic α-cells. Glucagon stimulates gluconeogenesis. Glucagon (1-29), bovine, human, porcine activates HNF4α and increases HNF4α phosphorylation. Dec 26 2024
E8182 3X FLAG peptide 3X FLAG peptides are FLAG-tagged peptides containing three repeats of the Asp-Tyr-Lys-Xaa-Xaa-Asp motif. 3X FLAG peptide can be used for protein separation and purification, and competitive elution with target proteins. Dec 26 2024
E8183 Firategrast Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity. Dec 26 2024
E8184 FAPI-4 FAPI-4 is a potent fibroblast activation protein (FAP) inhibitor for the targeting FAP. FAPI-4 can be used in cancer research. 68Ga-FAPI-4 PET/CT is a promising new diagnostic method for imaging various kinds of cancer, with good tumor-to-background contrast ratios. Dec 26 2024
E8185 A 438079 A 438079 is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9. Dec 26 2024
E8186 Triton X-100 Triton X-100 surfactant is an oligomeric blend that can be used for biochemical research. Dec 26 2024
E8187 DAF-FM DA DAF-FM DA (Diaminofluorescein-FM diacetate) is a fluorescent probe for the detection and bioimaging of nitric oxide (NO). DAF-FM DA spontaneously crosses the plasma membrane and is subsequently cleaved by esterases to generate intracellular DAF-FM (Ex/Em=495/515 nm). Dec 26 2024
E8188 Ro 31-8220 Ro 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7. Dec 26 2024
E8189 DMG-PEG 2000 DMG-PEG 2000 is used?for the preparation of liposome for siRNA delivery with improved transfection efficiency in vitro. DMG-PEG 2000 is also used for the?lipid nanoparticle for an oral plasmid DNA delivery approach in vivo through a facile surface modification to improve the mucus permeability and delivery efficiency of the nanoparticles. Dec 26 2024
E8190 L-Asparaginase L-Asparaginase (L-ASNase) is a deamidating enzyme that catalyses the hydrolysis of L-asparagine and L-glutamine, and can be used for the research of acute lymphoblastic leukemia. L-Asparaginase depletes L-asparagine from plasma resulting in inhibition of RNA and DNA synthesis with the subsequent blastic cell apoptosis. Dec 26 2024
E8191 Rat CGRP-(8-37) Rat CGRP-(8-37) (VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) is a highly selective CGRP receptor antagonist. Dec 26 2024
E8192 L-Leucyl-L-Leucine methyl ester hydrobromide L-Leucyl-L-Leucine methyl ester (LLOMe) hydrobromide, a dipeptide condensation product of L-leucine methyl ester generated by human monocytes or polymorphonuclear leukocytes, selectively eliminates lymphocytes with cytotoxic potential. L-Leucyl-L-Leucine methyl ester hydrobromide also can induce endolysosomal pathway stress. Dec 26 2024
E8193 Guanosine-5'-triphosphate disodium salt Guanosine 5'-triphosphate (5'-GTP) trisodium salt is a G protein (G proteins) signaling activator and a high-energy precursor in the biosynthesis of nucleotide units in DNA and RNA. Guanosine 5'-triphosphate trisodium salt can promote myogenic cell differentiation by upregulating miRNA (miR133a, miR133b) and myogenic regulatory factor expression, and by inducing human myogenic precursor cells to release exosomes containing guanosine molecules. Guanosine-5'-triphosphate disodium salt holds promise for research in biosynthesis and skeletal muscle regeneration. Dec 26 2024
E8194 DiD perchlorate DiD is a long-chain carbocyanine dye. Carbocyanine dyes are widely used as Di to label cells, organelles, liposomes, viruses and lipoproteins. Dec 26 2024
E8195 Ro 48-8071 Ro 48-8071 is an inhibitor of OSC (Oxidosqualene cyclase) with IC50 of appr 6.5 nM. Dec 26 2024
E8196 E 2012 E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat. Dec 26 2024
E8197 Oxytocin acetate Oxytocin (α-Hypophamine) acetate is a pleiotropic, hypothalamic peptide known for facilitating parturition, lactation, and prosocial behaviors. Oxytocin acetate can function as a stress-coping molecule with anti-inflammatory, antioxidant, and protective effects especially in the face of adversity or trauma. Dec 26 2024
E8198 TG6-10-1 TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors. Dec 26 2024
E8199 GNE-140 racemate GNE-140 racemate is a racemate mixture of (R)-GNE-140 and (S)-GNE-140. GNE-140 racemate is a potent lactate dehydrogenase A (LDHA) inhibitor. Dec 26 2024
E8200 Epirubicin Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin inhibits DNA and RNA synthesis. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity. Dec 26 2024
E8201 Amifostine Amifostine (WR2721) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine protects cells from damage by scavenging oxygen-derived free radicals. Amifostine reduces renal toxicity and has antiangiogenic action. Dec 26 2024
E8202 Icatibant Icatibant (HOE-140) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively. Dec 26 2024
E8203 Forodesine Forodesine (BCX-1777) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine is a potent human lymphocyte proliferation inhibitor. Forodesine could induce apoptosis in leukemic cells by increasing the dGTP levels. Dec 26 2024
E8204 EPZ020411 EPZ020411 is a selective inhibitor of PRMT6 with an IC50 of 10 nM, has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 can be used for the research of cancer. Dec 26 2024
E8205 Guadecitabine Guadecitabine (SGI-110) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS). Dec 26 2024
E8206 CAY10650 CAY10650 is a highly potent cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC50 value of 12 nM. CAY10650 suppresses lipid droplets formation and PGE2 secretion. Dec 26 2024
E8207 TDCPP TDCPP is a chlorinated analog of tris(2,3-dibromopropyl)phosphate (Tris) which is one of the most detected organophosphorus flame retardants (OPFRs) in the environment. Dec 26 2024
E8208 Thrombin (MW 37kDa) Thrombin (MW 37kDa) is a Na+-activated, allosteric serine protease that plays opposing functional roles in blood coagulation. Thrombin recognition sequence and can be used to digest GST-tagged proteins. Dec 26 2024
E8209 Alvespimycin Alvespimycin (17-DMAG) is a potent inhibitor of Hsp90, binding to Hsp90 with an EC50 of 62 ± 29 nM. Dec 26 2024
E8210 RO-9187 RO-9187 is a potent inhibitor of HCV virus replication with an IC50 of 171 nM. RO-9187 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. Dec 26 2024
E8211 Pimavanserin Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively. Dec 26 2024
E8212 Minocycline Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect. Dec 26 2024
E8154 Pronase E (Activity ≥ 7000 U/g) Pronase E (Activity ≥ 7000 U/g) is a mixture of proteolytic enzymes that is obtained from Streptomyces griseus and could digest protein into individual amino acids. Dec 26 2024
E8215 Collagenase,Type II Collagenase, Type II is a microbially derived matrix metalloproteinases (MMPs) and zinc peptidase. Collagenase, Type II breaksdown collagens1, 3, 5, 7, 8, 10, fibronectin, gelatin, aggrecann. Dec 26 2024
E6033 Cilastatin sodium Dec 25 2024
E4664 Osimertinib dimesylate Dec 25 2024
E6043 Vidarabine phosphate Dec 25 2024
E1677 Glecirasib Dec 25 2024
E1583 MFI8 Dec 25 2024
E1927 PF-05251749（CK1-IN-2） Dec 24 2024
E4712 SDU-071 Dec 24 2024
E4779 DMB Dec 24 2024
E1930 AD-8007 Dec 24 2024
E1616 AZD8797( KAND567) Dec 24 2024
E6027 Ibuprofen sodium Dec 24 2024
S7899 CHZ868 Dec 24 2024
E6025 Palbociclib 2HCL Palbociclib 2HCL (PD-0332991 dihydrochloride), the dihydrochloride salt of Palbociclib, is a highly specific inhibitor of Cdk4 and Cdk6, with IC50 values of 11 nM and 16 nM, respectively. It is a potent antiproliferative agent against retinoblastoma (Rb)-positive tumor cells in vitro, inducing a selective G1 cell cycle arrest and reducing phosphorylation at Ser780 and Ser795 on the Rb protein. Dec 22 2024
E6002 Ledipasvir D-tartrate Ledipasvir D-tartrate (GS-5885 D-tartrate), the D-tartrate salt form of ledipasvir, is an inhibitor of the HCV NS5A, which is essential for the replication of the virus. It exhibits EC50 of 31 pM against GT1a and 4 pM against GT1b replicons. Dec 22 2024
E6029 Lenalidomide hemihydrate Lenalidomide hemihydrate (CC-5013 hemihydrate) is a potent inhibitor of TNF-alpha with a IC50 of 13 nM. It induces tyrosine phosphorylation of CD28 on T cells, which subsequently activates NF-κB. It acts as a ligand for the ubiquitin E3 ligase cereblon (CRBN), leading to the selective ubiquitination and degradation of the lymphoid transcription factors IKZF1 and IKZF3 through the CRBN-CRL4 ubiquitin ligase complex. Dec 22 2024
E4710 KHK-6 KHK-6 is a potent ATP-competitive inhibitor of HPK1 kinase activity with an IC50 value of 20 nM. It significantly enhances CD3/CD28-induced production of cytokines by downregulating the HPK1-SLP-76 signaling cascade in the TCR signaling pathway. Dec 22 2024
E4717 CP681301 CP681301 is a highly specific, brain-permeable inhibitor of Cdk5. It exhibits antiproliferative and anti-tumor activity by reducing stem cell marker expression, and cell proliferation in mouse xenografts ex vivo. Dec 22 2024
E6035 (R)-Propranolol hydrochloride (R)-Propranolol (hydrochloride) (Dexpropranolol hydrochloride) is a nonselective antagonist of beta-adrenergic receptor (β-adrenergic receptor (βAR) ) that competitively blocks the action of epinephrine (EPI) and norepinephrine (NE) on β1- and β2-adrenoreceptors (AR). It exhibits anti-neuroblastoma activity and is effective in combination therapies for relapsed and refractory neuroblastoma patients. Dec 22 2024
E1913 MZ-101 MZ-101 (GYS1-IN-2) is a potent small molecule inhibitor of Glycogen synthase 1(GYS1) with an IC50 value of 0.041 µM. By depleting muscle glycogen, MZ-101 treatment normalizes glycogen levels and corrects transcriptional and metabolic abnormalities in Pompe mice. Dec 22 2024
E4722 GNE-495 GNE-495 is a potent and selective inhibitor of MAP4K4 with an IC50 value of 3.7 nM. It demonstrates excellent potency and good Pharmacokinetics in in vivo efficacy in a retinal angiogenesis model. Dec 20 2024
E7566 (±)-Alliin (±)-Alliin is the main active component of garlic. (±)-Alliin is a putative inhibitor of the main protease of SARS-CoV-2 (Mpro)[1]. Dec 20 2024
E7822 ON-013100 ON-013100, an antineoplastic agent, acts a mitotic inhibitor that could inhibit Cyclin D1 expression. Dec 20 2024
E8077 ML218 ML218 is a potent, selective and orally active T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier[1]. Dec 20 2024
E7567 McN-A-343 McN-A-343 is a selective M1 muscarinic agonist that stimulates muscarinic transmission in sympathetic ganglia. McN-A-343 reduces inflammation and oxidative stress in an experimental model of ulcerative colitis[1][2]. McN-A-343 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 20 2024
E7823 Guluronic acid Guluronic acid (G2013), one of the organic building blocks of hyaluronic acid, is a nonsteroidal anti-inflammatory agent has favorable anti-inflammatory effect[1][2]. Dec 20 2024
E8078 Cibacron Blue 3G-A Cibacron Blue 3G-A is an anthraquinone dye, inhibits the R46 β-lactamase with a Ki value of 1.2 uM[1]. Dec 20 2024
E7568 LCMV gp33-41 LCMV gp33-41, the carboxyl-extended 11-aa-long peptide, is an lymphocytic choriomeningitis virus sequence restricted by MHC class I H-2Db molecules and presented to cytotoxic T lymphocytes[1]. Dec 20 2024
E7824 CaMKII-IN-1 CaMKII-IN-1 is a potent and highly selective CaMKII inhibitor with IC50 of 63 nM; significantly high selectivity against CaMKIV, MLCK, p38a, Akt1, and PKC.IC50 value: 63 nMTarget: CaMKII Dec 20 2024
E8079 Propargyl-PEG1-acid Propargyl-PEG1-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-CRBN PROTACs Ibrutinib(HY-10997)-based PROTAC 4 and PROTAC 5. PROTAC 5 causes the degradation of BTK and induces the degradation of CSK, LYN, and LAT2 at 10 μM[1]. Propargyl-PEG1-acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 20 2024
E7569 (2R)-Octyl-α-hydroxyglutarate (2R)-Octyl-α-hydroxyglutarate ((2R)-Octyl-2-HG) is a modified form of D-isomer 2-Hydroxyglutarate. Dec 20 2024
E7825 TLR1 TLR1 (compound 4a) is a low molecular weight, cell-penetrating Toll/IL-1 receptor/resistance (TIR) domain/BB-Loop mimic. TLR1 inhibits IL-1 receptor-mediated responses[1]. Dec 20 2024
E8080 Coronaridine Coronaridine, an iboga type alkaloid, inhibits the wnt signaling pathway by decreasing β-catenin expression[1]. Dec 20 2024
E7570 2-Iodomelatonin 2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1  over MT2[1]. 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues[1]. Dec 20 2024
E7826 TNF-α (10-36), human TNF-α (10-36), human is a peptide of human TNF-α. Dec 20 2024
E8081 BMS-582949 hydrochloride BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease[1]. Dec 20 2024
E7571 FPR Agonist 43 FPR Agonist 43 (compound 43) is a dual formyl peptide receptor 1 (FPR1) and formyl peptide receptor 2 (FPR2)/ALX agonist[1][2]. Dec 20 2024
E7827 KDM5-IN-1 KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM. Dec 20 2024
E8082 Terutroban Terutroban is a thromboxane-prostaglandin receptor antagonist. Dec 20 2024
E7572 IT1t dihydrochloride IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM. Dec 20 2024
E7828 Edelinontrine Edelinontrine (PF-04447943) is a potent inhibitor of human recombinant PDE9A (IC50=12 nM) with >78-fold selectivity, respectively, over other PDE family members (IC50>1000 nM). Dec 20 2024
E8083 I2906 I2906 showed antimycobacterial and cytotoxic activity against mycobacterium tuberculosis.IC50 Value: Target: AntibacterialUnder in vitro conditions, I2906 showed excellent antimycobacterial activities and low cytotoxicity. In a murine model infected with M. tuberculosis H37Rv, the reductions on bacterial loads of both lungs and spleen were statistically significant (p < 0.05) between I2906-treated mice and untreated controls after 4 weeks. Further, the colony-forming unit counts in the lungs were dramatically lower (p < 0.05) than that of isoniazid-treated mice by the addition of I2906 after 8 weeks. Moreover, survival rate was increased by I2906 treatment. For multidrug-resistant strain infection, bacterial counts were reduced significantl Dec 20 2024
E7573 Flagelin 22 Flagelin 22 (Flagellin 22), a fragment of bacterial flagellin, is an effective elicitor in both plants and algae[1][2][3]. Dec 20 2024
E7829 Sangivamycin Sangivamycin (NSC 65346), a nucleoside analog, is a potent inhibitor of protein kinase C (PKC) with an Ki of 10 μM. Sangivamycin has potent antiproliferative activity against a variety of human cancers[1][2]. Dec 20 2024
E8084 Trimethylamine N-oxide-d9 Trimethylamine N-oxide-d9 is the deuterium labeled Trimethylamine N-oxide. Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway[1][2][3]. Dec 20 2024
E7574 EGTA-AM EGTA-AM is a membrane permeable form of EGTA, can be passively loaded into cells to generate intracellular EGTA; EGTA-AM is also a Ca2+ chelator with slow chelating dynamics. Dec 20 2024
E7830 R(+)-Methylindazone R(+)-Methylindazone (R(+)-IAA-94) is a potent indanyloxyacetic acid blocker of epithelial chloride channels. R(+)-Methylindazone inhibits Nef-sdAb19 (single-domain antibody) interaction and binds to negative factor (Nef)[1][2][3]. Dec 20 2024
E8085 YK11 YK11 is a partial agonist of androgen receptor, with osteogenic activity. Dec 20 2024
E7575 MAFP MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase. Dec 20 2024
E7831 Doxorubicinone Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin[1]. Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Dec 20 2024
E8086 Lupeol acetate Lupeol acetate is a derivative of Lupeol. Lupeol acetate is an anti-inflammatory, antibacterial, anti-trypanosomic and anticancer agent with oral activity. Lupeol acetate significantly improves the symptoms of rheumatoid arthritis by down-regulating the expression of inflammatory cytokines and osteoclast production. Lupeol acetate inhibits spermatogenesis in male rats and eventually led to infertility[1][2][3][4]. Dec 20 2024
E7576 Ubiquitin Isopeptidase Inhibitor I, G5 Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively. Dec 20 2024
E7832 trans-AUCB trans-AUCB (t-AUCB) is a potent, orally active and selective soluble epoxide hydrolase (sEH) inhibitor with IC50s of 1.3 nM, 8 nM, 8 nM for hsEH, mouse sEH and rat sEH, respectively. trans-AUCB has anti-glioma activity[1][2]. Dec 20 2024
E8087 NEP(1-40) NEP(1-40) is a Nogo-66 receptor (NgR) antagonist peptide, reversing the injury-induced shift in distribution of microglia morphologies by limiting myelin-based inhibition[1]. Dec 20 2024
E7577 Benfluorex hydrochloride Benfluorex hydrochloride (JP-992 hydrochloride) is a hepatic nuclear factor 4 alpha (HNF4α) activator. Dec 20 2024
E7833 N-alpha-Tosyl-L-lysine chloromethyl ketone hydrochloride N-alpha-Tosyl-L-lysine chloromethyl ketone (TLCK), a trypsin like protease inhibitor, sensitizes HeLa cells to Fas-mediated cell death. Dec 20 2024
E8088 S-23 S-23 is an orally active selective androgen receptor modulator (SARM) with a Ki of 1.7 nM. S-23 induces androgen receptor (AR)-mediated transcriptional activation in CV-1 cells. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats[1][2]. Dec 20 2024
E7578 (-)-Indolactam V (-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and Kds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity. Dec 20 2024
E7834 Givinostat hydrochloride Givinostat (ITF-2357) hydrochloride is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively[1][2][3]. Dec 20 2024
E8089 Chicanine Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity[1]. Dec 20 2024
E7579 Carboxyamidotriazole Carboxyamidotriazole (L-651582) is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole shows anti-tumor, anti-inflammatory and antiangiogenic effects[1][2]. Dec 20 2024
E7835 Ilacirnon CCX140 (CCX140-B) is a potent CCR2 antagonist. Dec 20 2024
E8090 Esterase, pig liver Esterase, pig liver (CESs), namely carboxylate hydrolases, are widely distributed in nature, commonly found in mammalian liver, and often used in biochemical research. Esterase catalyzes the hydrolysis of a variety of endogenous and exogenous substrates, including esters, thioesters, carbamates, and amides, hydrolyzing carboxylic acid esters to the corresponding alcohols and carboxylic acids[1]. Dec 20 2024
E7580 11beta-Hydroxyprogesterone 11beta-Hydroxyprogesterone is a potent inhibitors of 11β-Hydroxysteroid dehydrogenase; also activates human mineralocorticoid receptor in COS-7 cells with an ED50 of 10 nM. Dec 20 2024
E7836 TC14012 TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity[1][2]. Dec 20 2024
E8091 CIQ CIQ is a subunit-selective potentiator of NMDA receptors containing the NR2C or NR2D subunit. IC50 value: 2.7 μM (EC50, for NR2C) and 2.8 μM (EC50, NR2D)Target: NMDA receptorCIQ increases channel opening frequency of recombinant NR2Cor NR2D containing receptors by two-fold (EC50 = 2.7 and 2.8 μM, respectively), with no effect on NR2A or NR2B subtypes. CIQ does not alter the EC50 values for glutamate or glycine on channel opening. CIQ increases channel opening efficiency and enhances NMDA receptor responses. CIQ reduces associated behaviours in schizophrenia models and potentially enhances dopamine release in Parkinson's disease models. Dec 20 2024
E7581 2-Methoxyestrone 2-Methoxyestrone is a methoxylated catechol estrogen and metabolite of estrone, with a pKa of 10.81. Dec 20 2024
E7837 2F-Peracetyl-Fucose 2F-Peracetyl-Fucose (1,3,4-Tri-O-acetyl-2-deoxy-2-fluoro-L-fucopyranos) acts as a potent fucosyltransferase (FUT) inhibitor[1]. Dec 20 2024
E8092 MRS-1706 MRS-1706 is a potent and selective adenosine A2B receptor inverse agonist. MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1 and A3 receptors respectively. MRS-1706 blocks adenosine-mediated cAMP induction[1][2]. Dec 20 2024
E7582 (2-Chloropyridin-4-yl)methanamine hydrochloride (2-Chloropyridin-4-yl)methanamine hydrochloride is a selective LOXL2 inhibitor with an IC50 of 126 nM. Dec 20 2024
E7838 Iodipamide Iodipamide is a tri-iodinated benzoate derivative and ionic dimeric contrast agent used in diagnostic imaging. Dec 20 2024
E8093 Broflanilide Broflanilide is a potential insecticide and metabolized to Desmethyl-Broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA Receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM[1]. Dec 20 2024
E7583 RR6 RR6 is a potent, selective, reversible, competitive and orally active vanin inhibitor with an IC50 of 540 nM for recombinant vanin-1. RR6 also potently inhibits human, bovine and rat serum pantetheinase with IC50 values of 40 nM, 41 nM and 87 nM, respectively[1]. Dec 20 2024
E7839 LPA2 antagonist 1 LPA2 antagonist 1 is a LPA2 antagonist with an IC50 of 17 nM. Dec 20 2024
E8094 Resveratroloside Resveratroloside (Resveratrol glycoside) is a competitive inhibitior of α-glucosidase with an IC50 of 22.9 μM. Resveratroloside has the ability to regulate PBG (postprandial blood glucose) levels. Resveratroloside exhibits cardioprotective effect[1][2]. Dec 20 2024
E7584 Retaspimycin Retaspimycin is a potent inhibitor of Hsp90, with EC50s of 119 nM for both Hsp90 and Grp9. Dec 20 2024
E7840 EF24 EF24 is a curcumin analogue with greater anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK[1][2]. Dec 20 2024
E8095 LY450108 LY450108 is a potent AMPA receptor potentiator. LY450108 has the potential for depression and Parkinson's disease research[1][2][3][4]. Dec 20 2024
E7585 10,12-Tricosadiynoic acid 10,12-Tricosadiynoic acid is a highly specific, selective, high affinity and orally active acyl-CoA oxidase-1 (ACOX1) inhibitor. 10,12-Tricosadiynoic acid can treat high fat diet- or obesity-induced metabolic diseases by improving mitochondrial lipid and ROS metabolism[1]. 10,12-Tricosadiynoic acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 20 2024
E7841 Kisspeptin-54(human) Kisspeptin-54(human) (Metastin(human)) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) hinders tumor metastasis and stimulates gonadotropin secretion[1][2]. Dec 20 2024
E8096 NF449 octasodium NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a Gsα-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs[1][2]. Dec 20 2024
E7586 R121919 R121919 (NBI30775) is a potent and selective CRF1R antagonist with a Ki of 2 to 5 nM. R121919 has antidepressant and anxiolytic effects. R121919 alleviates defensive withdrawal in rats[1][2][3]. Dec 20 2024
E7842 Rhodiolin Rhodiolin is a flavonoid isolated from Rhodiola rosea[1]. Dec 20 2024
E8097 Syzalterin Syzalterin is an inhibitor of NO production with an IC50 of 1.87 μg/mL. Dec 20 2024
E7587 ITI-214 ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions[1][2]. Dec 20 2024
E7843 Hernandezine Hernandezine (Hernandesine) is isolated from Thalictrum glandulosissimum[1]. Dec 20 2024
E8098 BIIE-0246 BIIE-0246 is a potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist, with an IC50 of 15 nM. Dec 20 2024
E7588 Cytidine-5'-triphosphate Cytidine 5′-triphosphate (Cytidine triphosphate; 5'-CTP) is a nucleoside triphosphate and serves as a building block for nucleotides and nucleic acids, lipid biosynthesis. Cytidine triphosphate synthase can catalyze the formation of cytidine 5′-triphosphate from uridine 5′-triphosphate (UTP). Cytidine 5′-triphosphate is an essential biomolecule in the de novo pyrimidine biosynthetic pathway in T. gondii[1]. Dec 20 2024
E7844 Tpl2 Kinase Inhibitor 1 Tpl2 Kinase Inhibitor 1 is a 3-pyridylmethylamino analog, and is a selective Tpl2 inhibitor (IC50=50 nM). Tpl2 consists of COT kinase and MAP3K8. Tpl2 Kinase Inhibitor 1 plays an important role in the regulation of the inflammatory response and the progression of some cancers[1][2]. Dec 20 2024
E8099 Trofosfamide Trofosfamide is an orally bioavailable oxazaphosphorine derivative with antineoplastic activity[1]. Dec 20 2024
E7589 α-Bungarotoxin α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM[1][2]. Dec 20 2024
E7845 Actinomycin X2 Actinomycin X2 (Actinomycin V), produced by many Streptomyces sp., shows strong inhibition of MRSA with a minimum inhibitory concentration (MIC) value of 0.25 μg/mL. Actinomycin X2 can be used for cancer and bacterial infection[1][2]. Dec 20 2024
E8100 THIP THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 µM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders[1][2][3]. Dec 20 2024
E1890 A-967079 A-967079 is a selective antagonist of TRPA1 receptor with IC50 values of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively. A-967079 decreases the responses of wide dynamic range (WDR), and nociceptive specific (NS) neurons following noxious pinch stimulation and high-intensity mechanical stimulation in rats. It demonstrates strong penetration into the central nervous system (CNS). Dec 20 2024
E5661 3,5-O-Dicaffeoylquinic acid Dec 20 2024
E7590 OTS514 OTS514 is a highly potent TOPK inhibitor with an IC50 of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells[1]. OTS514 induces cell cycle arrest and apoptosis[2]. Dec 20 2024
E7846 Soblidotin Soblidotin (Auristatin PE) is a novel synthetic Dolastatin 10 derivative and inhibitor of tubulin polymerization. Dec 20 2024
E8101 AC-262536 AC-262536 is a selective and non-steroidal androgen receptor modulators (SARMs) with beneficial anabolic effects. AC-262536 exhibits potent agonist activity at the androgen receptor, with an affinity in the low nanomolar range (1-10 nM)[1]. Dec 20 2024
E7591 tBID tBID is a selective inhibitor of homeodomain-interacting protein kinase 2 (HIPK2) with an IC50 of  0.33 µM. Dec 20 2024
E7847 PETCM PETCM is an activator of caspase-3 and acts as an cytochrome c (cyto c)-dependent manner. PETCM promotes Apaf-1 oligomerization and induces cell apoptosis in HeLa cells[1][2]. Dec 20 2024
E8103 Fuscoside Fuscoside (OPC-21268) is an orally effective, nonpeptide, vasopressin V1 receptor antagonist with an IC50 of 0.4 μM. Dec 20 2024
E7592 T807 T807 a novel tau positron emission tomography (PET) tracer. Dec 20 2024
E7848 Otamixaban Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.IC50 value:Target: Factor Xa Otamixaban is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa. In vivo experiments have demonstrated that Otamixaban is highly efficacious in rodent, canine and porcine models of thrombosis. In addition, recent clinical findings indicate that Otamixaban is efficacious, safe and well tolerated in humans and therefore has considerable potential for the treatment of acute coronary syndrome. This review article chronicles the discovery a Dec 20 2024
E8104 Fingolimod phosphate Fingolimod phosphate (FTY720 phosphate) is an orally active sphingosine 1-phosphate (S1P) receptor agonist. Fingolimod phosphate can promote the neuroprotective effects of microglia. Fingolimod phosphate can be used for the research of multiple sclerosis and neurologic diseases[1]. Dec 20 2024
E7593 EPZ011989 EPZ011989 is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ011989 shows robust methyl mark inhibition and anti-tumor activity. EPZ011989 can be used for the research of various cancers[1]. EPZ011989 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 20 2024
E7849 Haloperidol hydrochloride Haloperidol hydrochloride is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic. Dec 20 2024
E8105 3-Epioleanolic acid 3-Epioleanolic acid is an active component of Verbena officinalis Linn, with anti-inflammatory activity[1]. Dec 20 2024
E7594 FM1-43 FM1-43 is a very lipophilic, water-soluble styrene dyes, can specifically bind to cell membranes and inner membrane organelles to produce fluorescence. FM1-43 is widely used in endocytic and exospic membrane structure markers. Dec 20 2024
E7850 AZP-531 AZP-531 is an analogue of unacylated ghrelin designed to improve glycaemic control and reduce weight. Dec 20 2024
E8106 Capillarisin Capillarisin, as a constituent from Artemisiae Capillaris herba, is found to exert anti-inflammatory and antioxidant properties. Capillarisin can be used for the research of asthma-mediated complications and can be a potential neuroprotectant against bupivacaine-induced neurotoxicity[1][2][3]. Dec 20 2024
E7595 ICA-121431 ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 μM). Dec 20 2024
E7851 GSK2256294A GSK2256294A (GSK 2256294) is a selective and orally active inhibitor of soluble epoxide hydrolase (sEH). GSK2256294A inhibits recombinant human sEH, rat sEH orthologs and murine sEH orthologs with IC50s of 27, 61 and 189 pM, respectively. GSK2256294A can be used for the research of chronic obstructive pulmonary disease (COPD) and cardiovascular disease[1]. Dec 20 2024
E8107 Tubulysin A Tubulysin A (TubA) is an anticancer and antiangiogenic agent with anti-microtubule, anti-mitosis and anti-proliferative activity against a variety of cancer cells with IC50 values in the pmol range. It can induce apoptosis of cancer cells and has no effect on normal cells. Tubulysins are a group of potent cytotoxins consisting of nine members (A-I). Tubulysin A can synthesize ADC as ADC Cytotoxin[1][2][3][4]. Dec 20 2024
E7596 BIX02189 BIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM. Dec 20 2024
E7852 CKI-7 CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases[1][2][3][4]. Dec 20 2024
E8108 PAR-2 (1-6) (human) PAR-2 (1-6) (human) (SLIGKV), a peptide ligand, is a PAR-2 agonist[1]. Dec 20 2024
P1208 PMX 205 acetate

PMX 205 acetate is a cyclic hexapeptide that acts as a potent C5a receptor (C5aR, CD88) antagonist with an IC50 of 31 nM.

 Dec 20 2024
E7597 16α-Hydroxyestrone 16α-Hydroxyestrone (16αOHE) is a major Estradiol metabolite. 16α-Hydroxyestrone (16αOHE) can be used for the research of metabolic disease[1]. Dec 20 2024
E7853 γ-L-Glutamyl-L-alanine γ-L-Glutamyl-L-alanine, composed of gamma-glutamate and alanine, is a proteolytic breakdown product of larger proteins. γ-L-Glutamyl-L-alanine is a natural substrate of the γ-Glutamylcyclotransferase. γ-L-Glutamyl-L-alanine is a positive modulator of calcium-sensing receptor (CaR) function[1][2][3][4]. Dec 20 2024
E8109 4-Hydroxyestrone 4-Hydroxyestrone (4-OHE1), an estrone metabolite, has strong neuroprotective effect against oxidative neurotoxicity. 4-Hydroxyestrone increases cytoplasmic translocation of p53 resulting from SIRT1-mediated deacetylation of p53. 4-Hydroxyestrone has little estrogenic activity[1]. Dec 20 2024
E7598 UNC0321 UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 63 pM and with assay-dependent IC50 values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC50 values of 15-23 nM. UNC0321 has anti-apoptotic activity and has potential application in diabetic vascular complications[1][3]. Dec 20 2024
E7854 Iberin Iberin (NSC 321801), a sulfoxide analogue of sulforaphane, is a naturally occurring member of isothiocyanate family. Iberin inhibits cell survival with an IC50 of 2.3 μM in HL60 cell. Iberin induces apoptosis. Dec 20 2024
E8110 Trofinetide Trofinetide (NNZ-2566), a synthetic analogue of the endogenous N-terminus tripeptide, Glycine-Proline-Glutamate (GPE), has been shown to be neuroprotective in animal models of brain injury. Dec 20 2024
E4972 Efaproxiral Efaproxiral(RSR13) is a synthetic allosteric modifier of haemoglobin that reduces its oxygen binding affinity, facilitating oxygen release. This increases the whole blood P50 and tissue partial pressure of oxygen (Po2), enhancing oxygen delivery to tissues and improving oxygenation in hypoxic tumors. Dec 20 2024
E7599 SB-334867 SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively[1]. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo[2][3]. Dec 20 2024
E7855 Propoxycaine hydrochloride Propoxycaine hydrochloride inhibits voltage-gated sodium channels, and thereby inhibits the ionic flux required for the initiation and conduction of impulses. Propoxycaine hydrochloride application can lead to a loss of sensation. Dec 20 2024
E8111 TPh A TPh A (Triphenyl Compound A) is a potent inhibitor of the nuclear protein pirin and binds specifically to pirin with a Ki of 0.6 uM. TPh A disrupts the formation of the bcl3–pirin complex. TPh A can be used as a novel small molecule tool to regulate pirin in cells[1]. Dec 20 2024
E7600 Exisulind Exisulind is an inactive metabolite of the nonsteroidal, anti-inflammatory agent sulindac[1]. Exisulind inhibits aldose reductase with an IC50 of 367 nM in vitro and may contribute to the beneficial pharmacological effects of sulindac on type 2 diabetic complications[2]. Dec 20 2024
E7856 Kuwanon A Kuwanon A is a flavone derivative isolated from the root barks of the mulberry tree (Morus alba L.); inhibits nitric oxide production with an IC50 of 10.5 μM. Dec 20 2024
E8112 VKGILS-NH2 VKGILS-NH2 is a reversed amino acid sequence control peptide for SLIGKV-NH2 (protease-activated receptor 2 (PAR2) agonist). VKGILS-NH2 has no effect on DNA synthesis in cells[1][2]. Dec 20 2024
E7601 Pyridoxylamine Pyridoxylamine is an advanced glycation end production (AGEs) and lipoxidation end products (ALEs) inhibitor, to protect against diabetes-induced retinal vascular lesions. Dec 20 2024
E7857 Fibrinogen-Binding Peptide Fibrinogen-Binding Peptide (designed by anticomplementarity hypothesis) is a presumptive peptide mimic of the vitronectin binding site on the fibrinogen receptor. Fibrinogen-Binding Peptide binds fibrinogen and inhibits both the adhesion of platelets to fibrinogen and platelet aggregation, and also inhibits the adhesion of platelets to vitronectin[1]. Dec 20 2024
E8113 L-Palmitoylcarnitine chloride L-Palmitoylcarnitine chloride, a long-chain acylcarnitine and a fatty acid metabolite, accumulates in the sarcolemma and deranges the membrane lipid environment during ischaemia. L-Palmitoylcarnitine chloride inhibits KATP channel activity, without affecting the single channel conductance, through interaction with Kir6.2[1]. Dec 20 2024
E7602 Otenabant Otenabant is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor. Dec 20 2024
E7858 ABT-639 ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker. Dec 20 2024
E8114 hPGDS-IN-1 hPGDS-IN-1 is a hPGDS inhibitor ,with IC50 of 12 nM in the Fluorescence Polarization Assay or the EIA assay.IC50 value: 12 nMTarget: hPGDSThe detailed information please refer to WO2011044307A1 and WO2010080563A2 Dec 20 2024
E7603 Furamidine dihydrochloride Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent[1][2][3]. Dec 20 2024
E7859 Cinaciguat Cinaciguat is an activator of guanylate cyclase (sGC), and used for acute decompensated heart failure. Dec 20 2024
E8115 Piperacetazine Piperacetazine is an antipsychotic prodrug, used forschizophrenia. Dec 20 2024
E7604 GSK-3β inhibitor 1 GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy, with an IC50 of 4.9 nM[1]. Dec 20 2024
E7860 Estradiol-d4 Estradiol-d4 is the deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway[1][2][3]. Dec 20 2024
E8116 DOTA-NHS-ester DOTA-NHS-ester is a linker for affibody molecules and is applied in small animals PET, SPECT, and CT. DOTA-NHS-ester can be used to label radiotherapeutic agents or imaging probes for the detection of tumors[1]. Dec 20 2024
E7605 Tecalcet Hydrochloride Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca2+[1][2][3]. Dec 20 2024
E7861 Tinoridine Tinoridine (Y-3642) is an orally active non-steroidal anti-inflammatory agent with potent antiperoxidative ability and radical scavenger activity. Tinoridine acts function by inhibiting COX enzyme, involves in hepatotoxicity inhibition. [1][2][3]. Dec 20 2024
E8117 3,4-Dihydroxybenzylamine hydrobromide 3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) is an improved dopamine analog cytotoxic and inhibits DNA polymerase activity in melanoma cells[2]. 3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) displays growth inhibitory activity in melanoma cell lines with varying degrees of tyrosinase activity[2]. Dec 20 2024
E7606 Pyridoxal isonicotinoyl hydrazone Pyridoxal isonicotinoyl hydrazone (PIH) is a lipophilic, tridentate Fe-chelating agent that shows high Fe chelation efficacy[1]. Dec 20 2024
E7862 G3-C12 G3-C12 is a galectin-3 binding peptide, with Kd of 88 nM, and shows anticancer activity. Dec 20 2024
E8118 BRD9876 BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research[1][2][3][4]. Dec 20 2024
E1793 TC-E5002(KDM2/7-IN-1) TC-E5002(KDM2/7-IN-1) is a selective inhibitor of histone demethylase KDM2/7 subfamily with IC50s of 6.8, 0.2, and 1.2 µM for KDM2A, KDM7A, and KDM7B, respectively. It is selective for the KDM2/7 subfamily over KDM4A, KDM4C, KDM5A, and KDM6A/UTX with IC50s of >120, 83, 55, and 100 µM, respectively. It exhibits antiproliferative activity, indicating its potential as an anticancer agent. Dec 20 2024
E7607 MMAE-d8 MMAE-d8 is a deuterated labeled MMAE, a potent mitotic inhibitor and a tubulin inhibitor. Dec 20 2024
E7863 Noladin ether Noladin ether is a potent and selective agonist of cannabinoid CB1 receptor, with a Ki of 21.2 nM. Noladin ether can cause hypothermia, intestinal immobility, and mild antinociception[1]. Dec 20 2024
E8119 Mifamurtide Mifamurtide (MTP-PE), an analog of the muramyl dipeptide (MDP), is a nonspecific immunomodulator by stimulating the immune response activating macrophages and monocytes. Mifamurtide is a specific ligand for NOD2 and acts as an insulin sensitizer. Mifamurtide has potential for use in rare disease and osteosarcoma research[1][2][3]. Dec 20 2024
E7608 MK-2894 MK-2894 is a potent, selective, orally active and high affinity (Ki=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC50=2.5 nM). MK-2894 possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis[1][2]. Dec 20 2024
E7864 GNE-272 GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300[1]. Dec 20 2024
E8120 Sibofimloc Sibofimloc (Antibiotic-202) is a first-in-class, gut-restricted, orally active FimH adhesion inhibitor extracted from patent WO2014100158A1, Compound Example 202. Sibofimloc has anti-bacterial infective activity. Sibofimloc is developed for inflammatory bowel disease (IBD)[1][2]. Dec 20 2024
E7609 USP7/USP47 inhibitor USP7/USP47 inhibitor is a selective ubiquitin-specific protease 7/47 (USP7/USP47) inhibitor, with EC50s of 0.42 μM and 1.0 μM, respectively. Dec 20 2024
E7865 MnTBAP chloride MnTBAP chloride is a superoxide dismutase (SOD) mimetic and peroxynitrite scavenger. MnTBAP chloride is a manganic porphyrin complex and has anti-oxidative property. MnTBAP chloride mediates anti-inflammatory effects through upregulation of BMPR-II and inhibition of the NFκB signaling. MnTBAP chloride has the potential for the fibrotic response in chronic kidney diseases (CKDs) research[1][2]. Dec 20 2024
E8121 Peanut Oil Peanut Oil can be used as an excipient. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs[1]. Dec 20 2024
E7610 JNJ16259685 JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM. Dec 20 2024
E7866 Hycanthone Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent[1]. Dec 20 2024
E8122 Folitixorin Folitixorin (5,10-methylenetetrahydrofolate) is a cofactor and an analog of leucovorin. Folitixorin is a promising agent for modulation of 5-FU cytotoxicity in adjuvant cancer research[1][2]. Dec 20 2024
E7611 HET0016 HET0016 is a potent and selective 20-hydroxyeicosatetraenoic acid (20-HETE) synthase inhibitor, with IC50 values of 17.7 nM, 12.1 nM and 20.6 nM for recombinant CYP4A1-, CYP4A2- and CYP4A3-catalyzed 20-HETE synthesis, respectively. HET0016 also is a selective CYP450 inhibitor, which has been shown to inhibit angiogenesis and tumor growth[1][2]. Dec 20 2024
E7867 Propargyl-C1-NHS ester Propargyl-C1-NHS ester is a nonclaevable linker for antibody-agent-conjugation (ADC). Propargyl-C1-NHS ester is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 20 2024
E8123 Methyl pyropheophorbide-a Methyl pyropheophorbide-a (Pyropheophorbide-a methyl ester), a chlorophyll-a derivative, is a potent photosensitizer that can be used in photodynamic therapy (PDT) of cancer. Methyl pyropheophorbide-a has photodynamic activity and can induce apoptosis and inhibit tumor growth[1][2]. Dec 20 2024
E7612 Z-Ala-Ala-Asn-AMC Z-Ala-Ala-Asn-AMC (Cbz-Ala-Ala-Asn-AMC) is the legumain substrate. Overexpressed legumain in 293 HEK-Leg cells potently cleaved CBZ-Ala-Ala-Asn-AMC[1]. Dec 20 2024
E7868 Lucifer Yellow CH dilithium salt Lucifer Yellow CH dilithium salt is a high-intensity fluorescent probe containing free hydrazyl groups. Lucifer Yellow CH can react with fatty aldehydes at room temperature. Lucifer Yellow CH serves as a biological tracer to monitor neuronal branching, regeneration, gap junction detection and characterization, and selective ablation of cells after aldehyde fixation. Lucifer yellow CH displays the maximum excitation/emission of 430 nm/540 nm, respectively[1][2]. Dec 20 2024
E8124 N6-(4-Hydroxybenzyl)adenosine N6-(4-Hydroxybenzyl)adenosine is a inhibitor of platelet aggregation induced in vitro by collagen and their activity range was demonstrated (IC50: 6.77-141 μM). IC50 value: 6.77-141 μMTarget: P2Y12receptorAnti-aggregation activity of N6-(4-Hydroxybenzyl)adenosine could involve an interaction with the P2Y12receptor binding site. Dec 20 2024
E7613 L-655708 L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (Ki=0.45 nM). Dec 20 2024
E7869 Dorzolamide Dorzolamide (L671152) is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity[1]. Dec 20 2024
E8125 3-Deoxysappanchalcone 3-Deoxysappanchalcone is a naturally-occurring chalcone compound isolated from Caesalpinia sappan L. (Leguminosae), which possesses anti-allergic, antiviral, anti-inflammatory and antioxidant activities. 3-Deoxysappanchalcone exerts anti-inflammatory activity via induce heme oxygenase-1 (HO-1) expression by activating the AKT/mTOR pathway in murine macrophages. 3-Deoxysappanchalcone also exhibits anti-influenza virus activity (H3N2, IC50 = 1.06 μM)[1][2]. Dec 20 2024
E7614 NBI-74330 NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of (125I)CXCL10 and (125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively. Dec 20 2024
E7870 SR 49059 SR 49059 (SR-49059) is a potent, orally active, selective vasopressin V1a antagonist with a Ki vaule of 1.4 nM[1]. Dec 20 2024
E8126 TP-024 TP-024 (FTBMT) is a selective GPR52 agonist with an EC50 of 75 nM[1]. TP-024 has antipsychotic and procognitive properties[2]. Dec 20 2024
E7615 CALP3 CALP3, a Ca2+-like peptide, is a potent Ca2+ channel blocker that activates EF hand motifs of Ca2+-binding proteins. CALP3 can functionally mimic increased [Ca2+]i by modulating the activity of Calmodulin (CaM), Ca2+ channels and pumps. CALP3 has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia[1][2]. Dec 20 2024
E7871 GPP78 GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects[1][2]. Dec 20 2024
E8127 Licogliflozin Licogliflozin is a sodium glucose cotransporter (SGLT1 and SGLT2) inhibitor. Dec 20 2024
E7616 Ampkinone Ampkinone is an indirect AMP-activated protein kinase (AMPK) activator. Dec 20 2024
E7872 Isoxanthohumol Isoxanthohumol is a prenylflavonoid from hops and beer. Isoxanthohumol exhibits an antiproliferative activity against several human cancer cell lines. Isoxanthohumol inhibits the development of lung metastatic foci in tumor-challenged animals. Isoxanthohumol shows an antiviral activity towards herpes viruses (HSV1 and HSV2) and bovine viral diarrhea virus (BVDV)[1][2]. Dec 20 2024
E8128 Lancerin Lancerin, isolated from the root bark of Cudraniu cochinchinensis, possesses anti-lipid peroxidation[1]. Dec 20 2024
E6031 Tipiracil Tipiracil [TPI (freebase)] is a potent inhibitor of thymidine phosphorylase. It increases exposure to its co-administered drug by inhibiting its metabolism through thymidine phosphorylase, enhancing its therapeutic effects and is used as adjunct therapy for certain gastric and colorectal cancers. Dec 20 2024
E7617 Activated Protein C (390-404), human Activated Protein C (390-404), human is a peptide of the activated protein C (a vitamin K-dependent serine protease), potently inhibits APC anticoagulant activity[1]. Dec 20 2024
E7873 Desmethylxanthohumol Desmethylxanthohumol is a prenylated hydroxychalcone isolated from hop cones (Humulus lupulus L.). Desmethylxanthohumol is a powerful apoptosis inducing agent. Desmethylxanthohumol has antiplasmodial, antiproliferative, and antioxidant bioactivities[1][2]. Dec 20 2024
E8129 YM022 YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively[1]. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo[3]. Dec 20 2024
E1562 Atrasentan hydrochloride Atrasentan hydrochloride (ABT-627 hydrochloride) is a selective endothelin A receptor antagonist with an IC50 of 0.0551 nM for ETA[1]. Dec 20 2024
E7618 CCR2 antagonist 4 CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM[1]. Dec 20 2024
E7874 Xanthohumol D Xanthohumol D, isolated from hops, is an inhibitor of quinone reductase-2 (QR-2) with the IC50 value of 110 μM, and binds to the active site of QR-2. Xanthohumol D shows antiproliferative activity on human cancer cell lines in vitro[1][2]. Dec 20 2024
E8130 TAT-14 TAT-14 is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1[1]. Dec 20 2024
E5097 Tribuloside Dec 20 2024
P1157 Z-FY-CHO Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific cathepsin L (CTSL) inhibitor[1][2]. Dec 20 2024
E7619 VH032 VH032 is a VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. VH032 is a VHL/HIF-1α interaction inhibitor with a KdPROTACs[1][2][3]. Dec 20 2024
E7875 Gypenoside LXXV Gypenoside LXXV, isolated from Gynostemma pentaphyllum, is one of the deglycosylated shapes of ginsenoside Rb1. Gypenoside LXXV significantly reduces cancer cell viability and displays an anti-cancer effect[1]. Dec 20 2024
E8131 RI-2 RI-2 is a reversible RAD51 inhibitor, with an IC50 of 44.17 μM, and specifically inhibits homologous recombination repair in human cells. Dec 20 2024
E1592 Gepotidacin Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor. Dec 20 2024
E7620 Dibutyryl-cGMP sodium Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [3H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K+ channels[1][2][3]. Dec 20 2024
E7876 GPRP acetate GPRP acetate (Gly-Pro-Arg-Pro acetate) is a fibrin polymerization inhibitor that inhibits the interaction of fibrinogen with the platelet membrane glycoprotein IIb/IIIa complex (GPIIb/IIIa)[1][2][3]. Dec 20 2024
E8132 SRT3109 SRT3109 is an antagonist of CXCR2, with a pIC50 of 8.2, and used in the research of chemokine mediated diseases. Dec 20 2024
E8102 MRT68921 MRT68921 is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively. Dec 20 2024
E7621 5,6-Dihydrouridine 5,6-Dihydrouridine is a modified base found in conserved positions in the D-loop of tRNA in Bacteria, Eukaryota, and some Archaea. Dec 20 2024
E7877 MLCK inhibitor peptide 18 MLCK inhibitor peptide 18 is a myosin light chain kinase (MLCK) inhibitor with an IC50 of 50 nM, and inhibits CaM kinase II only at 4000-fold higher concentrations. Dec 20 2024
E8133 Rhapontigenin 3'-O-glucoside Rhapontigenin 3'-O-glucoside is a derivative of Rhapontigenin. Rhapontigenin is a potent inactivator of human P450 1A1 and is a good candidate for a cancer chemopreventive agent[1]. Dec 20 2024
E1278 ACHP Hydrochloride ACHP Hydrochloride (IKK-2 Inhibitor VIII) is a highly potent and selective IKK-β inhibitor with an IC50 of 8.5 nM. Dec 20 2024
E7622 LP-533401 LP-533401 is a Tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut. Dec 20 2024
E7878 N-Bis(2-hydroxypropyl)nitrosamine N-Bis(2-hydroxypropyl)nitrosamine is an agent with carcinogenic activity. Dec 20 2024
E8134 Y-26763 Y-26763 is a K+ channel opener and active metabolite of Y-27152[1]. Y-26763 is an ATP-sensitive K+ (KATP) channel activator[2]. Dec 20 2024
S7882 BQ-788 BQ-788 is a potent, selective ETB receptor antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, poorly inhibiting the binding to ETA receptors in human neuroblastoma cell line SK-N-MC cells with IC50 of 1300 nM[1]. Dec 20 2024
E7623 Eglumegad Eglumegad (LY354740) is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 nM and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively. Dec 20 2024
E7879 LY367385 LY367385 is a highly selective and potent mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibiting of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 μM for mGlu5a. LY367385 has neuroprotective, anticonvulsant and antiepileptic effects[1][2]. Dec 20 2024
E8135 P-1075 P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation[1]. P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts[2]. Dec 20 2024
E7624 BMS-564929 BMS-564929 is an androgen receptor (AR) agonist, binds to androgen receptor (AR) with a Ki of 2.11±0.16 nM. Dec 20 2024
E7880 Thiodigalactoside Thiodigalactoside (TDG) is an orally active and potent galectin (GAL) inhibitor with Kd values of 24 μM, 49 μM for GAL1 and GAL3, respectively[1]. Thiodigalactoside, a non-metabolizable disaccharide, has anti-inflammatory and anti-cancer activity. Thiodigalactoside dramatically reduces body weight gain in diet-induced obese rats[2]. Dec 20 2024
E8136 BMS-779788 BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ. Dec 20 2024
E4631 DETA NONOate DETA NONOate (NOC 18) is an exogenous nitric oxide (NO) donor. DETA NONOate shows a slow release normal amounts of NO and long-acting[1][2]. Dec 20 2024
E7625 NSC781406 NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα. Dec 20 2024
E7881 Nifedipine-d6 Nifedipine-d6 is deuterium labeled nifedipine, and nifedipine is a potent calcium channel blocker. Dec 20 2024
E8137 Droloxifene Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats [1][2][3]. Dec 20 2024
E4864 Pentamidine Pentamidine (MP-601205) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities[1][2][3][4]. Dec 20 2024
E7626 6''-O-Acetylglycitin 6''-O-Acetylglycitin, a acetyl glucoside, is one of the isoflavone isomer in soybeans, shows various extents of content reduction dependent on storage temperature, packaging condition, and its isoflavone isomer kind[1]. Dec 20 2024
E7882 Ro 08-2750 Ro 08-2750 is a non-peptide and reversible nerve growth factor (NGF) inhibitor which binds to NGF, and with an IC50 of ~ 1 µM. Ro 08-2750 inhibits NGF binding to p75NTR selectively over TRKA[1]. Ro 08-2750 is a selective MSI RNA-binding activity inhibitor, with an IC50 of 2.7 μM[3]. Dec 20 2024
E8138 TB500 TB500 is a synthetic version of an active region of thymosin β4. TB500 is claimed to promote endothelial cell differentiation, angiogenesis in dermal tissues, keratinocyte migration, collagen deposition and decrease inflammation[1]. Dec 20 2024
E1778 Fasentin Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity[1][2][3]. Dec 20 2024
E7627 Y-33075 Y-33075 is a selective ROCK inhibitor derived from Y-27632, and is more potent than Y-27632, with an IC50 of 3.6 nM. Dec 20 2024
E7883 LX7101 LX7101 is a potent LIM-kinase, ROCK and PKA inhibitor with IC50s of 24 nM, 1.6 nM, 10 nM and <1 nM for LIMK1, LIMK2, ROCK2 and PKA, respectively. LX7101 proves significantly selective for LIMK2 with IC50 values of 4.3 nM and 32 nM for LIMK2 and LIMK1 at 2 μM ATP, respectively. LX7101 has the potential for ocular hypertension and associated glaucoma research[1][2]. Dec 20 2024
E8139 GSK 525768A GSK 525768A is the inactive enantiomer of GSK525762A. GSK 525768A has no activity towards BET. Dec 20 2024
S7431 TAPI-2 TAPI-2 (TNF Protease Inhibitor 2) is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20 μM for MMP[1]. TAPI-2 blocks the entry of infectious SARS-CoV[2]. Dec 20 2024
E7628 PD158780 PD158780 is a potent EGFR family inhibitor with IC50s of 8 pM, 49, 52, 52 nM for EGFR, ErbB2, ErbB3, and ErbB4, respectively. Dec 20 2024
E7884 Urolithin C Urolithin C, a gut-microbial metabolite of Ellagic acid, is a glucose-dependent activator of insulin secretion. Urolithin C is a L-type Ca2+ channel opener and enhances Ca2+ influx. Urolithin C induces cell apoptosis through a mitochondria-mediated pathway and also stimulates reactive oxygen species (ROS) formation[1][2]. Dec 20 2024
E8140 Pyridoclax Pyridoclax is a potential Mcl-1 inhibitor. Dec 20 2024
S8290 Xestospongin C Xestospongin C ((-)-Xestospongin C) is a selective, reversible inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor. Xestospongin C acts as an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) pump of internal stores. Xestospongin C blocks IP3-induced Ca2+ release from cerebellar microsomes with an IC50 of 358 nM. Xestospongin C is a valuable tool for investigating the structure and function of IP3Rs and Ca2+ signaling in neuronal and nonneuronal cells[1][2][3]. Dec 20 2024
E7629 PTP1B-IN-1 PTP1B-IN-1 (Compound 7a) is a small molecule inhibitor of PTP1B with an IC50 value of 1.6 mM. It is often used as the mother core for derivatives of analogues[1][2]. Dec 20 2024
E7885 TBA-7371 TBA-7371 is a potent, noncovalent DprE1 inhibitor. TBA-7371 has potent antitubercular activity [1]. Dec 20 2024
E8141 LUF6000 LUF6000 is an orally active allosteric modulator of the A3 adenosine receptor. LUF6000 has potent anti-inflammatory effect. Dec 20 2024
E1143 dTRIM24 dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC, consists of ligands for von Hippel-Lindau and TRIM24. Dec 20 2024
E7630 TG003 TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively[1]. Dec 20 2024
E7886 Thalidomide-O-amido-C4-N3 Thalidomide-O-amido-C4-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology. Thalidomide-O-amido-C4-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. Dec 20 2024
E8142 Deltonin Deltonin, a steroidal saponin, isolated from Dioscorea zingiberensis, has antitumor activity; Deltonin inhibits ERK1/2 and AKT activation. Dec 20 2024
E1555 Coumermycin A1 Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria. Coumermycin A1 shows anti-orthopoxvirus activity. Dec 20 2024
E7631 Cinromide Cinromide is an anticonvulsant agent. Cinromide inhibits epithelial neutral amino acid transporter B0AT1 (SLC6A19) with an IC50 of 0.5 μM[1][2]. Dec 20 2024
E7887 Mutant IDH1-IN-1 Mutant IDH1-IN-1 is a mutant-selective IDH1 inhibitor with with IC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively. Dec 20 2024
E8143 Ru(bpy)2(mcbpy-O-Su-ester)(PF6)2 Ru(bpy)2(mcbpy-O-Su-ester)(PF6)2 is a potent ruthenium-based dye. Ru(bpy)2(mcbpy-O-Su-ester)(PF6)2 can bu used as an effective quencher of quantum dots (QDs) fluorescence and the capture probe of virus antigen EV71. Ru(bpy)2(mcbpy-O-Su-ester)(PF6)2 can be used sensitive electrogenerated chemiluminescence (ECL) labels for detection of matrix metalloproteinases (MMPs)[1][2][3]. Dec 20 2024
E1935 A-770041 A-770041 is a selective and orally active Src-family Lck inhibitor. A-770041 inhibits Lck with an IC50 value of 147 nM with the presence of 1 mM ATP. A-770041 shows 300-fold selective to Lck over Fyn, the other Src family kinase involved in T-cell signaling. A-770041 can be used for the research of acute rejection[1][2]. Dec 20 2024
E7632 CDDO-EA CDDO-EA is an NF-E2 related factor 2/antioxidant response element (Nrf2/ARE) activator. Dec 20 2024
E7888 Decanoyl-RVKR-CMK Decanoyl-RVKR-CMK (DecRVKRcmk) inhibits over-expressed gp160 processing and HIV-1 replication[1]. Dec 20 2024
E1705 Mibefradil dihydrochloride Mibefradil dihydrochloride (Ro 40-5967 dihydrochloride) is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels (IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively)[1]. Dec 20 2024
E7633 CCR2-RA-[R] CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine receptor type 2 (CCR2) with an IC50 of 103 nM. Dec 20 2024
E7889 NKP608 NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo. IC50 value: 2.6 nMTarget: NK-1 receptorIn vitro, the binding of NKP608 to bovine retina was characterized by an IC50 of 2.6+/-0.4 nM, whereas the compound's affinity to other receptor binding sites, including NK-2 and NK-3, was much lower. Species differences in IC(50) values with NKP608 were less pronounced than with previously described NK-1 receptor antagonists, being 13+/-2 and 27+/-2 nM in gerbil midbrain and rat striatum, respectively. In vivo, using the hind foot thumping model in gerbils, NKP608 exhibited a potent NK-1 antagonistic activity foll Dec 20 2024
E1253 Helenalin Helenalin is an anti-inflammatory sesquiterpene lactone. Helenalin selectively inhibits transcription factor NF-κB by directly targeting p65. Helenalin has alkylating activity, targets the cysteine sulfhydryl groups in the p65 subunit of NF-κB, thereby inhibits its DNA binding[1][2]. Dec 20 2024
E7634 Z-Ile-Leu-aldehyde Z-Ile-Leu-aldehyde (Z-IL-CHO) is a potent and competitive peptide aldehyde inhibitor of γ-secretase and notch[1][2]. Dec 20 2024
E7890 Ketotifen Ketotifen (HC 20-511) is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention[1][2][3][4]. Dec 20 2024
E5160 Gypenoside XLVI Dec 20 2024
E5780 Laduviglusib trihydrochloride Laduviglusib (CHIR-99021) trihydrochloride is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib trihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib trihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib trihydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib trihydrochloride induces autophagy[1][2][3]. Dec 20 2024
E7635 Pyr10 Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels[1]. Dec 20 2024
E7891 HTS01037 HTS01037 is an inhibitor of fatty acid binding; and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 with a Ki of 0.67 μM. Dec 20 2024
E4970 Gemcitabine elaidate Gemcitabine elaidate (CP-4126) is lipophilic pro-agent of Gemcitabine. Gemcitabine elaidate is converted to Gemcitabine by esterases in order to be phosphorylated. Gemcitabine elaidate exhibits anti-tumor activity[1][2]. Dec 20 2024
E7636 Contezolid Contezolid (MRX-I), a new and orally active oxazolidinone, is an antibiotic in study for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. Contezolid (MRX-I) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI)[1][2]. Dec 20 2024
E7892 24, 25-Dihydroxy VD2 24, 25-Dihydroxy VD2 is a hydroxylated metabolite of Vitamin D2; a synthetic analog of Vitamin D. Dec 20 2024
E1906 AX-15836 AX-15836 is a potent and selective ERK5 inhibitor with an IC50 of 8 nM. Dec 20 2024
E7637 Phorbol 12,13-dibutyrate Phorbol 12,13-dibutyrate (Phorbol dibutyrate) is a PKC activator and a potent skin tumor promoter[1][2]. Dec 20 2024
E7893 PF-4840154 PF-4840154 is a potent, selective agonist of the rat and human TrpA1 channel with EC50s of 97 and 23 nM, respectively. PF-4840154 elicits TrpA1-mediated nocifensive behaviour in mouse[1]. Dec 20 2024
E1116 AACOCF3 AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeant trifluoromethyl ketone analog of arachidonic acid. AACOCF3 is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). AACOCF3 blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. AACOCF3 has the potential for the research of cardiovascular disease[1][2][3]. Dec 20 2024
E7638 Sutezolid Sutezolid (PNU-100480), an orally active oxazolidinone antimicrobial agent, acts by inhibiting bacterial protein synthesis. Sutezolid has potent activity against mycobacteria, and is used for the research of drug-resistant tuberculosis[1][2]. Dec 20 2024
E7894 GPR120 Agonist 3 GPR120 Agonist 3 is a selective Gpr120 agonist with a logEC50 of −7.62. Dec 20 2024
S7402 Filipin III Filipin III is the major component of Filipin, a 28-membered ring pentaene macrolide antifungal antibiotic produced by S. filipinensis, S. avermitilis and S. miharaensis. Filipin interacts with membrane sterols causing the alteration of membrane structure[1]. Dec 20 2024
E7639 Epetraborole hydrochloride Epetraborole (GSK2251052) hydrochloride is a novel leucyl-tRNA synthetase (LeuRS) inhibitor (IC50=0.31 μM), thereby inhibiting protein synthesis. Epetraborole hydrochloride can be used in multidrug-resistant gram-negative pathogens infection research[1][2][3]. Dec 20 2024
E7895 Lys-SMCC-DM1 Lys-SMCC-DM1 (Lys-Nε-MCC-DM1) is a agent-linker conjugates for ADC that can inhibit tubulin polymerization. Lys-SMCC-DM1 is the active metabolite of T-DM1. T-DM1 is a HER2-targeting ADC with a tubulin polymerization inhibitor DM1. Lys-SMCC-DM1 can be used in the research of breast cancer[1][2]. Dec 20 2024
E1675 Monochlorobimane Monochlorobimane (Chlorobimane) is a fluorescent dye (λex=380 nm, λem=470 nm) to measure glutathione (GSH) in cellular assays[1]. Dec 20 2024
E7640 Lithium chloride hydrate Lithium chloride hydrate, an orally active mood stabilizer, is a potent virus inhibitor and effective immunomodulatory agent. Lithium chloride hydrate has antidepressant activity by inhibiting GSK3β and promoting neurogenesis. Lithium chloride hydrate alleviates cognition dysfunction and the symptoms of acute mania and depression. Lithium chloride hydrate can also be used for research of virus infection and Alzheimer's disease[1][2][3]. Dec 20 2024
E7896 6"-O-Malonyldaidzin 6"-O-Malonyldaidzin is a malonylated isoflavone isolated from soybean seeds. 6"-O-Malonyldaidzin may has protective effect on eye[1][2]. Dec 20 2024
E1260 ZD7288 ZD7288 (ICI D7288) is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker[1]. Dec 20 2024
E7641 TNF-α (31-45), human TNF-α (31-45), human is a potent NF-kB pathway activator. TNF-αis a proinflammatory cytokine that induces necrosis or apoptosis. TNF alpha stimulates NF-κB pathway via TNFR2 promotes cancer growth, invasion, and metastasis[1][2][3]. Dec 20 2024
E7897 N6,N6-Dimethyladenosine N6,N6-Dimethyladenosine is a modified ribonucleoside previously found in rRNA, and also exhibits in mycobacterium bovis Bacille Calmette-Guérin tRNA[1]. Dec 20 2024
E5784 AICAR phosphate AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor[1][2]. Dec 20 2024
E7642 Taltobulin Taltobulin (HTI-286), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis[1]. Dec 20 2024
E7898 1-Methylinosine 1-Methylinosine is a modified nucleotide found at position 37 in tRNA 3' to the anticodon of eukaryotic tRNA[1]. Dec 20 2024
E1306 KDM5-C70 KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels[1][2]. Dec 20 2024
E7643 Rosiptor Rosiptor (AQX-1125) is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects. Rosiptor (AQX-1125) inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro[1][2]. Dec 20 2024
E7899 HS38 HS38 is a potent, selective, and ATP-competitive inhibitor of death-associated protein kinase 1 (DAPK1) and zipper-interacting protein kinase (ZIPK, also called DAPK3), with Kds of 300 nM and 280 nM, respectively. HS38 is also a PIM3 inhibitor with an IC50 of 200 nM. HS38 can be used for the research of smooth muscle related disorders[1]. Dec 20 2024
E4618 CD3254 CD3254 a potent and selective retinoid-X-receptor (RXR) agonist[1]. Dec 20 2024
E7644 Tozadenant Tozadenant is an adenosine A2A receptor antagonist, with Ki of 11.5 nM on human A2A and 6 nM on rhesus A2A. Dec 20 2024
E7900 Chlorantraniliprole Chlorantraniliprole is an insecticide that potently and selectively activates insect ryanodine receptor, with EC50s of 40 nM and 50 nM for Drosophila melanogaster and H. virescens ryanodine receptor, and ～300-fold more potent than that in the mouse myoblast cell line, C2C12 (EC50, 14 μM). Dec 20 2024
E6016 Dalbavancin hydrochloride Dalbavancin hydrochloride (MDL-63397 hydrochloride) is a semisynthetic lipoglycopeptide antibiotic with potent bactericidal activity against Gram-positive bacteria. Dalbavancin hydrochloride inhibits Staphylococcus aureus and Bacillus anthracis with MIC90s of 0.06 μg/mL and 0.25 μg/mL, respectively[1][2]. Dec 20 2024
E7645 Phenylacetylglutamine-d5 Phenylacetylglutamine-d5 is the deuterium labeled Phenylacetylglutamine. Phenylacetylglutamine is a colonic microbial metabolite from amino acid fermentation[1]. Dec 20 2024
E7901 Mofezolac Mofezolac, a non-steroidal anti-inflammatory drug (NSAID), is a selective, reversible and orally active COX-1 inhibitor with an IC50 of 1.44 nM. Mofezolac shows weak inhibitory activity on COX-2 (IC50 of 447 nM). Mofezolac can relieve pain and has anti-inflammatory activities[1]. Dec 20 2024
E1319 Corin Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histone deacetylase (HDAC), with a Ki(inact) of 110 nM for LSD1 and an IC50 of 147 nM for HDAC1. Dec 20 2024
E7646 Castanospermine Castanospermine is a natural alkaloid that can be extracted from black beans or the Moreton Bay chestnut tree (Castanospermum australae). Castanospermine is an α/ β-glucosidase inhibitor. Castanospermine has anti-inflammatory, antiviral replication and anti-metastatic effects on prostate cancer. Castanospermine can be used as an immunosuppressant to prevent transplant rejection[1][2][3][4]. Dec 20 2024
E7902 BMS-599626 Hydrochloride BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 Hydrochloride displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 Hydrochloride inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy[1][2]. Dec 20 2024
E1269 A-484954 A-484954 is a highly selective eukaryotic elongationfactor-2 kinase(eEF2K) inhibitor, with an IC50 of 280 nM. Dec 20 2024
E7647 8-OH-DPAT hydrobromide 8-OH-DPAT (8-Hydroxy-DPAT) hydrobromide is a potent and selective 5-HT1A agonist with a pIC50 of 8.19. 8-OH-DPAT hydrobromide has selectivity of almost 1000 fold for a subtype of the 5-HT1 binding site[1]. Dec 20 2024
E7903 Glucosylsphingosine Glucosylsphingosine (lyso-Gb1) is a deacylated form of glucosylceramide and is also degraded by the glucocerebrosidase. Glucosylsphingosine is a very promising, reliable and specific biomarker for monitoring Gaucher disease[1]. Dec 20 2024
E2875 Levobunolol(l-Bunolol) hydrochloride Levobunolol (l-Bunolol) hydrochloride is a potent and nonselective β-adrenergic receptor antagonist with an IC50 of 48 μM. Dec 20 2024
E5797 BTTAA BTTAA is a Cu(I)-stabilizing ligand, whch performs potently with ubiquitin Glu18AzF. Dec 20 2024
E7648 IC87201 IC87201, an inhibitor of PSD95-nNOS protein-protein interactions, suppresses NMDAR-dependent NO and cGMP formation. Dec 20 2024
E7904 Ritodrine Ritodrine (DU21220) is a β-adrenergic agonist, also an effective smooth muscle and uterine relaxant. Ritodrine prolongs contraction interval, can be used for researching arrest premature labor[1][2][3]. Dec 20 2024
E6028 Fosamprenavir Fosamprenavir (Amprenavir phosphate;GW 433908) is a phosphate ester proagent of the antiretroviral protease inhibitor Amprenavir, with improved solubility[1]. Anti-HIV infection[1]. Dec 20 2024
E7649 8-Bromo-cGMP sodium 8-Bromo-cGMP sodium, a membrane-permeable analogue of cGMP, is a PKG (protein kinase G) activator. 8-Bromo-cGMP sodium significantly inhibits Ca2+ macroscopic currents and impairs insulin release stimulated with high K+[1]. 8-Bromo-cGMP sodium has antinociceptive effects and results in vasodilator responses[2]. Dec 20 2024
E7905 Sulfobromophthalein disodium salt Sulfobromophthalein (Bromosulfophthalein) disodium salt is an organic anion dye used in the study of a variety of membrane carriers expressed in animal tissues and involved in transport of agents and metabolites[1]. Dec 20 2024
E4926 Alprenolol Alprenolol ((RS)-Alprenolol; dl-Alprenolol) is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent[1][2][3]. Dec 20 2024
E7650 LG100268 LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively[1]. LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively[2]. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy[3]. Dec 20 2024
E7906 Zuclopenthixol Zuclopenthixol is a thioxanthene derivative which acts as a mixed dopamine D1/D2 receptor antagonist. Dec 20 2024
E1531 GSK1940029 GSK1940029 (SCD inhibitor 1) is a stearoyl-coa desaturase (SCD) inhibitor extracted from patent WO/2009060053 A1, compound example 16. Dec 20 2024
E7651 AZD-0284 AZD-0284 is a selective inverse agonist of the nuclear receptor RORγ. AZD-0284 has the potential for plaque psoriasis vulgaris and respiratory tract disorders treatment[1]. Dec 20 2024
E7907 Nω-Propyl-L-arginine Nω-Propyl-L-arginine (N-omega-Propyl-L-arginine) is a potent, competitive, and highly selective inhibitor of neuronal nitric oxide synthase (nNOS), with a Ki of 57 nM. Nω-Propyl-L-arginine displays a 149-fold selectivity for nNOS over endothelial NOS (eNOS)[1][2]. Dec 20 2024
E4734 MeAIB MeAIB (α-(Methylamino)isobutyric acid) is a specific substrate for amino acid transport system A, especially System A (ATA1). It also inhibits SNAT2, which reduces intracellular levels of essential amino acids and impairs cell proliferation in porcine enterocytes by disrupting the mTOR signalling pathway. Dec 20 2024
E2507 BI605906 BI605906 is a novel IKKβ inhibitor with an IC50 value of 380 nM when assayed at 0.1 mM ATP. Dec 20 2024
E7652 Valsartan Ethyl Ester Valsartan Ethyl Ester is an impurity of Valsartan. Valsartan is an angiotensin II receptor antagonist for the treatment of high blood pressure and heart failure[1]. Dec 20 2024
E7908 Lasofoxifene Lasofoxifene (CP-336156) is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene can be used for research of breast cancer and postmenopausal osteoporosis[1][2]. Dec 20 2024
E1825 7rh 7rh (DDR1-IN-2) is a potent inhibitor of discoidin domain receptor 1 (DDR1), with an IC50 of 13.1 nM, and also less potently inhibits DDR2, with an IC50 of 203 nM. 7rh is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 20 2024
E7653 DC_517 DC_517 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 1.7 μM and 0.91 μM, respectively. Dec 20 2024
E7909 ITX3 ITX3 is a specific and nontoxic inhibitor of TrioN (N-terminal GEF domain of the multidomain Trio protein) with an IC50 value of 76 μM. ITX3 can be used for the research of agent[1][2]. Dec 20 2024
E4963 Clonidine Clonidine (Clonidin) is a direct-acting α2-adrenergic agonist. It is potentially used in the treatment of attention-deficit hyperactivity disorder (ADHD) in children and adolescents. Dec 20 2024
E4626 BAY 60-6583 BAY 60-6583 is a potent and high-affinity agonist of adenosine A2B receptor (EC50?= 3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with Ki values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model[1][5]. Dec 20 2024
E7654 Mardepodect Mardepodect (PF-2545920) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect can cross the blood-brain barrier[1][2]. Dec 20 2024
E7910 Tyrosine kinase inhibitor Tyrosine kinase inhibitor is a potent tyrosine kinase inhibitor. Dec 20 2024
E4754 Semustine Semustine is a member of the chloroethyl nitrosourea (CENU) family that induces DNA alkylation at the major groove, forming interstrand cross-links between guanine and cytosine bases (dG-dC). It exerts antitumor activity by inducing these DNA cross-links and is used as an antineoplastic alkylating agent for treating Lewis lung carcinoma, leukemia, and metastatic brain tumors. Dec 20 2024
E1953 Pevonedistat hydrochloride Pevonedistat hydrochloride (MLN4924 hydrochloride) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC50 of 4.7 nM[1]. Dec 20 2024
E7655 MC-Val-Cit-PAB-MMAF MC-Val-Cit-PAB-MMAF (Vc-MMAF) is a drug-linker conjugate for ADC by using the tubulin inhibitor, MMAF (HY-15579), linked via cathepsin cleavable MC-Val-Cit-PAB (HY-78738). MC-Val-Cit-PAB-MMAF shows antitumor activity[1]. Dec 20 2024
E7911 H-Val-Pro-Pro-OH H-Val-Pro-Pro-OH, a milk-derived proline peptides derivative, is an inhibitor of Angiotensin I converting enzyme (ACE), with an IC50 of 9 μM. Dec 20 2024
E1337 Arginase inhibitor 1 Arginase inhibitor 1 is a potent inhibitor of human arginases I and II with IC50s of 223 and 509 nM, respectively. Dec 20 2024
E7656 (S)-Tedizolid (S)-Tedizolid is the S-enantiomer of Tedizolid. Tedizolid is a novel oxazolidinone with activity against Gram-positive pathogens. (S)-Tedizolid is the less active isomer. Dec 20 2024
E7912 Beclomethasone 17-propionate Beclomethasone 17-propionate (Beclomethasone-17-monopropionate), an active metabolite of Beclomethasone dipropionate (HY-13571), is a glucocorticoid receptor (GR) agonist. Beclomethasone 17-propionate exhibits greater affinity for GR than Beclomethasone dipropionate. Beclomethasone 17-propionate effectively suppresses cytokine production in chronic obstructive pulmonary disease (COPD) lung macrophages[1][2][3]. Dec 20 2024
E5772 DC_AC50 DC_AC50 is a dual inhibitor of Atox1 and CCS (copper chaperones). Inhibiting intracellular copper chaperones as a means of reducing/preventing acquired chemotherapy resistance[1]. Dec 20 2024
E7657 Maleimide-DOTA Maleimide-DOTA is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Dec 20 2024
E7913 LY 303511 hydrochloride LY 303511 hydrochloride is a structural analogue of LY294002. LY303511 does not inhibit PI3K. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells. LY303511 reversibly blocks K+ currents (IC50=64.6±9.1 μM) in MIN6 insulinoma cells. Dec 20 2024
S9717 Vecabrutinib Vecabrutinib (SNS-062) is a potent, noncovalent BTK and ITK inhibitor, with Kd values of 0.3 nM and 2.2 nM, respectively. Vecabrutinib shows an IC50 of 24 nM for ITK[1][2]. Dec 20 2024
E7658 Fluxametamide Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls. Dec 20 2024
E7914 Desisobutyryl-ciclesonide Desisobutyryl-ciclesonide is the active metabolite of Ciclesonide. Desisobutyryl-ciclesonide has affinity for the glucocorticoid receptor. Dec 20 2024
E1172 Dynarrestin Dynarrestin is a aminothiazole inhibitor of cytoplasmic dyneins 1 and 2. Dynarrestin rapidly and reversibly inhibits dynein 1-driven microtubule gliding in vitro plus a range of dynein 1- and 2-dependent processes in cells without affecting ATP hydrolysis and interfering with ciliogenesis. Dynarrestin suppresses hedgehog (Hh)-dependent proliferation of neuronal precursors and tumor cells[1]. Dec 20 2024
E7659 RO-28-1675 RO-28-1675 is a potent allosteric glucokinase (GK) activator with an EC50 of 54 nM. RO-28-1675 can be used for the research of type 2 diabetes[1][2]. Dec 20 2024
E7915 9-Deazaguanine 9-Deazaguanine is a nucleoside analog with potent inhibitory activity against purine nucleoside phosphorylase (PNP)[1]. Dec 20 2024
E8144 PIM447 PIM447 (LGH447) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis[1][2]. Dec 20 2024
E7660 Neurotensin Neurotensin, a gut tridecapeptide, acts as a potent cellular mitogen for various colorectal and pancreatic cancers which possess high-affinity neurotensin receptors (NTR). Dec 20 2024
E7916 FTY720 (S)-Phosphate FTY720 (S)-Phosphate is an agonist of S1P receptor 1 (S1PR1), used in the research of acute inflammatory diseases such as acute lung injury. Dec 20 2024
E5776 Asymmetric dimethylarginine Asymmetric dimethylarginine is an endogenous inhibitor of nitric oxide synthase (NOS), and functions as a marker of endothelial dysfunction in a number of pathological states. Dec 20 2024
E7661 CDK9-IN-1 CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection, with an IC50 of 39 nM for CDK9/CycT1, extracted from reference, compound 87. Dec 20 2024
E7917 Ro 90-7501 Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response[2]. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner[3]. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells[4]. Dec 20 2024
S7822 Kifunensine Kifunensine, a potent and selective inhibitor of class I α-mannosidases isolated from Actinomycete, prevents α-mannosidases I from trimming mannose residues on glycoproteins. Kifunensine inhibits ERAD[1][2][3]. Dec 20 2024
E7662 α-Lipoic acid-NHS α-Lipoic acid-NHS is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Dec 20 2024
E7918 Obovatol Obovatol is a biphenyl ether lignan isolated from the leaves of Magnolia obovata Thunb[1]. Dec 20 2024
E1317 LY 345899 LY 345899 is a Folate analog and is a methylene tetrahydrofolate dehydrogenase (MTHFD1; DC301) and MTHFD2 inbhibitor with IC50 values of 96 nM and 663 nM, respectively and a Ki of 18 nM for MTHFD1[1][2][3]. Dec 20 2024
E7663 O-1602 O-1602 is an agonist of GPR55 (G protein-coupled receptor 55). O-1602 reduces the number and activation of hippocampal microglia induced by METH (methamphetamine). O-1602 decreases the expression levels of NLRP3 inflammasome proteins, including NLRP3, ASC and Caspase-1[1]. Dec 20 2024
E7919 (±)-Ibipinabant (±)-Ibipinabant ((±)-SLV319) is the racemate of SLV319. (±)-Ibipinabant ((±)-SLV319) is a potent and selective cannabinoid-1 (CB-1) receptor antagonist with an IC50 of 22 nM. Dec 20 2024
E1765 U-73343 U-73343, works as a protonophore, is an inactive analog of U-73122 and can be used as a negative control. U-73343 dose-dependently inhibits acid secretion irrespective of the stimulant. U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50 of 1-2.1 µM for PLC[1][2]. Dec 20 2024
E7664 TCS 401 TCS 401 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B). Dec 20 2024
E7920 Moringin Moringin is a potent and selective TRPA1 ion channel natural agonist with an EC50 of 3.14 μM. Moringin does not activate or activates very weakly the vanilloids somatosensory channels TRPV1, TRPV2, TRPV3 and TRPV4, and the melastatin cooling receptor TRPM8. Moringin has hypoglycemic, antimicrobial, anti-inflammatory, anticancer and neuroprotection activities[1][2]. Dec 20 2024
E4649 NNC 55-0396 NNC 55-0396 is a highly selective T-type calcium channel blocker with an IC50 value of 6.8 μM for Cav3.1 T-type channels. NNC 55-0396 can be used for the research of neurological disease research[1][2]. Dec 20 2024
E7665 bpV(phen) bpV(phen), a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity[1][2][3][4][5]. Dec 20 2024
E7921 TZ9 TZ9 is a selective Rad6 inhibitor. TZ9 inhibits Rad6B-induced histone H2A ubiquitination, downregulates intracellular β-catenin, induces G2-M arrest and apoptosis, and inhibits the proliferation and migration of metastatic human breast cancer cells[1]. Dec 20 2024
S8210 Jasplakinolide Jasplakinolide is a potent actin polymerization inducer and stabilizes pre-existing actin filaments. Jasplakinolide binds to F-actin competitively with phalloidin with a Kd of 15 nM. Jasplakinolide, a naturally occurring cyclic peptide from the marine sponge, has both fungicidal and anti-cancer activity[1][2]. Dec 20 2024
E7666 Cevipabulin Cevipabulin (TTI-237) is an oral, microtubule-active antitumor compound and inhibits the binding of [3H] vinblastine to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line[1][2]. Dec 20 2024
E7922 Rostafuroxin Rostafuroxin (PST 2238), a digitoxigenin derivative, is an orally active and potent Na+,K+-ATPase (ATP1A1) antognist. Rostafuroxin binds specifically to the ATP1A1 extracellular domain and blocks respiratory syncytial virus (RSV)-triggered EGFR Tyr845 phosphorylation. Rostafuroxin has antihypertensive and anti-RSV activity[1][2][3][4]. Dec 20 2024
E1898 JWG-071 JWG-071 is the kinase-selective chemical probe for ERK5. JWG-071 inhibits ERK5 and LRRK2 with IC50 values of 88nM and 109 nM, respectively[1]. Dec 20 2024
E7667 Bromperidol Bromperidol (R-11333) possesses antipsychotic activity, with a high affinity for central dopamine receptors D2. Bromperidol can kill Mycobacteria in a synergistic manner with Spectinomycin[1][2]. Dec 20 2024
E7923 Thioridazine Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs)[1][2][3][4]. Dec 20 2024
E4786 Carboxy-PTIO potassium Carboxy-PTIO potassium is a potent nitric oxide (NO) scavenger that can make a quick reaction with NO to produce NO2. Carboxy-PTIO potassium can prevent hypotension and endotoxic shock through the direct scavenging action against NO in lipopolysaccharide-stimulated rat model[1][2][3]. Dec 20 2024
E7668 Azimilide Azimilide(NE-10064) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.IC50 value:Target: in vitro: Azimilide blocked HERG channels at 0.1 and 1 Hz with IC50s of 1.4 microM and 5.2 microM respectively. Azimilide blockade of HERG channels expressed in Xenopus oocytes and I(Kr) in mouse AT-1 cells was decreased under conditions of high [K+]e, whereas block of slowly activating I(Ks) channels was not affected by changes in [K+]e [1]. Azimilide suppressed the following currents (Kd in parenthesis): IKr (< 1 microM at -20 mV), IKs (1.8 microM at +30 mV), L-type Ca current (17.8 microM at +10 mV), and Na current (19 microM at -40 mV). Azimilide was Dec 20 2024
E7924 GSK189254A GSK189254A (GSK189254 free base) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively. Dec 20 2024
E1594 Difamilast Difamilast (OPA-15406) is a topical, selective and nonsteroidal phosphodiesterase-4 (PDE4) inhibitor with particularly efficient inhibition of subtype B (IC50=11.2 nM). Difamilast can be used for the research of mild to moderate atopic dermatitis (AD)[1][2][3]. Dec 20 2024
E7669 Filorexant Filorexant (MK-6096) is an orally bioavailable potent and selective reversible antagonist of OX1 and OX2 receptor(<3 nM in binding). Dec 20 2024
E7925 SKA-121 SKA-121 is a selective KCa3.1 activator. SKA-121 exhibits EC50s of 109 nM and 4.4 μM for KCa3.1 and KCa2.3, respectively. Dec 20 2024
E1012 GW280264X GW280264X is the mixed ADAM10/TACE (ADAM17) metalloproteinases inhibitor. GW280264X potently blocks TACE (ADAM17) and ADAM10 with IC50s of 8.0 nM and 11.5 nM, respectively[1]. ADAM10 and 17 modulate the immunogenicity of glioblastoma-initiating cells[2]. Dec 20 2024
E7670 Anguizole Anguizole is a small molecule inhibitor of HCV replication and alters NS4B's subcellular distribution.IC50 Value: Target: HCV Dec 20 2024
E7926 Purpurogallin Purpurogallin is a naturally phenol extracted from the plants of Quercus spp, has potent xanthine oxidase (XO) inhibitory activity with an IC50 of 0.2 µM. Purpurogallin has antioxidant and anti-inflammatory effects[1][2][3]. Dec 20 2024
E4735 2-NP 2-NP is a selective enhancer of STAT1 transcription. 2-NP can enhance the ability of IFN-γ to inhibit the proliferation of human breast cancer and fibrosarcoma cells[1]. Dec 20 2024
E7671 TFLLR-NH2(TFA) TFLLR-NH2 (TFA) is a selective PAR1 agonist with an EC50 of 1.9 μM. Dec 20 2024
E7927 (Z)-Semaxanib (Z)-Semaxanib (compound (z)-1) is a potent tyrosine kinase inhibitor. (Z)-Semaxanib shows cytotoxicity for TAMH and HepG2 cells with IC50s of 6.28 µM and 8.17 µM, respectively[1]. Dec 20 2024
E2857 W-54011 W-54011 is a potent and orally active non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils with a Ki value of 2.2 nM. W-54011 also inhibits C5a-induced intracellular Ca2+ mobilization, chemotaxis, and generation of ROS in human neutrophils with IC50s of 3.1 nM, 2.7 nM, and 1.6 nM, respectively[1]. Dec 20 2024
E7672 Prinaberel Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis[1][2][3]. Dec 20 2024
E7928 PF-01247324 PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel. Dec 20 2024
E1774 Pyrithione Pyrithione, a Transition metal complexe, is a zinc ionophore that causes increased zinc levels within mammalian cells. Pyrithione has potent bactericidal and anti-fungal activity[1][2]. Dec 20 2024
E7673 SJG-136 SJG-136 is a DNA cross-linking agent, with an XL50 of 45 nM for pBR322 DNA. SJG-136 has potent antitumor activity. Dec 20 2024
E7929 Zatebradine hydrochloride Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively[1]. Dec 20 2024
E4999 Sulfo-NHS-SS-Biotin sodium Sulfo-NHS-SS-biotin is a long-chain cleavable and cell-impermeant amine-reactive biotinylation reagent. Sulfo-NHS-SS-biotin can be used for the labeling and purifying of cell-surface protein[1]. Dec 20 2024
E7674 AP1867 AP1867 is a synthetic FKBP12F36V-directed ligand[1]. Dec 20 2024
E7930 BAY 61-3606 BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM[1]. BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell[2]. BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates[3]. Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells[4]. Dec 20 2024
E6034 Trovafloxacin Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1[1][2][3]. Dec 20 2024
E7675 Lasalocid Lasalocid (Lasalocid-A; Ionophore X-537A; Antibiotic X-537A) is an antibacterial and anticoccidial agent used in feed additives. Dec 20 2024
E7931 Lexithromycin Lexithromycin is an erythromycin A derivative, with antibacterial activity. Dec 20 2024
E2650 ITX5061 ITX5061 is a type II inhibitor of p38 MAPK and also an antagonist of scavenger receptor B1 (SR-B1). Dec 20 2024
E7676 SB-224289 hydrochloride SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect. Dec 20 2024
E7932 Valnoctamide Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAA receptors[1]. Dec 20 2024
E1766 Lometrexol Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor[1][2][3]. Dec 20 2024
E7677 MJN110 MJN110 is an orally active and selective monoacylglycerol lipase (MAGL) inhibitor with IC50s of 9.1 nM and 2.1 nM for hMAGL and 2-arachidonoylglycerol (2-AG), respectively[1]. MJN110 produces opioid-sparing effects and displays strong antihyperalgesic activity[2]. Dec 20 2024
E7933 1alpha-Hydroxy VD4 1alpha-Hydroxy VD4 , a 1alpha(OH)D derivative, can effectively induce the differentiation of monoblastic leukaemia U937, P39/TSU and P31/FUJ cells. IC50 value；Target: VD analog Dec 20 2024
E5189 Andrograpanin Dec 20 2024
E5796 MAGL-IN-5 MAGL-IN-5 (CAY10499) is a non-selective lipase inhibitor with IC50 values of 144, 90, and 14 nM for human recombinant monoacylglycerol lipase(MAGL),hormone sensitive lipase(HSL), and fatty acid amide hydrolase(FAAH) respectively[1][2]. Dec 20 2024
E7678 Cot inhibitor-2 Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM[1]. Dec 20 2024
E7934 3-O-(2-Aminoethyl)-25-hydroxyvitamin D3 3-O-(2-Aminoethyl)-25-hydroxyvitamin D3 is a Vitamin D3 derivative. Dec 20 2024
E2685 (E/Z)-BML264 (E/Z)-BML264 (N-(p-amylcinnamoyl) Anthranilic Acid) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker[1][2]. (E/Z)-BML264 (N-(p-amylcinnamoyl) Anthranilic Acid) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia[3]. Dec 20 2024
E7679 Resminostat hydrochloride Resminostat hydrochloride is a potent inhibitor of HDAC1, HDAC3 and HDAC6, with mean IC50 values of 42.5, 50.1, 71.8 nM, respectively, and shows less potent activities against HDAC8, with an IC50 of 877 nM. Dec 20 2024
E7935 Inecalcitol Inecalcitol (TX 522), a unique vitamin D3 analog, is an orally active vitamin D receptor (VDR) agonist with a Kd of 0.53 nM. Inecalcitol can induce cell apoptosis and has potent anticancer activities[1][2][3][4]. Inecalcitol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 20 2024
E5814 OGT 2115 OGT 2115 is a potent, cell-permeable and orally active heparanase inhibitor with an IC50 of 0.4 μM. OGT 2115 has anti-angiogenic properties (IC50 of 1 μM). OGT 2115 also inhibits heparan sulfate degradation activity[1][2]. Dec 20 2024
E7680 A 419259 A 419259 is a broad-spectrum pyrrolo-pyrimidine inhibitor, has high selectivity towards the Src family. A 419259 shows inhibitory effect for Src, Lck and Lyn with IC50 of 9 nM, <3 nM and <3 nM, respectively[1][2]. Dec 20 2024
E7936 5,6-trans-Vitamin D2 5,6-trans-Vitamin D2 is the isomer of Vitamin D2[1]. Dec 20 2024
S7058 Refametinib (R enantiomer) Refametinib R enantiomer is a MEK inhibitor extracted from patent WO2007014011A2, compound 1022, has an EC50 of 2.0-15 nM. Dec 20 2024
E7681 MK-6892 MK-6892 is a potent, selective, and full agonist for the high affinity nicotinic acid (NA) receptor GPR109A. Ki and GTPγS EC50 of MK-6892 on the Human GPR109A is 4 nM and 16 nM, respectively. Dec 20 2024
E7937 Fidarestat Fidarestat (SNK 860) is an inhibitor of aldose reductase, with IC50s of 26 nM, 33 μM, and 1.8 μM for aldose reductase, AKR1B10 and V301L AKR1B10, respectively; Fidarestat (SNK 860) has the potential to treat diabetic disease. Dec 20 2024
E2828 AG 1295 AG 1295 is a selective platelet-derived growth factor receptor (PDGFR) tyrosine-kinase inhibitor. AG1295 abolishes autophosphorylation of the PDGFR whereas not affects the autophosphorylation of the EGF receptor[1][2][3][4]. Dec 20 2024
E7682 Nomifensine Nomifensine is a norepinephrine-dopamine reuptake inhibitor, increases the amount of synaptic norepinephrine and dopamine available to receptors by blocking the dopamine and norepinephrine reuptake transporters. Dec 20 2024
E7938 Cyclo(RADfK) Cyclo(RADfK) is a selective α(v)β(3) integrin ligand that has been extensively used for research, therapy, and diagnosis of neoangiogenesis. Dec 20 2024
S8462 Toxoflavin Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex, also acts as an inhibitor of KDM4A, with antitumor activity[1][2]. Antibiotic properties. Dec 20 2024
E7683 Pergolide Pergolide (LY127809 (free base)) is an ergot-derived orally active dopamine receptor agonist. Pergolide can be used for Parkinson disease research[1]. Dec 20 2024
E7939 Manzamine A Manzamine A, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A has antimalarial and anticancer activities. Manzamine A also shows potent activity against HSV-1[1][2][3][4]. Dec 20 2024
E1273 Mal-amido-PEG2-C2-amido-Ph-C2-CO-AZD Mal-amido-PEG2-C2-amido-Ph-C2-CO-AZD (Mal-PEG2-AZD) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Dec 20 2024
E7684 Ac2-26 Ac2-26, an active N-terminal peptide of annexin A1 (AnxA1), attenuates ischemia-reperfusion-induced acute lung injury. Ac2-26 also decreases AnxA1 protein expression, inhibits the activation of NF-κB and MAPK pathways in the injured lung tissue[1]. Dec 20 2024
E7940 ACY-957 ACY-957 is an orally active and selective inhibitor of HDAC1 and HDAC2, with IC50s of 7 nM, 18 nM, and 1300 nM against HDAC1/2/3, respectively, and shows no inhibition on HDAC4/5/6/7/8/9[1]. Dec 20 2024
E1729 Senexin B Senexin B (SNX2-1-165; BCD-115) is a potent, highly water-soluble and bioavailable CDK8/19 inhibitor, with Kds of 140 nM for CDK8 and 80 nM for CDK19. Dec 20 2024
E7685 LE135 LE135 is a potent RAR antagonist that binds selectively to RARα (Ki of 1.4 μM) and RARβ (Ki of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent TRPV1 and TRPA1 receptors activator with EC50s of 2.5 μM and 20 μM, respectively[1][2]. Dec 20 2024
E7941 Aurothioglucose Aurothioglucose (Gold thioglucose), containing monovalent gold ion, is a potent active-site inhibitor of TrxR1 (thioredoxin reductase 1), with an IC50 of 65 nM. Aurothioglucose inhibits the DNA binding of NF-κB in vitro. Aurothioglucose shows anti-HIV and anti-rheumatic activities[1][2]. Dec 20 2024
E1557 GSK2194069 GSK2194069 is a potent inhibitor of β-ketoyl reductase (KR) of fatty acid synthase (FASN), with an IC50 value of 7.7 nM. GSK2194069 shows specifically inhibitory effect on FAS expressing cancer cells, by acting potent efficacy on acetoacetyl-CoA, NADPH with IC50 or Ki values of 4.8 nM and 5.6 nM, respectively[1][2][3]. Dec 20 2024
E7686 Withanone Withanone is an active constituent from Withania somnifera roots with multifunctional neuroprotective effect in alleviating cognitive dysfunction. Withanone affords protection against N-methyl-D-aspartate (NMDA)-induced excitotoxicity in Neuron-like cells[1][2]. Dec 20 2024
E7942 Fipexide Fipexide, a parachloro-phenossiacetic acid derivative, is an orally active nootropic agent. Fipexide reduces striatal adenylate cyclase activity. Fipexide has positive effect on cognitive performance by dopaminergic neurotransmission. Fipexide is used for senile dementia research. Fipexide acts as a chemical inducer in callus formation, shoot regeneration and Agrobacterium infection[1][2]. Dec 20 2024
S9939 Odevixibat Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis[1]. Dec 20 2024
E7687 MK-8033 MK-8033 is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs)[1][2]. Dec 20 2024
E7943 6-FITC 6-FITC (6-Fluorescein Isothiocyanate) is a derivative of fluorescein used in wide-ranging applications including flow cytometry. Dec 20 2024
E1534 GSK840 GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 0.9 nM, and inhibits kinase activity with an IC50 of 0.3 nM[1]. Dec 20 2024
E7688 L67 L67 (DNA Ligase Inhibitor) is a competitive DNA ligase inhibitor that effectively inhibits DNA ligases I/III (both IC50 are 10 μM). L67 can cause nuclear DNA damage by reducing levels of mitochondrial DNA and increasing levels of mitochondrially-generated ROS. L67 also activates the Caspase 1-dependent apoptosis pathway in cancer cells, can be used in cancer research[1][2]. Dec 20 2024
E7944 Vipadenant Vipadenant (BIIB-014; CEB-4520) is an adenosine receptor antagonist, with Kis of 1.3 nM and 68 nM for A2A and A1, respectively. Dec 20 2024
S7481 Bryostatin 1 Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties[1][2][3][4]. Dec 20 2024
E7689 (R)-(-)-Rolipram (R)-(-)-Rolipram is the R-enantiomer of Rolipram. Rolipram is a selective inhibitor of phosphodiesterases PDE4 with IC50 of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, respectively. Dec 20 2024
E7945 MF498 MF498 is a selective and orally active E prostanoid Receptor 4 (EP4) antagonist with a Ki value of 0.7 nM. MF498 can be used in the research of inflammation, such as rheumatoid and osteoarthritis[1][2]. Dec 20 2024
E1779 Dobutamine Dobutamine is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine can increase cardiac output and correct hypoperfusion[1][2][3][4]. Dec 20 2024
E7690 7α,25-Dihydroxycholesterol 7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells[1][2]. Dec 20 2024
E7946 Esculentoside H Esculentoside H (EsH) is a saponin isolated from the root extract of perennial plant Phytolacca esculenta[1]. Esculentoside H (EH) has anti-tumor activity, the mechanism is related to the capacity for TNFrelease[2].Esculentoside H (EsH) suppresses colon cancer cell migration through blockage of the JNK1/2 and NF-κB signaling-mediated matrix metalloproteinases-9 (MMP-9) expression[1]. Dec 20 2024
S4487 Gilteritinib hemifumarate Gilteritinib (ASP2215) hemifumarate is a potent and ATP-competitive FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively. Dec 20 2024
E7691 Mps1-IN-3 Mps1-IN-3 is a potent and selective MPS1 kinase inhibitor, with an IC50 of 50 nM. Dec 20 2024
E7947 Methylpiperidino pyrazole Methylpiperidino pyrazole (MPP) is a potent and selective ER (estrogen receptor) modulator. Methylpiperidino pyrazole induces significant apoptosis in the endometrial cancer and oLE cell lines. Methylpiperidino pyrazole reverses the the positive effects of beta-estradiol. Methylpiperidino pyrazole has mixed agonist/antagonist action on murine uterine ERalpha in vivo[1][2][3]. Dec 20 2024
E1250 (R)-CPP (R)-CPP is a highly potent NMDA receptor antagonist[1]. Dec 20 2024
E7692 N-Acetyltyramine N-Acetyltyramine is a quorum-sensing inhibitor (QSI) compound produced by V. alginolyticus M3-10. N-Acetyltyramine is capable of inhibiting the QS of C. violaceum ATCC 12472. N-acetyltyramine reverses resistance in Doxorubicin-resistant leukemia P388 cells[1][2]. Dec 20 2024
E4633 Pyocyanin Pyocyanin (Pyocyanine) is a toxic, quorum sensing (QS) controlled metabolite produced by Pseudomonas aeruginosa. Pyocyanin is a REDOX active compound that promotes the production of reactive oxygen species (ROS). Pyocyanin has antibacterial and anti-inflammatory activity[1][2][3][4]. Dec 20 2024
E7693 Tofacitinib metabolite-1 Tofacitinib metabolite-1 is a metabolite of Tofacitinib, a JAK inhibitor. Tofacitinib metabolite-1 can be used in the pharmacokinetics and metabolism studies of tofacitinib[1][2]. Dec 20 2024
E7948 Sisomicin Sisomicin is a broad-spectrum aminoglycoside antibiotic produced by Micromonospora inyoensis. Sisomicin is highly active against Gram-positive bacteria[1][2]. Dec 20 2024
E4863 Phentolamine Phentolamine is a potent, selective and orally active α1 adrenergic and α2 adrenergic receptor antagonist. Phentolamine can be used for the research of erectile dysfunction[1][2][3]. Dec 20 2024
E7694 VU 0240551 VU 0240551 is a potent neuronal K-Cl cotransporter KCC2 inhibitor (IC50=560 nM) and is selective versus NKCC1. VU 0240551 also inhibits hERG and L-type Ca2+ channels. VU 0240551 attenuates GABA-induced hyperpolarization of P cells, produces a positive shift in the P cell GABA reversal potential and enhances P cell synaptic transmission[1][2]. Dec 20 2024
E7949 Ac-DEVD-CMK Ac-DEVD-CMK (Caspase-3 Inhibitor III) is a selective and irreversible caspase-3 inhibitor. Ac-DEVD-CMK significantly inhibits apoptosis induced by high levels of glucose or 3,20-dibenzoate (IDB; HY-137295). Ac-DEVD-CMK can be used in a variety of experimental approaches to inhibit apoptosis[1][2][3]. Dec 20 2024
E4027 SB 202474 SB 202474, a negative analog of SB203580. SB 202474, which has no ability to inhibit p38 MAPK activity and is widely used as a negative control compound in p38 MAPK studies, also suppressed melanin synthesis induction[1]. Dec 20 2024
E7695 SB-277011 SB-277011 is a potent and delective dopamine D3 receptor antagonist (pKi values are 8.0, 6.0, 5.0 and <5.2 for D3, D2, 5-HT1D and 5-HT1B respectively); brain penetrant.IC50 value: 8.0 (pKi)Target: D3 receptor Dec 20 2024
E7950 Carperitide acetate Carperitide acetate (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine acetate) is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. Carperitide acetate inhibits endothelin-1 secretion in a dose-dependent way. Dec 20 2024
E1420 Talampanel Talampanel (LY300164) is an orally and selective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor antagonis with anti-seizure activity[1]. Talampanel (IVAX) has neuroprotective effects in rodent stroke models[2]. Talampanel attenuates caspase-3 dependent apoptosis in mouse brain[2]. Dec 20 2024
E7696 (Rac)-HAMI 3379 (Rac)-HAMI 3379 is the racemate of HAMI 3379. HAMI 3379 is a potent and selective Cysteinyl leukotriene (CysLT2) receptor antagonist[1][2]. Dec 20 2024
E7951 (RS)-MCPG (RS)-MCPG (alpha-MCPG) is a competitive and selective group I/group II metabotropic glutamate receptor (mGluR) antagonist. (RS)-MCPG blocks theta-burst stimulation (TBS)-induced shifts in both juvenile and neonatal rat hippocampal neurons[1][2]. Dec 20 2024
E2654 (±)-Zanubrutinib (±)-Zanubrutinib ((±)-BGB-3111) is the racemate of Zanubrutinib (HY-101474A). (±)-Zanubrutinib inhibits Bruton's tyrosine kinase (Btk) with an IC50 of 0.63 nM[1]. Dec 20 2024
E7697 DB04760 DB04760 (compound 4) is a potent, highly selective, non-zinc-chelating MMP-13 inhibitor with an IC50 of 8 nM[1]. DB04760 significantly reduces paclitaxel neurotoxicity and has anticancer activity[2]. Dec 20 2024
E7952 PYZD-4409 PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells[1]. Dec 20 2024
E1366 Artemisitene Artemisitene, a natural derivative of Artemisinin, is a Nrf2 activator with antioxidant and anticancer activities. Artemisitene activates Nrf2 by decreasing Nrf2 ubiquitination and increasing its stability[1][2]. Dec 20 2024
E7698 Tanaproget Tanaproget (NSP-989) is a novel nonsteroidal progesterone receptor agonist which can bind to the PR from various species with a higher relative affinity than reference steroidal progestins.IC50 value: 0.1 nM (EC50, induce alkaline phosphatase activity) [1]Target: progesterone receptorTanaproget represents a potential first-in-class nonsteroidal PR agonist for contraception with improved safety and side effect profiles versus currently available steroidal oral contraceptives.in vitro: In T47D cells, TNPR induces alkaline phosphatase activity with an EC(50) value of 0.1 nm, comparable with potent steroidal progestins such as medroxyprogesterone acetate (MPA) and trimegestone (TMG), albeit with a reduced efficacy ( approximately 60%). In a mam Dec 20 2024
E7953 PF 1022A PF 1022A is a cyclooctadepsipeptide with broadspectrum anthelmintic properties produced by fermentation of the fungus Mycelia sterilia. PF 1022A is a channel-forming ionophore. PF 1022A showes strong anthelmintic activities against Ascaridia galli in chickens. PF 1022A also can be used for angiostrongyliasis research[1][2][3]. Dec 20 2024
E6007 Pexidartinib Hydrochloride Pexidartinib Hydrochloride is an oral tyrosine kinase inhibitor of colony-stimulating factor 1 receptor (CSF1R). It significantly reduces macrophage levels in adipose tissue without altering overall myeloid cell counts in mice. It also induces developmental and immunotoxic effects in zebrafish embryos by hyperactivating Wnt signaling. Dec 20 2024
E5809 Dactolisib Tosylate Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2. Dec 20 2024
E7699 Dynole 34-2 Dynole 34-2 is a dynamin GTPase inhibitor (IC50s=6.9 and 14.2 µM for dynamin1 and dynamin2 GTPase activity, respectively) with antimitotic effect. Dynole 34-2 induces apoptosis, as revealed by cell blebbing, DNA fragmentation, and PARP cleavage[1]. Dynole 34-2 also potently inhibits receptor mediated endocytosis (RME)[2]. Dec 20 2024
E7954 Bafilomycin C1 Bafilomycin C1 is a macrolide antibiotic isolated from Streptomyces sp. Bafilomycin C1 is a potent, specific and reversible inhibitor of vacuolar-type H+-ATPases (V-ATPases). Bafilomycin C1 inhibits growth of gram-positive bacteria and fungi[2]. Bafilomycin C1 induces cell apoptosis and can be used for the study of hepatocellular carcinoma (HCC)[2]. Dec 20 2024
E1268 Maresin 1 Maresin 1, produced by human Mφs from endogenous docosahexaenoic acid (DHA) and a specialized proresolving mediator, stimulates intracellular [Ca2+] and secretion. Maresin 1 possesses anti-inflammatory activity[1][2][3]. Dec 20 2024
E7700 PPADS tetrasodium PPADS tetrasodiuma is a non-selective P2X receptor antagonist. PPADS tetrasodiuma blocks recombinant P2X1, -2, -3, -5 with IC50s ranging from 1 to 2.6 μM. PPADS tetrasodiuma blocks native P2Y2-like (IC50~0.9 mM) and recombinant P2Y4 (IC50~15 mM) receptors. PPADS tetrasodiuma is an inhibitor of the reverse mode of the Na/Ca2+ exchanger in guinea pig airway smooth muscle[1][2]. Dec 20 2024
E7955 FeTCPP FeTCPP (Iron(III) meso-Tetra(4-carboxyphenyl)porphine chloride) is a metallic porphyrin compound formed by the coordination of a central iron ion (Fe3+) with four 4-carboxyphenylporphyrins (TCPP). FeTCPP can be used as a catalyst for catalytic, electrochemical, photochemical and biomedical research. FeTCPP has high photocatalytic performance for p-nitrophenol under visible light. FeTCPP also has peroxisase-like activity, which is used in bionic catalysis research[1][2]. Dec 20 2024
E1741 Rupintrivir Rupintrivirvr (AG7088), an antiviral agent, is a potent, selective and irreversible inhibitor of human rhinovirus (HRV) 3C protease. Rupintrivirvr inhibits replication of a panel of 48 different HRV serotypes in H1-HeLA and MRC-5 cell protection assays, with a mean EC50 of 0.023 μM. Rupintrivirvr shows immune-modulatory effect[1][2]. Dec 20 2024
E7701 Piboserod Piboserod (SB 207266) is a selective 5-HT(4) receptor antagonist.IC50 value:Target: 5-HT4 antagonistin vitro: Piboserod did not modify the basal contractions but concentration-dependently antagonized the ability of 5-HT to enhance bladder strip contractions to EFS. In presence of 1 and 100 nM of piboserod, the maximal 5-HT-induced potentiations were reduced to 45.0+/-7.9 and 38.7+/-8.7%, respectively [1].in vivo: Piboserod significantly increased LVEF by 1.7% vs. placebo (CI 0.3, 3.2, P = 0.020), primarily through reduced end-systolic volume from 165 to 158 mL (P = 0.060). There was a trend for greater increase in LVEF (2.7%, CI -1.1, 6.6, P = 0.15) in a small subset of patients not on chronic beta-blocker therapy. There was no significant Dec 20 2024
E7956 Fosmidomycin sodium salt Fosmidomycin sodium salt is a phosphonic acid antibiotic and a antimalarial agent, which is active against both Gram-negative and Gram-positive bacteria. Dec 20 2024
S2463 LY2334737 LY2334737 is an nucleoside analog and is an orally active proagent of Gemcitabine. LY2334737 exhibits inhibitory activity against enterovirus A71 (EV-A71) infection. LY2334737 has antiviral and anticancer effects[1][2]. Dec 20 2024
E7702 Calcein Blue Calcein Blue, a membrane-impermeant fluorescent dye, is a coumarin derivative that contains an iminodiacetic acid structure. Calcein Blue is also a metallofluorochromic indicator[1][2][3]. Dec 20 2024
E7957 tcY-NH2 tcY-NH2 ((trans-Cinnamoyl)-YPGKF-NH2) is a potent selective PAR4 antagonist peptide. tcY-NH2 inhibits thrombin- and AY-NH2-induced platelet aggregation and endostatin release, and can be used in the research of inflammation, immunology[1][2][6]. Dec 20 2024
E4638 PI-828 PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively[1]. Dec 20 2024
E7703 A 419259 trihydrochloride A 419259 trihydrochloride is a Src family kinases inhibitor with IC50s of 9 nM, 3 nM and 3 nM for Src, Lck and Lyn, respectively[1][2]. Dec 20 2024
E7958 Polymyxin B nonapeptide Polymyxin B nonapeptide is a cyclic peptide obtained from Polymyxin B by proteolytic removal of its terminal amino acyl residue. Polymyxin B nonapeptide is less toxic, lacks bactericidal activity, and retains its ability to render gram-negative bacteria susceptible to several antibiotics by permeabilizing their outer membranes[1][2][3]. Dec 20 2024
E1527 Icomidocholic acid Icomidocholic acid (Aramchol) is a conjugate of cholic acid and arachidic acid that could inhibit stearoyl coenzyme A desaturase 1 (SCD1) activity. Icomidocholic acid has potential use in nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH) treatment[1]. Dec 20 2024
E7704 CARM1-IN-1 CARM1-IN-1 is a potent and specific CARM1(Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 uM; shows very low activity against PRMT1 and SET7(IC50 > 600 uM). IC50 value: 8.6 uM [1]Target: CRAM1 inhibitorin vitro: CARM1-IN-1(Cmp 7g) displayed high and selective CARM1 inhibition, with lower or no activity against a panel of different PRMTs or HKMTs. In human LNCaP cells, 7g showed a significant dose-dependent reduction of the PSA promoter activity. Dec 20 2024
E7959 Inolitazone Inolitazone a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition. Dec 20 2024
E2386 c-Met inhibitor 1 c-Met inhibitor 1 is an inhibitor of the c-Met receptor signaling pathway useful for the treatment of cancer including gastric, glioblastoma, and pancreatic cancer. IC50 value:Target: c-MetMore details please refer to Patent WO 2012015677 A1. Dec 20 2024
E7705 LE 300 LE 300 is a potent and selective dopamine D1-like receptor antagonist with Kis of 1.9 nM and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively. LE 300 is an antagonist of the 5-HT2A receptor with a pA2 of 8.32 in a rat tail artery assay[1][2]. Dec 20 2024
E7960 DAA-1106 DAA1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), as a potent and selective agonist at the peripheral benzodiazepine receptor.Target:PBRin vitro: DAA1106 binding to PBR was significantly increased in widespread areas in MCI subjects when compared to healthy controls.[1] DAA-1106 is a drug which acts as a potent and selective agonist at the peripheral benzodiazepine receptor, also known as the mitochondrial 18 kDa translocator protein or TSPO, but with no affinity at the GABAA receptor. [2]in vivo: DAA-1106 has anxiolytic effects in animal studies. DAA-1106 has a sub-nanomolar binding affinity (Ki) of 0.28nM, and has been used extensively in its 3H or 11C radiolabelled form to map TSPO in the body and bra Dec 20 2024
E1730 Metergoline Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na+ channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation[1][2][3]. Dec 20 2024
E7706 CY 208-243 CY 208-243 is a selective dopamine D1 receptor agonist which exhibits antiparkinsonian activity[1]. Dec 20 2024
E7961 Inolitazone dihydrochloride Inolitazone dihydrochloride (Efatutazone dihydrochloride) is a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition. Dec 20 2024
E1456 Vesnarinone Vesnarinone (OPC-8212) is an orally active phosphodiesterase 3 (PDE3) inhibitor. Vesnarinone can increase in calcium flux and decrease in potassium flux. Vesnarinone shows dose-dependent positive inotropic activity. Vesnarinone can be used in heart failure research[1][2][3][4]. Dec 20 2024
E7707 7-Chlorokynurenic acid 7-Chlorokynurenic acid (7-CKA) is a potent and selective antagonist of the glycine B coagonist site of the N-methyl-D-aspartate (NMDA) receptor (IC50=0.56 μM). 7-Chlorokynurenic acid is also a potent inhibitor of the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM. 7-Chlorokynurenic acid has potent antinociceptive actions after neuraxial delivery[1][2]. Dec 20 2024
E7962 Sisunatovir Sisunatovir (RV521), an orally available inhibitor of the RSV protein, exhibits potent efficacy against a panel of clinical isolates of RSV-A and RSV-B viruses, with IC50s of 1.4 nM and 1.0 nM, respectively[1]. Dec 20 2024
S7615 MS417 MS417 is a selective BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM). Dec 20 2024
S7695 BAZ2-ICR BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe[1]. Dec 20 2024
E7708 CGP7930 CGP7930 (3-(3’,5’-Di-tert-butyl-4’-hydroxy) phenyl-2, 2-dimethylpropanol) is a positive metabotropic GABAB receptor allosteric modulator. CGP7930 enhances the inhibitory effect of l-baclofen on the oscillatory activity of cultured cortical neurons[1]. Dec 20 2024
E7963 Pipequaline Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity[1][2]. Dec 20 2024
E6014 Primaquine Primaquine, an 8-aminoquinoline, is an antimalarial agent and a potent gametocytocidal in falciparum malaria. It also prevents relapse in vivax and ovale malaria. Dec 20 2024
E1416 Rilapladib Rilapladib (SB 659032) is a selective Lp-PLA2 (lipoprotein-associated phospholipase A2) inhibitor with an IC50 of 230 pM[1]. Rilapladib (SB 659032) is also a PAFR (Platelet Activating Factor Receptor) antagonist[2]. Dec 20 2024
E7709 N-Acetylhistamine N-Acetylhistamine is a histamine metabolite. N-acetylhistamine can be used as a potential biomarker of histidine metabolism for anaphylactoid reactions. Dec 20 2024
E7964 2'-C-Methyladenosine 2'-C-Methyladenosine is an inhibitor of hepatitis C virus (HCV) replication. 2'-C-Methyladenosine inhibits HCV replicon and NS5B-catalyzed RNA synthesis with IC50 values of 0.3μM and 1.9 μM, respectively. 2'-C-Methyladenosine also potently inhibits LRV1 in Leishmania guyanensis (Lgy) and Leishmania braziliensis[1][2]. Dec 20 2024
E4995 Cl-amidine hydrochloride Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model[1][2][3][4][5]. Dec 20 2024
E8145 PRT-060318 PRT-060318 (PRT318) is a novel selective inhibitor of the tyrosine kinase Syk with an IC50 of 4 nM. Dec 20 2024
E7710 CP-640186 hydrochloride CP-640186 hydrochloride is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 hydrochloride can also stimulate muscle fatty acid oxidation[1][2]. Dec 20 2024
E7965 (2S)-6-Prenylnaringenin (2S)-6-Prenylnaringenin is the most efficient compound in forebrain. (2S)-6-Prenylnaringenin acts as a GABAA positive allosteric modulator at α+β- binding interface[1]. Dec 20 2024
E2383 SR-3677 SR-3677 is a potent and selective ROCK-II inhibitor with an IC50 of ~3 nM. Dec 20 2024
E7711 Manganese(salen) chloride Manganese(salen) chloride (EUK-8), a superoxide dismutase and catalase mimetic, is an antioxidant with oxyradical scavenging properties. Manganese(salen) chloride ameliorates acute lung injury in endotoxemic swine[1][2]. Dec 20 2024
E7966 Nicotinic acid mononucleotide Nicotinic acid mononucleotide (NAMN) is formed from nicotinic acid (NA) via the nicotinic acid phosphoribosyltransferase in the biosynthesis of NAD+. Nicotinate mononucleotide is a substrate for nicotinamide mononucleotide/Nicotinic acid mononucleotide adenylyltransferase[1][2]. Dec 20 2024
E7457 Cebranopadol Cebranopadol is an analgesic NOP and opioid receptor agonist with Kis/EC50s of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM for human NOP, MOP, KOP and delta-opioid peptide (DOP) receptor, respectively. Dec 20 2024
E7712 Sucrose phosphorylase Sucrose phosphorylase is a bacterial transglucosidase that catalyzes the conversion of sucrose and phosphate into α-D-glucose-1-phosphate and D-fructose. The glucosylated Sucrose phosphorylase can also be hydrolyzed into α-D-glucose, or transfer the glucoyl to the hydroxyl group of the receptor, and then decomposed into new α-D-glucoside products. The enzymatic activity of base phosphorylase to substrate and product is weak[1]. Dec 20 2024
E7967 Isoformononetin Isoformononetin is an analog of Daidzein (HY-N0019) and has immunoprotective effects. Isoformononetin inhibits the differentiation of Th17 and B-cells lymphopoesis to promote osteogenesis in estrogen-deficient bone loss conditions[1]. Dec 20 2024
E7458 Dehydrocorydaline chloride Dehydrocorydaline chloride (13-Methylpalmatine chloride) is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP[1]. Dehydrocorydaline chloride elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities[2]. Dehydrocorydaline chloride shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain[3]. Dec 20 2024
E7713 Uridine diphosphate glucose Uridine diphosphate glucose (Standard) is the analytical standard of Uridine diphosphate glucose. This product is intended for research and analytical applications. Uridine diphosphate glucose is the precursor of glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids in animal tissues and in some microorganisms. Uridine diphosphate glucose is an agonist of the P2Y14 receptor, a neuroimmune system GPCR. Dec 20 2024
E7968 Phaseollin Phaseollin is an isoflavonoid phytoalexin that can be isolated from Phaseolus vulgaris . Phaseollin is toxic to bean hypocotyl and endocarp cells, and causes a complete lysis of sheep erythrocytes[1]. Dec 20 2024
E7459 TMC353121 TMC353121 is a potent respiratory syncytial virus (RSV) fusion inhibitor with pEC50 of 9.9. Dec 20 2024
E7714 Imatinib-d8 Imatinib-d8 is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2]. Dec 20 2024
E7969 Moracin D Moracin D is a flavonoid that can be isolated from Morus alba. Moracin D induces cell apoptosis and shows hypoglycemic, antiadipogenic, antifungal and antitumor effects. Moracin D can be used for fungal infection and breast cancer research[1][2][3]. Dec 20 2024
E7460 K145 hydrochloride K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 μM and a Ki of 6.4 μM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity[1]. Dec 20 2024
E7715 Ivermectin B1a Ivermectin B1a, a derivative of Avermectin B1a (HY-15308), is a main component of Ivermectin (HY-15310)[1]. Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19[2]. Dec 20 2024
E7970 Pyronaridine Pyronaridine is an orally active Mannich base anti-malarial agent. Pyronaridine is active against P. falciparum and Echinococcus granulosus infection[1][2]. Dec 20 2024
E7461 K-7174 K-7174 is an orally active proteasome and GATA inhibitor. K-7174 is a cell adhesion inhibitor. K-7174 induces cell apoptosis. K-7174 shows antitumor activities, it can be used for the research of cancer[1][2][3]. Dec 20 2024
E7716 Dihydroergotamine mesylate Dihydroergotamine mesylate is an ergot alkaloid that can be used for the research of migraines[1][2][3]. Dec 20 2024
E7971 (+)-Afzelechin (+)-Afzelechin, isolated from rhizomes of Bergenia ligulata, is an alpha-glucosidase activity inhibitor with an ID50 (50% inhibition dose) value of 0.13 mM. (+)-Afzelechin can delay the absorption of carbohydrates in food to suppress postprandial hyperglycemia and hyperinsulinemia[1]. Dec 20 2024
E7462 Merestinib dihydrochloride Merestinib dihydrochloride (LY2801653 dihydrochloride) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib dihydrochloride also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM)[1][2]. Dec 20 2024
E7717 Quinidine sulfate Quinidine Monosulfate is an antiarrhythmic agent. Quinidine Monosulfate is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine Monosulfate is also a K+ channel blocker with an IC50 of 19.9 μM, and can induce apoptosis. Quinidine Monosulfate can be used for malaria research[1][2][3][4]. Dec 20 2024
E7972 Isosilybin A Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis[1][2]. Dec 20 2024
E7463 LM11A-31 dihydrochloride LM11A-31 dihydrochloride, a non-peptide p75NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. LM11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression[1][2]. Dec 20 2024
E7718 CJ-42794 CJ-42794 (CJ-042794) is a potent, orally active, selective prostaglandin E receptor 4 (EP4) antagonist with an IC50 value of 10 nM, which is 200-fold more selective than EP1, EP2 and EP3. CJ-42794 can be used in research of gastric ulcers[1][2]. Dec 20 2024
E7973 Isosilybin B Isosilybin B, a flavonolignan isolated from Silybum marianum, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation[1][2]. Dec 20 2024
E7464 BMS-345541 hydrochloride BMS-345541 hydrochloride is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK. Dec 20 2024
E7719 Imisopasem manganese Imisopasem manganese (M40403) is a stable non-peptidyl mimetic of manganese superoxide MnSOD. Dec 20 2024
E7974 Tenofovir diphosphate Tenofovir diphosphate (TFV-DP) is a competitive DNA polymerases inhibitor (with respect to dATP) and a substrate of HIV type 1 (HIV-1) reverse transcriptase (RT)[1]. Dec 20 2024
E7465 Narlaprevir Narlaprevir (SCH 900518) is a selective and orally bioavailable NS3 protease inhibitor with a Ki value of 6 nM and an EC90 value of 40 nM[1]. Narlaprevir also inhibits the HCV nonstructural protein 3 serine protease[2]. Narlaprevir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.3 μM[3]. Dec 20 2024
E7720 Methyl 3-O-methylgallate Methyl 3-O-methylgallate (M3OMG) possesses antioxidant effect and can protect neuronal cells from oxidative damage[1]. Dec 20 2024
E7975 CCG-63802 CCG-63802 is a selective, reversible and allosteric RGS4 inhibitor. CCG-63802 specifically binds to RGS4 and blocks the RGS4-Gαo interaction, with an IC50 value of 1.9 μM[1]. Dec 20 2024
E7466 GW627368 GW627368 (GW627368X) is a novel, potent and selective competitive antagonist of prostanoid EP4 receptor with additional human TP receptor affinity, with pKi values of 7.0 and 6.8 for human prostanoid EP4 and TP receptors respectively[1]. Dec 20 2024
E7721 Bicyclomycin benzoate Bicyclomycin benzoate is an antibiotic exhibiting activity against a broad spectrum of Gram-negative bacteria and against the Gram-positive bacterium. Dec 20 2024
E7976 Asparagusic acid Asparagusic acid is a sulfur-containing flavor component produced by Asparagus officinalis Linn., with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor[1][2][3]. Dec 20 2024
E7467 Hematoporphyrin Hematoporphyrin (Hematoporphyrin IX), a photosensitizer, is a substrate for affinity chromatography of heme-binding proteins. Hematoporphyrin can induce apoptosis in U87 glioma cells and decrease tumor growth in vivo when exposed to red light[1][2][3]. Dec 20 2024
E7722 Hardwickiic acid Hardwickiic acid ((-)-Hardwikiic acid) is an antinociceptive compound that blocks Tetrodotoxin-sensitive voltage-dependent sodium channels. Hardwickiic acid shows insecticidal activity[1][2]. Dec 20 2024
E7977 Choline-d9 chloride Choline-d9 (chloride) is the deuterium labeled Choline chloride. Choline chloride is an organic compound and a quaternary ammonium salt, an acyl group acceptor and choline acetyltransferase substrate, also is an important additive in feed especially for chickens where it accelerates growth. Dec 20 2024
E7468 Defactinib hydrochloride Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner. Dec 20 2024
E7723 GS-6201 GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM)[1]. GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse[2]. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice[3]. Dec 20 2024
E7978 Danegaptide Danegaptide (GAP-134) is a potent, selective and orally active gap-junction modifier with an antiarrhythmic effect[1][2]. Dec 20 2024
E7469 Cholera toxin Cholera toxin (Choleragen), an AB(5)-subunit toxin, enters host cells by binding the ganglioside GM1 at the plasma membrane (PM) and travels retrograde through the trans-Golgi Network into the endoplasmic reticulum (ER)[1]. Choleragen activates adenylate cyclase by catalyzing ADP-ribosylation of Gs alpha, the stimulatory guanine nucleotide-binding protein[2]. Dec 20 2024
E7724 DGAT1-IN-1 DGAT1-IN-1 is a potent DGAT1 inhibitor with IC50 of < 10 nM(cell lysate from Hep3B cells overexpressing human DGAT1).IC50 value: < 10 nMTarget: DGAT1 inhibitorImidazopyridine and imidazothiazole compounds as inhibitors of diacylglycerol o-acyltransferase type 1 enzyme and their preparationBy Kim, Dooseop; Bok, Juhan; Shin, Sunmi From PCT Int. Appl. (2013), WO 2013119040 A1 20130815. Dec 20 2024
E7979 NBI-98782 NBI-98782 is a high affinity and selectivity vesicular monoamine transporter 2 (VMAT2) inhibitor with a Ki of 3 nM. NBI-98782 has antipsychotic activity[1]. Dec 20 2024
E7470 AGN 194310 AGN 194310 (VTP-194310) is a high affinity, potent and selective retinioic acid receptors (RARs) pan-antagonist with Kd values of 3 nM, 2 nM, 5 nM for RARα, RARβ, RARγ, respectively[1][2]. AGN 194310 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 20 2024
E7725 Doxepin Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant. Doxepin has therapeutic effects in atopic dermatitis，chronic urticarial，can improve cognitive processes， protect central nervous system. Doxepin has also been proposed as a protective factor against oxidative stress[1][2][3]. Dec 20 2024
E7980 Fumitremorgin C Fumitremorgin C is a potent and selective ABCG2/BRCP inhibitor. Dec 20 2024
E7471 GW311616 GW-311616 is a potent, orally bioavailable, long duration and selective human neutrophil elastase (HNE) inhibitor with IC50 value of 22 nM and Ki value of 0.31 nM[1]. Dec 20 2024
E7726 Palmitelaidic Acid Palmitelaidic Acid (9-trans-Hexadecenoic acid) is the trans isomer of palmitoleic acid. Palmitoleic acid is one of the most abundant fatty acids in serum and tissue. Dec 20 2024
E7981 Nelotanserin Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively. Dec 20 2024
E7472 Pam3CSK4 Pam3CSK4 is a toll-like receptor 1/2 (TLR1/2) agonist with an EC50 of 0.47 ng/mL for human TLR1/2[1]. Dec 20 2024
E7727 Clavulanate lithium Clavulanate lithium is a potent β-lactamase inhibitor and acts as an antibiotic[1][2]. Dec 20 2024
E7982 Cirsilineol Cirsilineol, a natural flavone compound, selectively inhibits IFN-γ/STAT1/T-bet signaling in intestinal CD4+ T cells. Cirsilineol has potent immunosuppressive and anti-tumor properties. Cirsilineol significantly ameliorates trinitro-benzene sulfonic acid (TNBS)-induced T-cell-mediated experimental colitis in mice[1]. Dec 20 2024
E7473 UAMC-3203 hydrochloride UAMC-3203 hydrochloride is a potent and selective Ferroptosis inhibitor with an IC50 of 12 nM[1]. Dec 20 2024
E7728 Hydroxocobalamin monohydrochloride Hydroxocobalamin monohydrochloride (Vitamin B12a monohydrochloride) is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the treatment of vitamin B12 deficiency including pernicious anemia[1][2]. Dec 20 2024
E7983 EIDD-2749 EIDD-2749 (4'-Fluorouridine) is an orally active RdRp inhibitor. EIDD-2749 effectively blocks the replication of RSV and SARS-CoV-2. EIDD-2749 also exhibits activity against HCV and lymphocytic choriomeningitis virus (LCMV). EIDD-2749 is a promising oral therapeutic candidate for COVID-19 and is also suitable for research on other RNA viruses[1][2][3]. Dec 20 2024
E7474 PFI-2 PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0  nM and (S)-PFI-2 shows inhibiting activity with IC50  value of 1.0  μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis[1][2]. Dec 20 2024
E7729 AMG-3969 AMG-3969 is a potent glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor with an IC50 of 4 nM. Dec 20 2024
E7984 Fenbendazole-d3 Fenbendazole-d3 is a deuterium labeled Fenbendazole. Fenbendazole-d3 is a HIF-1α agonist and activates the HIF-1α-related GLUT1 pathway. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53[1][2][3][4]. Dec 20 2024
E7475 AM095 AM095 is a selective LPA1 receptor antagonist. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively. Dec 20 2024
E7730 CCT244747 CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM. Dec 20 2024
E7985 Carbenicillin Carbenicillin is a broad-spectrum semi-synthetic penicillin antibiotic for gram-negative bacteria. Carbenicillin can interfere the cell wall synthesis while displaying low toxicity to plant tissue[1][2]. Dec 20 2024
E7476 TY-52156 TY-52156 is a potent and selective S1P3 receptor antagonist with a Ki value of 110 nM[1]. Dec 20 2024
E7731 ML-030 ML-030 is a potent PDE4 inhibitor, with IC50 of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 49.2 nM for PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and PDE4D2, respectively. Dec 20 2024
E7986 Ticarcillin Ticarcillin is a semisynthetic, extended-spectrum, carboxypenicillin antibacterial agent, and is active against gram-positive cocci, including streptococci and staphylococci. Ticarcillin is also effective against most gram-negative organisms, including Pseudomonas aeruginosa. Ticarcillin can be used in lower respiratory tract infections, skin and skin structure infections, urinary tract infections, and intraabdominal infections research[1][2][3]. Dec 20 2024
E7732 GNF4877 GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells)[1]. Dec 20 2024
E7987 Ganfeborole hydrochloride Ganfeborole hydrochloride (GSK656) is a potent antitubercular agent, acting as an inhibitor of Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS), with an IC50 of 0.2 μM. Dec 20 2024
E5556 Britannin Dec 20 2024
E7477 Enmetazobactam Enmetazobactam (AAI101) is an extended-spectrum β-lactamase inhibitor, against many resistant Gram-negative pathogens[1][2]. Dec 20 2024
E7733 SB 242084 dihydrochloride SB 242084 dihydrochloride is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (crosses the blood-brain barrier). SB 242084 dihydrochloride increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 dihydrochloride also increases mitochondrial gene expression and oxidative metabolism via 5-HT2A receptor. SB 242084 dihydrochloride has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage[1][2][3]. Dec 20 2024
E7988 Aclacinomycin A hydrochloride Aclacinomycin A (Aclarubicin) hydrochloride is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A hydrochloride is an inhibitor of topoisomerase I and II. Aclacinomycin A hydrochloride inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A hydrochloride might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis[1][2][3]. Dec 20 2024
E7478 Peretinoin Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1[1]. Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression[2]. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC50 of 9 μM[3]. Dec 20 2024
E7734 5-Pentadecylresorcinol 5-Pentadecylresorcinol (Adipostatin A) is a glycerol-3-phosphate dehydrogenase (GPDH) inhibitor with an IC50 of 4.1 µM. Adipostatin A shows good larvicidal activity against Aedes aegypti[1][2]. Dec 20 2024
E7989 Telcagepant Telcagepant (MK-0974) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with Kis of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively. Dec 20 2024
E7479 Cyclo(Phe-Pro) Cyclo(Phe-Pro) (Cyclo(phenylalanylprolyl)), a Vibrio vulnificus quorum-sensing molecule, inhibits retinoic acid-inducible gene-I (RIG-I) polyubiquitination, through its specific interaction with RIG-I, to blunt IRF-3 activation and type-I IFN production. Cyclo(Phe-Pro) (Cyclo(phenylalanylprolyl)) enhances susceptibility to hepatitis C virus (HCV), as well as Sendai and influenza viruses[1]. Dec 20 2024
E7735 5-Hydroxylansoprazole 5-Hydroxylansoprazole (AG1908) is an active metabolite of Lansoprazole in plasma. Lansoprazole is metabolized by CYP2C19 forming 5-Hydroxylansoprazole. Lansoprazole is a gastric proton-pump inhibitor and is effective in the treatment of various peptic diseases[1][2]. Dec 20 2024
E7990 Ecteinascidin 770 Ecteinascidin 770 (ET-770) is a 1,2,3,4-tetrahydroisoquinoline alkaloid with potent anti-cancer activities; inhibits U373MG cells with an IC50 of 4.83 nM. Dec 20 2024
E7480 BAY-598 BAY-598 is selective small molecule inhibitor of SMYD2 with an IC50 of 27 nM[1][2]. Dec 20 2024
E7736 FlAsH-EDT2 FlAsH-EDT2 is a protein labeling reagent. FlAsH-EDT2 also is a membrane-permeant fluorogenic biarsenicals. FlAsH-EDT2 binds to CCXXCC motifs and non-specifically to endogenous cysteine-rich proteins. FlAsH-EDT2 can be useful only for labeling those recombinant proteins that express at a very high level[1][2]. Dec 20 2024
E7991 Harmol Harmol is a TFEB activator, an orally active monoamine oxidase inhibitor that has anti-tumor, anti-depressant, and anti-aging effects. Harmol can induce cell mitosis, autophagy and apoptosis. Harmol promotes the degradation of α-synuclein through the regulation of the autophagy-lysosomal pathway, improving motor deficits in mouse models of Parkinson's disease[1][2][3][4]. Dec 20 2024
E7481 Givinostat Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Dec 20 2024
E7737 Adenosine 5′-diphosphoribose sodium Adenosine 5′-diphosphoribose sodium (ADP ribose sodium) is a nicotinamide adenine nucleotide (NAD+) metabolite. Adenosine 5′-diphosphoribose sodium is the most potent and primary intracellular Ca2+-permeable cation TRPM2 channel activator. Adenosine 5′-diphosphoribose sodium also can enhance autophagy[1][2]. Dec 20 2024
E7992 Endoxifen Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study[1][2]. Dec 20 2024
E7482 Z-Gly-Gly-Arg-AMC acetate Z-Gly-Gly-Arg-AMC acetate is a thrombin-specific fluorogenic substrate for testing of thrombin generation in PRP and platelet-poor plasma (PPP). Dec 20 2024
E7738 Alkynyl myristic acid Alkynyl myristic acid is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Alkynyl myristic acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 20 2024
E7993 CCG-63808 CCG-63808 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins. Dec 20 2024
E7483 Pifithrin-α, p-Nitro, Cyclic Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED50=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue[1][2]. Dec 20 2024
E7739 8-Azaadenosine 8-Azaadenosine is a potent ADAR1 inhibitor and an A-to-I editing inhibitor. 8-Azaadenosine blocks RNA editing and inhibits proliferation, 3D growth, invasion, and migration in thyroid cancer cells[1][2]. Dec 20 2024
E7994 Imidazoleacetic acid Imidazoleacetic acid is an endogenous ligand that stimulates imidazole receptors. Dec 20 2024
S8703 Milademetan Milademetan(RAIN-32, DS-3032) is an oral, selective inhibitor of the MDM2-p53 complex that reactivates p53 to induce cancer cell apoptosis and exhibits an anti-tumor effect. Dec 20 2024
E7484 Cligosiban Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents[1][2]. Dec 20 2024
E7740 Ocaperidone Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT2, a1-adrenergic receptor, dopamine D2, histamine H1 and a2-adrenergic receptor, respectively, and a pEC50 and pKi of 7.60 and 8.08 for h5-HT1A. Dec 20 2024
E7995 Crosstide Crosstide is a peptide analog of glycogen synthase kinase α/β fusion protein sequence which is a substrate for Akt. Dec 20 2024
E7485 U-46619 U-46619 (9,11-Methanoepoxy PGH2) is a stable analogue of Thromboxane A2 (HY-113350) (TXA2) and acts as a potent TXA2 (TP) agonist. U-46619 also is a RhoA agonist. U-46619 stimulates the activation of RhoA through TXA2 receptor activation[1][4][5]. Dec 20 2024
E7741 WEHI-345 WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation[1]. Dec 20 2024
E7996 Roquefortine C Roquefortine C, a fungal cyclopeptide isolated from Penicillium roquefortii, activates P-gp and also inhibits P450-3A and other haemoproteins. Roquefortine C has bacteriostatic activities against Gram-positive bacteria[1]. Dec 20 2024
E5579 Asatone Dec 20 2024
E7486 MC-DOXHZN MC-DOXHZN ((E/Z)-Aldoxorubicin) is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), with acid-sensitive properties[1]. Dec 20 2024
E7742 12S-HHT 12S-HHT (12(S)-HHTrE) is an enzymatic product of prostaglandin H2 (PGH2) derived from cyclooxygenase (COX)-mediated arachidonic acid metabolism. 12S-HHT is an endogenous ligand for BLT2 that fully activates BLT2 in vivo. 12S-HHT suppresses UV-induced IL-6 synthesis in keratinocytes, exerting an anti-inflammatory activity[1][2]. Dec 20 2024
E7997 Pristinamycin IA Pristinamycin IA (Mikamycin B) is a cycle-peptidic macrolactone antibiotic. Pristinamycin IA is a substrate of P-glycoprotein and inhibits its function. Pristinamycin IA is active against StaphyloEoccus and Srreptococcus[1]. Dec 20 2024
E7487 Daun02 Daun02 is a proagent of the topoisomerase inhibitor Daunorubicin. Dec 20 2024
E7743 CMS-121 CMS-121 is a quinolone derivative and an orally active acetyl-CoA carboxylase 1 (ACC1) inhibitor. CMS-121 protects HT22 cells against ischemia and oxidative damage with EC50 values of 7 nM and 200 nM, respectively. CMS-121 has strong neuroprotective, anti-inflammatory, antioxidative and renoprotective activities[1][2][3]. Dec 20 2024
E7998 PD 123319 ditrifluoroacetate PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM. Dec 20 2024
E7488 SB 242084 SB 242084 is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (crosses the blood-brain barrier). SB 242084 increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via 5-HT2A receptor. SB 242084 has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage[1][2][3]. Dec 20 2024
E7744 Siramesine Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity[1][2][3]. Dec 20 2024
E7999 GSK-J2 GSK-J2 is an isomer of GSK-J1 that does not have any specific activity. GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A. Dec 20 2024
E7489 MK-0773 MK-0773 is a selective androgen receptor modulators (SARMs) that binds to AR with an IC50 of 6.6 nM. Dec 20 2024
E7745 Milnacipran Milnacipran is a serotonin-norepinephrine reuptake inhibitor (SNRI) used in the clinical treatment of fibromyalgia.Target: SNRIMilnacipran (Ixel, Savella, Dalcipran, Toledomin) is a serotonin-norepinephrine reuptake inhibitor (SNRI) used in the clinical treatment of fibromyalgia. It is not approved for the clinical treatment of major depressive disorder in the USA, but it is in other countries.Milnacipran inhibits the reuptake of serotonin and norepinephrine in an approximately 1:3 ratio, respectively; in practical use this means a relatively balanced action upon bothneurotransmitters. Increasing both neurotransmitters concentration simultaneously works synergistically to treat both depression and fibromyalgia. Milnacipran exerts no signifi Dec 20 2024
E8000 BIX02188 BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM. Dec 20 2024
E7490 Meclofenamic acid Meclofenamic acid (Meclofenamate) is a non-steroidal anti-inflammatory agent. Meclofenamic acid is a highly selective FTO (fat mass and obesity-associated) enzyme inhibitor. Meclofenamic acid competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid is a non-selective gap-junction blocker. Meclofenamic acid inhibits hKv2.1 and hKv1.1, with IC50 values of 56.0 and 155.9 μM, respectively[1][2][3][4]. Dec 20 2024
E7746 Gadopentetic acid Gadopentetic acid (Gd-DTPA) is a paramagnetic contrast agent. Gadopentetic acid commonly implemented by a bolus intravenous injection in Dynamic contrast-enhanced MRI (DCE-MRI) studies. Gadopentetic acid also can be used for the research of nephrogenic systemic fibrosis (NSF)[1][2]. Dec 20 2024
E8001 Rezafungin acetate Rezafungin acetate (Biafungin acetate) is a next-generation, broad-spectrum, and long-lasting echinocandin. Rezafungin acetate shows potent antifungal activity against Candida spp., Aspergillus spp., and Pneumocystis spp.[1][2]. Dec 20 2024
E7491 BS-181 hydrochloride BS-181 hydrochloride is a highly selective CDK7 inhibitor with IC50 of 21 nM, and > 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9. Dec 20 2024
E7747 Ripasudil free base Ripasudil free base (K-115 free base) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively. Dec 20 2024
E8002 Isoguvacine hydrochloride Isoguvacine hydrochloride is a GABA receptor agonist. Dec 20 2024
E7492 Almorexant Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca2+ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis[1][2][3][4]. Dec 20 2024
E7748 Docebenone Docebenone (AA 861) is a potent, selective and orally active 5-LO (5-lipoxygenase) inhibitor. Dec 20 2024
E8003 Tephrosin Tephrosin is a natural rotenoid which has potent antitumor activities. Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors[1]. Dec 20 2024
E4716 QS11 QS11 acts as an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 μM. QS11 regulates Wnt/β-catenin signaling by interacting with ARF GTPase-activating protein 1 (ARFGAP1) and influences protein trafficking. Additionally, QS11 suppresses the migration of breast cancer cells that overexpress ARFGAP1. Dec 20 2024
E7493 Sonidegib diphosphate Sonidegib diphosphate (Erismodegib diphosphate) is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively[1]. Dec 20 2024
E7749 FT011 FT011 is an anti-fibrotic agent, reduces mRNA expression of collagens I and III and inhibits collagen synthesis[1]. FT011 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 20 2024
E8004 Polymyxin B1 Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment[1][2]. Dec 20 2024
E7494 MB05032 MB05032 is a special and efficacious gluconeogenesis inhibitor targeted the AMP binding site of fructose 1,6-bisphosphatase (FBPase) with an IC50 value of 16 nM. Dec 20 2024
E7750 Ro 01-6128 Ro 01-6128 is a positive allosteric modulator of mGluR1[1]. Dec 20 2024
E8005 SB-674042 SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd=5.03 nM), exhibits 100-fold selectivity for OX1 over OX2 receptors with IC50 values of 3.76 nM and 531 nM, respectively[1][4]. Dec 20 2024
E5594 Angoline Dec 20 2024
E7495 SID 26681509 SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G[1]. Dec 20 2024
E7751 PD 90780 PD 90780 is a non peptide antagonist of nerve growth factor (NGF). PD 90780 interacts with NGF, prevents NGF binds with p75NTR. PD 90780 inhibits NGF-p75NTR interaction with IC50s of 23.1 and 1.8 µM in PC12 cells and PC12nnr5 cells, respectively[1] . Dec 20 2024
E8006 Angeloylgomisin O Angeloylgomisin O, a lignin extract of Schisandra rubriflora. Anti-inflammatory properties[1]. Dec 20 2024
E7496 CDK9-IN-2 CDK9-IN-2 is a special cyclin-dependent kinase 9 (CDK9) inhibitor, extracted from patent WO/2012131594A1, compound CDKI(8), has an IC50 of 5 nM and 7 nM in H929 multiple myeloma(MM) cell line (72 hours) and A2058 skin cell line (72 hours), respectively. Dec 20 2024
E7752 Hydroxyphenyl Fluorescein Hydroxyphenyl Fluorescein (HPF) is a stable ROS fluorescent probe dye. Hydroxyphenyl Fluorescein has stronger specificity and stability than H2DCFDA (HY-D0940). Hydroxyphenyl Fluorescein can produce strong green fluorescence through hydroxyl radical reaction with intracellular peroxynitroso. Hydroxyphenyl Fluorescein can be applied for fluorescence microscopy, high-throughput imager, luciferase microplate reader or flow cytometry. Ex/Em=490/515 nm[1]. Dec 20 2024
E8007 NSC139021 NSC139021 (ERGi-USU) is a highly selective inhibitor for the growth of ERG-positive cancer cells with IC50s ranging from 30 to 400 nM. Dec 20 2024
E7497 p-Cresyl sulfate potassium p-Cresyl sulfate potassium is a uremic toxin that binds to a prototype protein. p-Cresyl sulfate potassium activates the JNK and p38 MAPK signaling pathways. p-Cresyl sulfate potassium has pro-inflammatory activity[1][2]. Dec 20 2024
E7753 (E)-4-Oxo-2-nonenal (E)-4-Oxo-2-nonenal (4-ONE) is one of the major hemolytic decomposition products of lipid hydroperoxides. (E)-4-Oxo-2-nonenal is a major product of the FeII-mediated breakdown of lipid hydroperoxides. (E)-4-Oxo-2-nonenal is a potent transient receptor potential ankyrin 1 (TRPA1) agonist[1][2][3]. Dec 20 2024
E8008 QNZ46 QNZ46 is a NR2C/NR2D-selective NMDA receptor non-competitive antagonist (IC50 values are 3, 6, 229, and >300, >300 μM for NR2D, NR2C, NR2A, NR2B, and GluR1, respectively). IC50 value: 3 μM (for NR2D), 6 μM (for NR2C), 229 μM (for NR2D NR2A)Target: NR2D, NR2C, NR2Ain vitro: QNZ46 is a noncompetitive inhibitor of GluN2C/D containing NMDA receptors. KD and IC50 values for binding and inhibition of GluN1/Glun2D receptors by QNZ46 are 4.9 and 3.9 μM, respectively. QNZ46 does not compete for binding of glutamate or glycine, but QNZ46 receptor binding requires the binding of glutamate to the GluN2 subunit. Dec 20 2024
E7498 DCP-LA DCP-LA (FR236924), a linoleic acid derivative, selectively and directly activates PKCε. DCP-LA activates Ca(2+)/calmodulin-dependent protein kinase II (CaMKII) and inhibits protein phosphatase-1 (PP-1) to stimulate AMPA receptor exocytosis. DCP-LA inhibits activation of caspase-3/-9 and protects neurons at least in part from oxidative stress-induced apoptosis[1][2][3]. Dec 20 2024
E7754 FMK 9a FMK 9a is an autophagin-1 inhibitor with IC50 values of 80 and 73 μM in FRET and LRA assay. Dec 20 2024
E8009 4-Azido-L-phenylalanine hydrochloride 4-Azido-L-phenylalanine hydrochloride is an unnatural amino acid, which is used as an effective vibrational reporter of local protein environments. 4-Azido-L-phenylalanine (hydrochloride) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. Dec 20 2024
E7499 WAY-100635 WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71.WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist[1][2][3]. Dec 20 2024
E7755 DSPE-PEG2000-Mal ammonium DSPE-PEG-Maleimide has DSPE phospholipid and maleimide to prepare nanostructured lipid carrier. DSPE-PEG-Maleimide extends blood circulation time and higher stability for encapsulated agents[1][2]. DSPE-PEG5000-Mal ammonium contains PEG5000. Dec 20 2024
E8010 Methylproamine Methylproamine is a DNA-binding radioprotector, acts by repair of transient radiation-induced oxidative species on DNA. Methylproamine also protects against ionizing radiation by preventing DNA double-strand breaks[1]. Dec 20 2024
E7500 BOC-D-FMK Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor. Boc-D-FMK inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM. Dec 20 2024
E7756 Imipramine Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects[1][2][3][4][5]. Dec 20 2024
E8011 TAS-103 dihydrochloride TAS-103 dihydrochloride is a dual inhibitor of DNA topoisomerase I/II, used for cancer research. Dec 20 2024
E7501 MK 0893 MK 0893 is a potent and selective glucagon receptor antagonist with an IC50 of 6.6 nM. Dec 20 2024
E7757 TNP-470 TNP-470 is a methionine aminopeptidase-2 inhibitor and also an angiogenesis inhibitor. Dec 20 2024
E8012 2-(Methylamino)-1H-purin-6(7H)-one 2-(Methylamino)-1H-purin-6(7H)-one (N2-Methylguanine) is a modified nucleoside. 2-(Methylamino)-1H-purin-6(7H)-one is an endogenous methylated nucleoside found in human fluids. Dec 20 2024
E7502 J-113863 J-113863 is a potent and selective CCR1 antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect[1][2][3]. Dec 20 2024
E7758 AF12198 AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo[1]. Dec 20 2024
E8013 Deoxycytidine triphosphate Deoxycytidine triphosphate (dCTP) is a nucleoside triphosphate that can be used for DNA synthesis. Deoxycytidine triphosphate has many applications, such as real-time PCR, cDNA synthesis, and DNA sequencing[1][2][3]. Dec 20 2024
E7503 Hydroxyfasudil Hydroxyfasudil is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively. Dec 20 2024
E7759 GRGDSP GRGDSP, a synthetic linear RGD peptide, is an integrin inhibitor. Dec 20 2024
E8014 ML 145 ML 145 is a selective and competitive human GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM. ML 145 has over 1000-fold more selective for GPR35 compared to GPR55 (IC50/EC50=21.7 μM)[1]. ML 145 has no significant activity for GPR35 at either rodent ortholog[2]. Dec 20 2024
E7504 AZ-23 AZ-23 is an ATP-competitive and orally bioavailable Trk kinase A/B/C inhibitor with IC50s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck), respectively. Dec 20 2024
E7760 DNP-X, SE DNP-X, SE (6-(2,4-Dinitrophenyl)aminohexanoic acid, succinimidyl ester), the DNP-X acid modified by succinimidyl ester, is an amine-reactive building block for developing a probe, which can be recognized by anti-DNP antibodies. DNP-X, SE (6-(2,4-Dinitrophenyl)aminohexanoic acid, succinimidyl ester) is also an excellent amine-reactive FRET quencher paired with Trp or Tyr. Dec 20 2024
E8015 ABT-239 ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist. Dec 20 2024
E7505 GN44028 GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers[1][3]. Dec 20 2024
E7761 GSK319347A GSK319347A is a dual inhibitor of TBK1 and IKKε with IC50s of 93 nM and 469 nM, respectively. GSK319347A also inhibits IKK2 with an IC50 of 790 nM. Dec 20 2024
E8016 β-Amyloid (1-40) (rat) β-Amyloid (1-40) (rat) is a rat form of the amyloid β-peptide, which accumulates as an insoluble extracellular deposit around neurons, giving rise to the senile plaques associated with Alzheimer's disease (AD). β-Amyloid (1-40) (rat) increases 45Ca2+ influx, induces neurodegeneration in the rat hippocampal neurons of the CA1 subfield. β-Amyloid (1-40) (rat) induces apoptosis. β-Amyloid (1-40) (rat) can be used for the research of Alzheimer's disease[1][2]. Dec 20 2024
E7506 Fluorescein di(β-D-galactopyranoside) Fluorescein di(β-D-galactopyranoside) is a fluorogenic substrate for β-galactosidase (λex=485 nm, λem=535 nm). Dec 20 2024
E7762 CTCE-9908 CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells[1][2]. Dec 20 2024
E8017 OR-1896 OR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) III isoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K+ channels and has Ca2+-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation[1]. Dec 20 2024
E7507 L-Azidohomoalanine hydrochloride L-Azidohomoalanine hydrochloride is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1]. L-Azidohomoalanine (hydrochloride) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. Dec 20 2024
E7763 UDP-rhamnose UDP-rhamnose is one of the substrates for pectin synthesis in cell wall. UDP-rhamnose can be identified in fungi, it is one of the most common sugar donor in plants[1]. Dec 20 2024
E8018 BAY-299 BAY-299 is a very potent, dual inhibitor with IC50s of 67 nM for BRPF2 bromodomains (BD), 8 nM for TAF1 BD2, and 106 nM for TAF1L BD2. Dec 20 2024
E7508 Levcromakalim Levcromakalim ((-)-Cromakalim) is an ATP-sensitive K+ channel (KATP) activator. Dec 20 2024
E7764 Atrial natriuretic factor (1-28) (human, porcine) Atrial natriuretic factor (1-28) (human, porcine) is a potent suppressor of pro-opiomelanocortin (POMC) mRNA but a weak inhibitor of βEP-LI release[1][2]. Dec 20 2024
E8019 TD-198946 TD-198946, a thienoindazole derivative, is a potent chondrogenic agent. Dec 20 2024
E7509 Ipatasertib dihydrochloride Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive pan-Akt inhibitor with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively. Dec 20 2024
E7765 5-(N,N-Hexamethylene)-amiloride 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na+/H+ exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively[1][2]. Dec 20 2024
E8020 Bepridil hydrochloride Bepridil hydrochloride (CERM 1978) is a calcium channel blocker, with antianginal activity. Dec 20 2024
E7510 SCH 563705 SCH 563705 is a potent and orally available CXCR2 and CXCR1 antagonist, with IC50s of 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively. Dec 20 2024
E7766 Selenocystine Selenocystine is a broad-spectrum anti-cancer agent. Selenocystine induces DNA damage in HepG2 cells, particularly in the form of DNA double strand breaks (DSBs). Selenocystine exhibits great promise as a therapeutic or adjuvant agent targeting DNA repair for cancer treatment[1]. Dec 20 2024
E8021 NADP sodium hydrate NADP sodium hydrate is the sodium salt hydrate form of NADP (HY-113325). NADP is a coenzyme involved in cellular electron transfer reactions in biological metabolism, which is alternately oxidized (NADP+) and reduced (NADPH), and can maintain cellular redox homeostasis and regulate many biological events, including cellular metabolism. NADPH is a universal electron donor that provides reducing ability for synthetic metabolic reactions and redox balance. NADPH plays a multifunctional role in regulating inflammation, redox homeostasis, and synthetic metabolism processes[1][4]. Dec 20 2024
E7511 MI-773 MI-773 is a potent MDM2-p53 protein‐protein interaction (PPI) inhibitor with high binding affinity against MDM2 (Kd=8.2 nM). MI-773 has antitumor activity[1][2]. Dec 20 2024
E7767 Calcein Blue AM Calcein Blue AM is a cellular dye agent[1]. Dec 20 2024
E8022 AZ505 ditrifluoroacetate AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM. Dec 20 2024
E7512 NB-598 Maleate NB-598 Maleate is a potent and competitive inhibitor of squalene epoxidase (SE), and suppresses triglyceride biosynthesis through the farnesol pathway. NB-598 (Maleate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 20 2024
E7768 C527 C527 is a is a pan DUB enzyme inhibitor, with a high potency for the USP1/UAF1 complex (IC50=0.88 μM). Dec 20 2024
E8023 Proctolin Proctolin is an endogenous pentapeptide that acts as an excitatory neuromodulator. Dec 20 2024
E7513 Ro 25-6981 Ro 25-6981 is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 has the potential for the research of parkinson's disease (PD)[1][2][3]. Dec 20 2024
E7769 GRF (1-29) amide (rat) GRF (1-29) amide (rat) is a synthetic peptide which can stimulate the growth hormone (GH) secretion. Dec 20 2024
E8024 AC-55541 AC-55541 is a highly selective protease-activated receptor 2 (PAR2) agonist (pEC50=6.7), displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation. AC-55541 has pEC50 values of 5.9 and 6.6 in PI hydrolysis assays and Ca2+ mobilization assays and exhibits pronociceptive activity in vivo[1]. Dec 20 2024
E7514 CCT241533 CCT241533 is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM[1]. Dec 20 2024
E7770 MCLA hydrochloride MCLA hydrochloride is a chemiluminescent reagent which can be used to quantify aqueous concentrations of superoxide. Dec 20 2024
E8025 Gadobutrol Gadobutrol (Gd-DO3A-butrol; ZK 135079) is a nonionic paramagnetic macrocyclic gadolinium-based contrast agent that can be used for magnetic resonance imaging (MRI)[1]. Dec 20 2024
E7515 Elacridar hydrochloride Elacridar hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on agent distribution to brain and it can be used for the research of cancer[1][2]. Dec 20 2024
E7771 GSK-3 inhibitor 1 GSK-3 inhibitor 1 (compound core 3) is a GSK-3 inhibitor that induces stem/progenitor cell self-renewal (e.g. induces stem/progenitor cell proliferation while maintaining the ability to differentiate into tissue cells in the progeny)[1][2]. Dec 20 2024
E8026 Licorice glycoside C2 Licorice glycoside C2 is a oleanane-type triterpene oligoglycoside isolated from Glycyrrhiza uralensis. Various biological activities are associated with licorice extracts, such as anti-viral, anti-microbial, antioxidant, anti-inflammatory, anti-ulcer, anti-cancer and anti-HIV effects[1]. Dec 20 2024
E7516 Acetoacetic acid sodium Acetoacetic acid sodium is a metabolite of non-esterified fatty acids, involved in the development of human diabetes. Acetoacetic acid sodium induces oxidative stress to inhibit the assembly of very low density lipoprotein in bovine hepatocytes[1]. Dec 20 2024
E7772 Ulixertinib hydrochloride Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line[1][2]. Dec 20 2024
E8027 Pyr6 Pyr6 is a selective inhibitor of TRPC3 with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).IC50 value: 0.49 uM [1]Target: TRPC3 inhibitorPyr6 is a selective SOCE inhibitor (Yonetoku et al., 2008; Sweeney et al., 2009), Pyr6 displayed 37-fold (1.58 OM) higher potency for RBL SOCE than for TRPC3 ROCE, with an IC50 comparable to that of Pyr2 and Pyr3. Pyr6 at 3 uM diminished TRPC3 currents to only 52%. Consistent with inhibition of Orai channel activity Pyr2, Pyr3 or Pyr6 substantially inhibited typical Orai downstream signalling events in RBL mast cells (NFAT activation and degranulation) activated by passive store depletion. Dec 20 2024
E5001 SMILAGENIN Dec 20 2024
E7517 R-1479 R-1479 (4'-Azidocytidine), a nucleoside analogue, is a specific inhibitor of RNA-dependent RNA polymerase (RdRp) of HCV. R-1479 inhibits HCV replication in the HCV subgenomic replicon system (IC50=1.28 μM)[1][2][3]. R-1479 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. Dec 20 2024
E7773 R 59-022 R 59-022 (DKGI-I) is a DGK inhibitor (IC50: 2.8 µM). R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils[1][2][3][4]. Dec 20 2024
E8028 FGH10019 FGH10019 is a novel sterol regulatory element-binding protein (SREBP) inhibitor with IC50 of 1 μM. Dec 20 2024
E7518 Balapiravir Balapiravir (Ro 4588161; R1626) is an orally active proagent of a nucleoside analogue inhibitor of the RNA-dependent RNA polymerase (RdRp) of HCV (R1479; 4'-Azidocytidine). Balapiravir has anti-HCV activity[1][2][3]. Balapiravir is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. Dec 20 2024
E7774 L-Alanosine L-Alanosine (NSC-153353), an antibiotic from Streptomyces alanosinicus, has antineoplastic activity. L-Alanosine (NSC-153353) inhibits adenylosuccinate synthetase, which converts inosine monophospate (IMP) into adenylosuccinate. L-Alanosine (NSC-153353) blocks the common de novo purine biosynthesis pathway and, thereby, inhibits tumor cells with MTAP deficiency[1][2][3]. Dec 20 2024
E8029 Z-VDVAD-FMK Z-VDVAD-FMK is a special inhibitor of caspase-2. Z-VDVAD-FMK produces a reduction in Lovastatin-induced apoptosis[1][2][3]. Dec 20 2024
E7519 UK 356618 UK 356618 (Compound 4j) is a potent and selective inhibitor of matrix metalloprotease-3 (MMP-3) with an IC50 of 5.9 nM. UK 356618 is less potent against MMP-1, MMP-2, MMP-9, MMP-13 and MMP-14 compared with MMP-3[1]. Dec 20 2024
E7775 Dodecanoylcarnitine Dodecanoylcarnitine is present in fatty acid oxidation disorders such as long-chain acyl CoA dehydrogenase deficiency, carnitine palmitoyltransferase I/II deficiency, and is also associated with celiac disease. Dec 20 2024
E8030 Chlorphenoxamine Chlorphenoxamine is an antihistamine and anticholinergic used as an antipruritic and antiparkinsonian agent. Target: Histamine Receptor Dec 20 2024
E7520 CCT251236 CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC50 of 19 nM for inhibition of HSF1-mediated HSP72 induction. Dec 20 2024
E7776 JNJ-17203212 JNJ-17203212 is a selective, potent and competitive TRPV1 antagonist. JNJ-17203212 is developed for researching pain management, such as migraine[1][2]. Dec 20 2024
E8031 Alkynyl Palmitic Acid Alkynyl Palmitic Acid (Alk-C16) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Alkynyl Palmitic Acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 20 2024
E7521 MDL-29951 MDL-29951 is a novel glycine antagonist of NMDA receptor activation, with Ki of 0.14 μM for [3H]glycine binding in vitro and in vivo. Dec 20 2024
E7777 Dimemorfan phosphate Dimemorfan phosphate is a sigma 1 receptor agonist, used as a potent antitussive. Dec 20 2024
E8032 EPQpYEEIPIYL EPQpYEEIPIYL, a phosphopeptide, is a Src homology 2 (SH2) domain ligand. EPQpYEEIPIYL activates Src family members (e.g. Lck, Hck, Fyn) by binding to SH2 domains[1][2]. Dec 20 2024
E7522 Palosuran Palosuran (ACT-058362) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC50 of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran can improves pancreatic and renal function in diabetic rats[1][2]. Dec 20 2024
E7778 GW274150 GW274150 is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM). GW274150 also displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 exerts a protective role in an acute model of lung injury inflammation[1][2]. Dec 20 2024
E8033 DO-264 DO-264 is a selective and in vivo-active inhibitor of Abhydrolase Domain Containing 12 (ABHD12), with an IC50 of 11 nM. Dec 20 2024
S9565 Vigabatrin Vigabatrin (γ-Vinyl-GABA), an inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase[1][2][3]. Dec 20 2024
E7523 Naspm Naspm (1-Naphthyl acetyl spermine), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist. Dec 20 2024
E7779 1400W 1400W is a slow, tight binding, and highly selective inducible nitric-oxide synthase (iNOS) inhibitor, with a Kd value ≤ 7 nM. 1400W inhibits iNOS induction in microglial cells, and reduces generation of NO, thereby mitigating oxidative stress and neuronal cell apoptosis in the rat cerebral cortex, and improving the spatial memory dysfunction caused by acute hypobaric hypoxia-reoxygenation[1][2]. Dec 20 2024
E8034 1-Stearoyl-2-arachidonoyl-sn-glycerol 1-Stearoyl-2-arachidonoyl-sn-glycerol is a diacylglycerol (DAG) containing polyunsaturated fatty acids. 1-Stearoyl-2-arachidonoyl-sn-glycerol can activate PKC. 1-Stearoyl-2-arachidonoyl-sn-glycerol also can augment nonselective cation channel (NSCC) activity[1][2]. Dec 20 2024
E5034 (3S)-3β-Butyl-1,3,4,5-tetrahydroisobenzofuran-1-one Dec 20 2024
E7524 G-418 G-418 (Geneticin) is an aminoglycoside antibiotic with a structure similar to gentamicin. It is toxic to both eukaryotic and prokaryotic cells and works by interfering with protein synthesis[1]. Dec 20 2024
E7780 Lck Inhibitor Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis[1]. Dec 20 2024
E8035 NSC 146109 hydrochloride NSC 146109 hydrochloride is a small-molecule p53 activator that target MDMX and can be used for breast cancer research. NSC 146109 hydrochloride is a pseudourea derivative, promotes breast cancer cells to undergo apoptosis through activating p53 and inducing expression of proapoptotic genes[1]. Dec 20 2024
E7525 MI-538 MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM. Dec 20 2024
E7781 ML224 ML224 (NCGC00242364) is a selective TSHR antagonist with an IC50 value of 2.1 µM. ML224 can be used in the study of Graves' disease and other thyroid disorders. Dec 20 2024
E8036 AM404 AM404, an inhibitor of endocannabinoid reuptake, blocks anandamide transport with IC50 values in the low micromolar range[1]. AM404 is able to relax rat isolated hepatic arteries contracted with Phenylephrine, with a pEC50 value of 7.4 (corresponding to an EC50 of 0.04 µM). Neuroprotective Effect[2]. Dec 20 2024
E7526 AVN-944 AVN-944 (VX-944) is an orally active, potent, selective, noncompetitive and specific inhibitor of IMPDH (inosine monophosphate dehydrogenase). AVN-944 is an essential rate-limiting enzyme in de novo guanine nucleotide synthesis. AVN-944 is also an inhibitor of arenavirus RNA synthesis, and blocks arenavirus infection. AVN-944 has broad anti-cancer activities, and can be used for multiple myeloma (MM) and acute myeloid leukemia (AML) research[1][2][3]. Dec 20 2024
E7782 HIV-1 integrase inhibitor HIV-1 integrase inhibitor is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. Dec 20 2024
E8037 TCH-165 TCH-165 is a small molecule modulator of proteasome assembly, which increases 20S levels and facilitates 20S-mediated protein degradation[1]. Dec 20 2024
E7527 ATN-224 ATN-224 is an oral Cu2+/Zn2+-superoxide dismutase 1 (SOD1) inhibitor. ATN-224 inhibits SOD1 activity in endothelial cells, an effect that is dose dependent with an IC50 of 17.5±3.7 nM. Dec 20 2024
E7783 NBD-557 NBD-557 is a potentially HIV-1 inhibitor.IC50 Value: Target: HIVNBD-557, is small molecule organic compounds with drug-like properties. It showed potent cell fusion and virus-cell fusion inhibitory activity at low micromolar levels. A systematic study showed that NBD-557 target viral entry by inhibiting the binding of HIV-1 envelope glycoprotein gp120 to the cellular receptor CD4 but did not inhibit reverse transcriptase, integrase, or protease, indicating that they do not target the later stages of the HIV-1 life cycle to inhibit HIV-1 infection. NBD-557 potent inhibitors of both X4 and R5 viruses tested in CXCR4 and CCR5 expressing cell lines, respectively, indicating that its anti-HIV-1 activity is not dependent on the coreceptor tropism Dec 20 2024
E8038 Nourseothricin sulfate Nourseothricin sulfate (Streptothricin sulfate) is a broad-spectrum antibiotic that destroys the outer membrane of Gram-negative bacteria and is a dominant selective marker for Fonsecaea pedrosoi[1][2]. Nourseothricin sulfate inhibits protein biosynthesis in prokaryotic cells and strongly inhibits the growth of eukaryotes like fungi and can also be used as a elective marker for a wide range of organisms including bacteria, yeast, filamentous fungi, and plant cells[3]. Dec 20 2024
E7528 2',5'-Dideoxyadenosine 2',5'-Dideoxyadenosine is a potent and non-competitive adenylyl cyclase inhibitor via binding the P-site with an IC50 of 3 µM . 2',5'-Dideoxyadenosine is a nucleoside analog and exerts a potent antiadrenergic action in heart[1][2]. Dec 20 2024
E7784 N,N-Dimethylsphingosine N,N-Dimethylsphingosine is a potent inhbitor of SphK (sphingosine kinase) as an endogenous metabolite of sphingosine produced in various tissues and tumor cell lines[1]. Dec 20 2024
E8039 Roluperidone Roluperidone (CYR-101) is a novel cyclic amide derivative that has high equipotent affinities for 5-HT2A and sigma-2 receptors (Ki of 7.53 nM and 8.19 nM for 5-HT2A and sigma-2, respectively). Dec 20 2024
E7529 Mibefradil Mibefradil (Ro 40-5967) is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels displaying IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively[1]. Dec 20 2024
E7785 D-erythro-MAPP D-erythro-MAPP (D-e-MAPP) is a ceramidase inhibitor, with an IC50 of 1-5 μM in vitro[1]. Dec 20 2024
E8040 Lipoxin A4 Lipoxin A4 (LXA4), an endogenous lipoxygenase-derived eicosanoid mediator, has potent dual pro-resolving and anti-inflammatory properties[1]. Lipoxin A4 inhibits proliferation and inflammatory cytokine/chemokine production of human epidermal keratinocytes (NHEKs) associated with the ERK1/2 and NF-kB pathways[2]. Lipoxin A4 inhibits serum amyloid A (SAA)-mediated IL-8 release with an IC50 value of 25.74 nM[3]. Dec 20 2024
E7530 BQ-788 sodium salt BQ-788 sodium salt is a potent and selective ETB receptor antagonist, inhibiting ET-1 binding to ETB receptors with an IC50 of 1.2 nM in human Girrardi heart cells[1]. Dec 20 2024
E7786 ATPγS tetralithium salt ATPγS (tetralithium salt) is a substrate for the nucleotide hydrolysis and RNA unwinding activities of eukaryotic translation initiation factor eIF4A[1]. Dec 20 2024
E8041 TD52 TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity[1]. TD52 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 20 2024
E7531 Necrostatin 2 Necrostatin 2 is a potent necroptosis inhibitor. EC50 for inhibition of necroptosis in FADD-deficient Jurkat T cells treated with TNF-α is 0.05 μM. Necrostatin 2 is also a RIPK1 inhibitor. Dec 20 2024
E7787 Dihydrofluorescein diacetate Dihydrofluorescein diacetate is a fluorimetric probe mainly used for oxidative stress measurements, in both cell-free systems and cellular models. Dec 20 2024
E8042 MC 1046 MC 1046(Impurity A of Calcipotriol) is an impurity of Calcipotriol; Calcipotriol (MC 903; Calcipotriene) is a ligand of VDR-like receptors. IC50 value:Target: Vitamin D3 analog that displays minimal effects on calcium homeostasis. Regulates cell differentiation and proliferation; Calcipotriol (MC 903; Calcipotriene) exhibits antiproliferative activity against human HL-60, HL60/MX2, MCF-7, T47D, SCC-25 and mouse WEHI-3 cancer cell lines. Dec 20 2024
E5670 Silybin Dec 20 2024
E7532 Eravacycline dihydrochloride Eravacycline dihydrochloride (TP-434 dihydrochloride) is a potent and broad-spectrum antibacterial agent. Dec 20 2024
E7788 Otenzepad Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively[1]. Dec 20 2024
E8043 Nicotinamide-d4 Nicotinamide-d4 is the deuterium labeled Nicotinamide. Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1. Dec 20 2024
E7533 Iclaprim Iclaprim is a new selective bacterial Dihydrofolate inhibitor, which can inhibit the growth of S. aureus (MRSA) with an MIC90 of 0.06 μg/mL. Dec 20 2024
E7789 A 839977 A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta[1]. Dec 20 2024
E8044 Caerulomycin A Caerulomycin A (Cerulomycin; Caerulomycin), an antifungal compound, induces generation of T cells, enhances TGF-β-Smad3 protein signaling via suppressing interferon-γ-induced STAT1 signaling. Antifungal and antibiotic activity, and used in autoimmune diseases[1]. Dec 20 2024
E7534 Delavirdine Delavirdine (U 90152) is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine is an inhibitor of HIV-1 replication and can can be used for the study of AIDs[1]. Dec 20 2024
E7790 BIO-1211 BIO-1211 is a highly selective and orally active α4β1 (VLA-4) inhibitor, with IC50 values of 4 nM and 2 μM for α4β1 and α4β7, respectively[1][2][3]. Dec 20 2024
E8045 (R)-Ketorolac (R)-Ketorolac is the R-enantiomer of Ketorolac, shows potent analgesic activity, reduces ulcerogenic potential. (R)-Ketorolac is inactive on COX[1]. Dec 20 2024
E7535 MK-3207 MK-3207 is an orally active, highly selective and species-specific CGRP receptor antagonist (for human CGRP receptor: IC50=0.12 nM; Ki=0.024 nM). MK-3207 can be used for migraine studies[1]. Dec 20 2024
E7791 (R)-(-)-Gossypol (R)-(-)-Gossypol (AT-101) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively. Dec 20 2024
E8046 Cycloartenyl ferulate Cycloartenyl ferulate (Cycloartenol ferulate) is one of the typical triterpene alcohols and possesses several biological activities including anti-oxidative activity, antiallergic activity, anti-inflammatory and anticancer activities[1]. Dec 20 2024
E7536 Mps1-IN-1 Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM[1]. Dec 20 2024
E7792 MDL 72527 MDL 72527 is a potent polyamine oxidase (PAO) inhibitor. MDL 72527 shows a lysosomotropic effect. MDL 72527 shows neuroprotective effects[1][2]. Dec 20 2024
E8047 Methyl Green Methyl Green is a potent fluorescent dye. Methyl Green is a DNA stains of cells and electrophoretic gels. Methyl Green can be used as a stain for direct measuring of viability by both microscopy and flow cytometry, with peaks at 633 and 677 nm[1][2]. Dec 20 2024
E7537 MPEP Hydrochloride MPEP Hydrochloride is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP Hydrochloride has anxiolytic-or antidepressant-like effects[1][2]. MPEP (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 20 2024
E7793 PRT062607 PRT062607(P505-15; PRT-2607; BIIB-057) is a highly specific and potent inhibitor of Syk with IC50 of 1-2 nM; >80-fold selective for Syk than Fgr, Lyn, FAK, Pyk2 and Zap70.IC50 value: 1-2 nM [1]Target:Syk kinase inhibitorin vitro: In human whole blood, P505-15 potently inhibited B cell antigen receptor-mediated B cell signaling and activation (IC50 0.27 and 0.28 μM, respectively) and Fcε receptor 1-mediated basophil degranulation (IC50 0.15 μM) [1]. P505-15 successfully inhibited SYK-mediated B-cell receptor signaling and decreased cell viability in NHL and CLL [2]. PRT318 and P505-15 effectively antagonize CLL cell survival after BCR triggering and in nurse-like cell-co-cultures. Moreover, they inhibit BCR-dependent secretion of the chemoki Dec 20 2024
E8048 2-Furoyl-LIGRLO-amide 2-Furoyl-LIGRLO-amide is a potent and selective proteinase-activated receptor 2 (PAR2) agonist with a pD2 value of 7.0[1][2].. Dec 20 2024
E7538 CU-CPT17e CU-CPT17e is a potent multi-Toll-like receptor (TLR) agonist that activates TLR3, TLR8, and TLR9. Dec 20 2024
E7794 Caerulein, desulfated Caerulein, desulfated is the desulfurated form of Caerulein. Caerulein is a decapeptide having the same five carboxyl-terminal amino acids as gastrin and cholecystokinin (CCK)[1]. Dec 20 2024
E8049 Topilutamide Topilutamide is a topical nonsteroidal antiandrogen (NSAA). Dec 20 2024
E7539 Domatinostat tosylate Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Dec 20 2024
E7795 Liquidambaric lactone Liquidambaric lactone is a compound isolated from Euonymus grandiflorus Wall[1]. Dec 20 2024
E8050 JJKK 048 JJKK 048 is an ultrapotent and highly selective inhibitor of Monoacylglycerol lipase (MAGL). Dec 20 2024
E7540 TG 100572 Hydrochloride TG 100572 Hydrochloride is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively. Dec 20 2024
E7796 JNJ-10397049 JNJ-10397049 is a potent and selective orexin 2 receptor (OX2R) antagonist, with a pKi of 8.3. JNJ-10397049 is 600-fold selective for the OX2R over the OX1R[1][2]. Dec 20 2024
E8051 Ximelagatran Ximelagatran (H 376/95) is an orally active thrombin inhibitor that selectively and competitively inhibits both free and clot-bound thrombin. Ximelagatran is an anticoagulant agent with a rapid onset of anticoagulant effect, predictable, dose-dependent pharmcokinetics and pharmacodynamics[1][2]. Dec 20 2024
E7541 TG 100801 TG 100801 is a proagent that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively. Dec 20 2024
E7797 Mitoguazone Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment[1][2][3][4]. Dec 20 2024
E8052 CPA inhibitor CPA inhibitor (Carboxypeptidase inhibitor; compound 5) is a potent carboxypeptidase A (CPA) inhibitor with a Ki of 0.32 μM[1]. Dec 20 2024
E7542 EOC317 EOC317 (ACTB-1003) is an oral kinase inhibitor with IC50s of 6, 2 and 4 nM for FGFR1, VEGFR2 and Tie-2. Dec 20 2024
E7798 Cot inhibitor-1 Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC50 of 5.7 nM[1]. Dec 20 2024
E8053 CP-547632 CP-547632 is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy[1]. Dec 20 2024
E7543 Zaurategrast Zaurategrast (CT7758) is a potent and oral-effective α4-integrin inhibitor[1]. Dec 20 2024
E7799 CU-CPT9b CU-CPT9b is a specific TLR8 antagonist, with an IC50 of 0.7 nM. CU-CPT9b shows high binding affinity towards TLR8 with a Kd of 21 nM[1]. Dec 20 2024
E8054 Benzyl-α-GalNAc Benzyl-α-GalNAc is a potent O-glycosylation inhibitor. Benzyl-α-GalNAc effectively inhibits the proliferation and activation of LX-2 cells and suppresses the expression of collagen I/III, which has good potential for investigation in liver fibrosis. Benzyl-α-GalNAc also significantly enhances the anti-tumour activity of 5-FU (HY-90006) (e.g. pancreatic cancer) by inhibiting O-glycosylation[1][2][3]. Dec 20 2024
E5723 Anemarrhenasaponin I Dec 20 2024
E7544 1G244 1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects[1][2]. Dec 20 2024
E7800 Gentianine Gentianine, an active metabolite of Swertiamarin, has anti-diabetic effect and anti-inflammatory property[1][2]. Dec 20 2024
E8055 Hematoporphyrin monomethyl ether Hematoporphyrin monomethyl ether, second generation of porphyrin-related photosensitizer, is characterized by its single form, high yield of singlet oxygen, high selectivity, and low toxicity, which has been widely used in the diagnosis and research of various tumors, including lung cancer, bladder cancer, and nevus flammeus and brain glioma[1]. Dec 20 2024
E7545 PSI-7409 PSI-7409 is the active 5'-triphosphate metabolite of Sofosbuvir (PSI-7977). Sofosbuvir (PSI-7977) is a selective and highly active nucleotide analog inhibitor of HCV. Dec 20 2024
E7801 (S)-Propafenone (S)-Propafenone ((S)-SA-79) is the S-enantiomer of Propafenone. (S)-Propafenone ((S)-SA-79) exerts beta-blocking action and the sodium channel-dependent antiarrhythmic class 1 activity[1]. Dec 20 2024
E8056 Saponarin Saponarin is a natural flavonoid isolated from Gypsophila trichotoma, with antioxidant, anti-inflammatory and hepatoprotective activities. Saponarin activates AMPK in a calcium-dependent manner, thus regulating gluconeogenesis and glucose uptake[1][2][3]. Dec 20 2024
E7546 PZM21 PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM[1][2][3]. Dec 20 2024
E7802 GR 113808 GR 113808 is a potent and highly selective 5-HT4 receptor antagonist (pKb= 8.8). GR 113808 shows 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors[1]. Dec 20 2024
E8057 Meloside A Meloside A (Isovitexin 2''-O-glucoside) is a phenylpropanoid isolated from barley with antioxidant activity. In barley, phenylpropanoids have been described as having protective properties against excess UV-B radiation and have been linked to resistance to pathogens[1][2]. Dec 20 2024
E7547 LY2955303 LY2955303 is a potent and selective retinoic acid receptor gamma (RARγ) antagonist with a Ki of 1.09 nM. Dec 20 2024
E7803 Rescinnamine Rescinnamine is a derivative of the indole alkaloid reserpine. Rescinnamine shows sedative effects. Rescinnamine can be used for hypertension research[1][2]. Dec 20 2024
E8058 TC-S 7005 TC-S 7005 is a Polo-like kinases (Plks) inhibitor with IC50s of 4 nM, 24 nM and 214 nM for Plk2, Plk3, and Plk1, respectively[1]. Dec 20 2024
E7548 Ch55 Ch55 is a potent synthetic retinoid. Ch55 binds to RAR-α and RAR-β receptors with high affinity. Ch55 displays low affinity for cellular retinoic acid binding protein (CRABP). Ch55 is a potent inducer of the differentiation of HL60 cells with an EC50 of 200 nM. Ch55 can be used for cancer research[1][2]. Dec 20 2024
E7804 2,3-Dehydro-2-deoxy-N-acetylneuraminic acid N-acetyl-2,3-dehydro-2-Deoxyneuraminic Acid (Neu5Ac2en) is a potent neuraminidase (sialidase) inhibitor. N-acetyl-2,3-dehydro-2-Deoxyneuraminic Acid shows inhibitory activities against human neuraminidase enzymes with IC50s of 143, 43, 61, and 74 μM for NEU1, NEU2, NEU3, and NEU4, respectively. Anti-influenza virus activity[1][2]. Dec 20 2024
E8059 VH032-cyclopropane-F VH032-cyclopropane-F is the VH032-based VHL ligand. VH032-cyclopropane-F can be connected to the ligand for protein (e.g., SMARCA BD ligand) by a linker to form PROTACs (e.g., PROTAC 1). PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4[1]. Dec 20 2024
E7549 Halofantrine hydrochloride Halofantrine hydrochloride (SKF-102886) is a blocker of delayed rectifier potassium current via the inhibition of human-ether-a-go-go-related gene (HERG) channel and a potent antimalarial compound[1][2]. Dec 20 2024
E7805 cis-Epoxysuccinic acid cis-Epoxysuccinic acid is a succinate receptor (SUCNR1/GPR91) agonist. cis-Epoxysuccinic acid inhibits cAMP levels with an EC50 value of 2.7 µM. cis-Epoxysuccinic acid can be used for the research of cardiovascular system[1]. Dec 20 2024
E8060 N-Acetylprocainamide N-Acetylprocainamide is a class III antiarrhythmic, which blocks K+ channels. Dec 20 2024
E7550 Filanesib Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity[1]. Dec 20 2024
E7806 Thyrotropin-Releasing Hormone (TRH), Free Acid Thyrotropin-Releasing Hormone (TRH), Free Acid (TRH-OH) is a physiological metabolite of Thyrotropin-Releasing Hormone. Dec 20 2024
E8061 5'-Deoxyadenosine 5'-Deoxyadenosine is an oxidized nucleoside found in the urine of normal subjects. 5'-Deoxyadenosine shows anti-orthopoxvirus activity[1]. Dec 20 2024
E7551 MK-5046 MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC50 and an EC50 value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity[1][2][3]. Dec 20 2024
E7807 BETP BETP is an agonist of glucagon-like peptide-1 (GLP-1) receptor, with EC50s of 0.66 and 0.755 μM for human and rat GLP-1 receptor, respectively. Dec 20 2024
E8062 D-64131 D-64131 is an orally active tubulin inhibitor, with an IC50 of 0.53 μM for tubulin polymerization. D-64131 has antimitotic activity. D-64131 can be used for cancer research[1][2]. Dec 20 2024
E7552 Reparixin L-lysine salt Reparixin L-lysine salt is an allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation. Dec 20 2024
E7808 PSB-603 PSB-603 is a potent and highly selective A2B adenosine receptor antagonist exhibiting a Ki value of 0.553 nM and virtually no affinity for the human and rat A1 and A2A and the human A3 receptors up to a concentration of 10 μM[1]. Dec 20 2024
E8063 Acumapimod Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC50 of less than 1 μM for p38α. Dec 20 2024
E5773 Gypenoside L Gypenoside L, is a saponin from Gynostemma pentaphyllum, increases SA-β-galactosidase activity, enhances senescence-associated cytokine production, inhibits proliferation and LPS-induced nitric oxide (NO) production, induces S-phase arrest, and activates p21, p27, p38, ERK MAPK, and NF-κB pathways to promote senescence. Dec 20 2024
E7553 DMP 777 DMP 777 is a potent, selective, and orally active human leukocyte elastase (HLE) inhibitor. Dec 20 2024
E7809 Acridine Orange base Acridine Orange base is a cell-permeable fluorescent dye that stains organisms (bacteria, parasites, viruses, etc.) bright orange and, when used under appropriate conditions (pH=3.5, Ex=460 nm), distinguishes human cells in green for detection by fluorescence microscopy. Acridine Orange base fluoresces green when bound to dsDNA (Ex=488, Em=520-524) and red when bound to ssDNA (Ex=457, Em=630-644) or ssRNA (Ex=457, Em=630-644), also can be used in cell cycle assays[1][2][3]. Dec 20 2024
E8064 Pseudomonas quinolone signal Pseudomonas Quinolone Signal (Compound C), a signaling molecule produced by Pseudomonas aeruginosa, can activate lasB. Pseudomonas Quinolone Signal can be used in the study of virulence regulation in Pseudomonas aeruginosa[1]. Dec 20 2024
E7554 Bay 65-1942 hydrochloride Bay 65-1942 hydrochloride is an ATP-competitive and selective IKKβ inhibitor. Dec 20 2024
E7810 Eicosadienoic acid Eicosadienoic acid is a rare, naturally occurring n-6 polyunsaturated fatty acid found mainly in animal tissues[1][2]. Dec 20 2024
E8065 FGFR4-IN-1 FGFR4-IN-1 is a potent inhibiotr of FGFR4 with IC50 of 0.7 nM. Dec 20 2024
E7555 Acridine Orange 10-Nonyl Bromide Acridine Orange 10-Nonyl Bromide is a fluorescent probe for cardiolipin (λex: 489 nm, λem: 525 nm). Dec 20 2024
E7811 Quercetin 3-O-sambubioside Quercetin-3-O-sambubioside is a monomeric compound found in Eucommia ulmoides male flowers. Quercetin-3-O-sambubioside promotes the stimulation of the nerve center. Antioxidant and anticancer activities[1][2]. Dec 20 2024
E8066 Kongensin A Kongensin A is a natural product isolated from Croton kongensis. Kongensin A is an effective, covalent HSP90 inhibitor that blocks RIP3-dependent necroptosishas. Kongensin A is a potent necroptosis inhibitor and an apoptosis inducer. Kongensin A has potential anti-necroptosis and anti-inflammation applications[1]. Dec 20 2024
E7556 Ceftobiprole Ceftobiprole (Ro 63-9141) is a broad-spectrum cephalosporin with high levels of in vitro activity against methicillin- (MRSA) and vancomycin-resistant staphylococci (VRSA) and penicillin-resistant streptococci with a MIC90 value of 2 μg/mL for MRSA. Ceftobiprole also inhibits gram-positive and gram-negative pathogens[1][2][3]. Dec 20 2024
E7812 Pyronaridine tetraphosphate Pyronaridine tetraphosphate is an orally active Mannich base anti-malarial agent. Pyronaridine tetraphosphate is active against P. falciparum and Echinococcus granulosus infection[1][2]. Dec 20 2024
E8067 5(6)-Carboxy-2',7'-dichlorofluorescein 5(6)-Carboxy-2',7'-dichlorofluorescein is an ideal substrate for MRP2 vesicular transport assay, with excellent detection and transport properties[1]. Dec 20 2024
E7557 Bromobimane Bromobimane (Monobromobimane) is a nonfluorescent and converts into fluorescent products when reacts with thiols. Bromobimane has potential applications in labeling thiols[1][2]. Dec 20 2024
E7813 Naspm trihydrochloride Naspm trihydrochloride (1-Naphthylacetyl spermine trihydrochloride), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist. Dec 20 2024
E8068 Abemaciclib metabolite M2 Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s of 1.2 and 1.3 nM, respectively. Anti-cancer activity[1][2]. Dec 20 2024
E7558 Ac4ManNAz (80% α isomer) Ac4ManNAz is an azido-containing metabolic glycoprotein labeling reagent. Ac4ManNAz can be used to selectively modify proteins. Ac4ManNAz can be used in cell labeling, tracking and proteomic analysis[1][2]. Ac4ManNAz is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. Dec 20 2024
E7814 Pictilisib dimethanesulfonate Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Dec 20 2024
E8069 GDP366 GDP366, a dual inhibitor of survivin and Op18, induces cell growth inhibition, cellular senescence and mitotic catastrophe in human cancer cells. Dec 20 2024
E7559 RS 09 RS09 is a LPS peptide mimic serves as a candidate to be considered as a new class of TLR4 agonist adjuvant. RS09 increases antibody production in a vaccine setting[1]. Dec 20 2024
E7815 LX-1031 LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally. Dec 20 2024
E8070 Coclaurine Coclaurine is a class of tetrahydroisoquinoline alkaloids that can be isolated from Sarcopetalum harveyanum. Coclaurine is a nicotinic acetylcholine receptor (nAChRs) antagonist[1][2]. Dec 20 2024
E7560 HC-070 HC-070 is an antagonist of TRPC4/TRPC5, with IC50s of 9.3 nM and 46 nM for hTRPC5 and hTRPC4 in cells, respectively. Dec 20 2024
E7816 MELK-8a hydrochloride MELK-8a hydrochloride is a novel maternal embryonic leucine zipper kinase (MELK) inhibitor with an IC50 of 2 nM. Dec 20 2024
E8071 Chromafenozide Chromafenozide (ANS118) is a lepidopteran insecticide; it is highly effective in controlling various lepidopteran pests. Dec 20 2024
E7561 Pradigastat Pradigastat (LCQ-908) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor with IC50 at 0.157 µM. Pradigastat is primarily used to study diseases associated with abnormal triglyceride metabolism. Pradigastat has anti-obesity and anti-diabetic effects. Pradigastat inhibited BCRP, OATP1B1, OATP1B3 and OAT3 activities with IC50 of 5 µM, 1.66µM, 3.34µM and 0.973µM, respectively. In addition, Pradigastat has antiviral activity and can inhibit hepatitis C virus replication in vitro[1][2][3][4]. Dec 20 2024
E7817 20(S)-Hydroxycholesterol 20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells[1][2]. Dec 20 2024
E8072 Sagittatoside A Sagittatoside A is a natural compound isolated from traditional Chinese herb Yinyanghuo (Herba Epimdii). Dec 20 2024
E7562 Ikarugamycin Ikarugamycin is an antibiotic and a inhibitor of clathrin-mediated endocytosis (CME)[1]. Dec 20 2024
E7818 INCA-6 INCA-6 (Triptycene-1,4-quinone) is a cell-permeable NFAT inhibitor. INCA-6 specifically blocks targeting of NFAT(P) substrate to the  calcineurin (CN) phosphatase site and is an effective inhibitor of CN-NFAT signaling[1][2][3]. Dec 20 2024
E8073 Sagittatoside B Sagittatoside B is a natural compound isolated from traditional Chinese herb Yinyanghuo (Herba Epimdii). Dec 20 2024
E7563 1-Methylguanosine 1-Methylguanosine is a methylated nucleoside originating from RNA degradation. 1-Methylguanosine is a tumour marker[1]. Dec 20 2024
E7819 TTA-A2 TTA-A2 is a potent, selective and orally active t-type voltage gated calcium channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy[1][2]. Dec 20 2024
E8074 Oxazine 1 perchlorate Oxazine 1 perchlorate is a symmetric cationic dye (λex=653 nm, λem=666 nm). Dec 20 2024
E7564 3-Methylcytidine 3-Methylcytidine, a urinary nucleoside, can be used as a biomarker of four different types of cancer: lung cancer, gastric cancer, colon cancer, and breast cancer[1]. Dec 20 2024
E7820 RAGE antagonist peptide RAGE antagonist peptide is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide (RAP) possesses anti-tumor and anti-inflammatory activities[1][2]. Dec 20 2024
E8075 Ucf-101 Ucf-101 is a selective and competitive inhibitor of pro-apoptotic protease Omi/HtrA2, with an IC50 of 9.5 μM for His-Omi. Ucf-101 exhibits very little activity against various other serine proteases (IC50>200 μM). Ucf-101 has a natural red fluorescence at 543 nm that is used to monitor its ability to enter mammalian cells. Ucf-101 has a significant cardioprotective effect against MI/R injury and also has certain neuroprotective effect[1][2][3]. Dec 20 2024
E7565 360A iodide 360A iodide is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay. Dec 20 2024
E7821 BODIPY 505/515 BODIPY505/515 is a BODIPY dye. BODIPY dye is a small molecule dye with strong ultraviolet absorption ability, its fluorescence peak is relatively sharp, and the quantum yield is high. They are relatively insensitive to the polarity and pH of the environment and are relatively stable under different physiological conditions. Due to its structural asymmetry, BODIPY derives a variety of structural products. BODIPY lipid droplet dyes can well pass through the cell membrane into the cell, and localize the neutral lipids in the cell to specifically stain the lipid droplets, which can be used for labeling of live cells and fixed cells[1]. Maximum excitation/emission wavelength: 505/515 nm[1]. Dec 20 2024
E8076 Phenylethanolamine A Phenylethanolamine A acts as a β-adrenergic agonist. Phenylethanolamine A is a byproduct during the Ractopamine synthesis process[1]. Dec 20 2024
E4608 4-Hydroperoxy cyclophosphamide 4-Hydroperoxy cyclophosphamide is the active metabolite form of the precursor Cyclophosphamide. 4-Hydroperoxy cyclophosphamide cross-links DNA to induce T cell apoptosis independent of caspase receptor activation, and can activate the mitochondrial death pathway by producing reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide can be used in the study of rheumatoid arthritis and autoimmune diseases[1][2]. Dec 19 2024
E7010 (±)-BI-D (±)-BI-D is a potent ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site. Dec 19 2024
E7214 Sabinene Sabinene is an naturally occurring bicyclic monoterpene which can be used as flavorings, perfume additives, fine chemicals, and advanced biofuels. Sabinene is also an orally active compound to attenuates skeletal muscle atrophy and regulates ROS-mediated MAPK/MuRF-1 pathways. Dec 19 2024
E7436 Galanin (1-30), human Galanin (1-30), human is a 30-amino acid neuropeptide, and acts as an agonist of GalR1 and GalR2 receptors, with Kis of both 1 nM. Dec 19 2024
E4998 Polyinosinic-polycytidylic acid sodium Polyinosinic-polycytidylic acid (Poly(I:C)) sodium is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis. Dec 19 2024
E7215 p-Tolualdehyde p-Tolualdehyde is an endogenous metabolite. Dec 19 2024
E7437 Phenol Red Phenol red (Phenolsulfonephthalein) is a pH indicator dye, relying on a distinct color change from pink to yellow in case of a positive reaction . Dec 19 2024
E7011 1,3-Diphenylisobenzofuran 1,3-Diphenylisobenzofuran (DPBF) has been developed as a selective probe for the detection and quantitative determination of hydrogen peroxide in samples containing different reactive nitrogen and oxygen species (RNOS). DPBF is a fluorescent probe which, for almost 20 years, was believed to react in a highly specific manner toward some reactive oxygen species such as singlet oxygen and hydroxy, alkyloxy or alkylperoxy radicals. Dec 19 2024
E7216 Isoquinoline Isoquinoline is an analog of pyridine. Isoquinoline structural-based alkaloids, such as tropoloisoquinoline, phthalideisoquinoline, and naphthylisoquinoline has anti-cancer activities. Dec 19 2024
E7438 Desmethylglycitein Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes. Dec 19 2024
E7012 Conduritol B epoxide Conduritol B epoxide is an irreversible covalently bound acid β-glucosidase (GCase) inhibitor. Dec 19 2024
E7217 7-Ethoxyresorufin 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase. Dec 19 2024
E7439 Medicarpin Medicarpin is a flavonoid isolated from Medicago sativa. Medicarpin induces apoptosis and overcome multidrug resistance in leukemia P388 cells by modulating P-gp-mediated efflux of agents. Dec 19 2024
E1311 Paxilline Paxilline is an indole alkaloid mycotoxin from Penicillium paxilli, acts as a potent BK channels inhibitor by an almost exclusively closed-channel block mechanism. Paxilline also inhibits the sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) with IC50s between 5 μM and 50 μM for differing isoforms. Paxilline possesses significant anticonvulsant activity. Dec 19 2024
E7218 4-Methylumbelliferyl β-D-galactopyranoside 4-Methylumbelliferyl β-D-galactopyranoside is a fluorescent substrate for β-galactosidase which, when cleaved, produces a water-soluble blue fluorescent coumarin fluorophore that can be detected using a fluoroenzymeter or fluorometer. Dec 19 2024
E7440 Alkaline phosphatase, Bovine intestine Alkaline phosphatase, Bovine intestine (Apase) is a membrane-bound glycoprotein that catalyzes the hydrolysis of phosphate monoesters at alkaline pH. Alkaline phosphatase can be used in molecular biology and enzyme-free analysis. Inhibition of tissue nonspecific alkaline phosphatase can block intracellular lipid accumulation. Dec 19 2024
E7013 MBX-2982 MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist. Dec 19 2024
E7219 Biotin-PEG3-azide Biotin-PEG3-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Biotin-PEG3-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. Dec 19 2024
E0224 Chicoric acid Chicoric acid (Cichoric acid), an orally active dicaffeyltartaric acid, induces reactive oxygen species (ROS) generation. Chicoric acid inhibits cell viability and induces mitochondria-dependent apoptosis in 3T3-L1 preadipocytes through ROS-mediated PI3K/Akt and MAPK signaling pathways. Chicoric acid increases glucose uptake, improves insulin resistance, and attenuates glucosamine-induced inflammation. Chicoric acid has antidiabetic properties and antioxidant, anti-inflammatory effects. Dec 19 2024
E7014 5-Carboxyfluorescein diacetate N-succinimidyl ester 5-Carboxyfluorescein diacetate N-succinimidyl ester is a cell permeable dye (Ex=492 nm, Em=517 nm). 5-Carboxyfluorescein diacetate N-succinimidyl ester can label cells by covalently binding to intracellular molecules. 5-Carboxyfluorescein diacetate N-succinimidyl ester is used to track lymphocyte migration and proliferation. Dec 19 2024
E7220 WWL70 WWL70 is a selective alpha/beta hydrolase domain 6 (ABHD6) inhibitor with an IC50 of 70 nM. Dec 19 2024
E7441 Pyranine Pyranine (HPTS; Solvent Green 7) is a pH-sensitive fluorescent indicator. Pyranine acts as a class of fluorescent chemosensor for the Cu+ ion(λex=450 nm, λem=510 nm). Dec 19 2024
E1755 SR144528 SR144528 is a potent and selective CB2 receptor antagonist with a Ki of 0.6 nM. Dec 19 2024
E7221 7-Aminoactinomycin D 7-Aminoactinomycin D (7-AAD) a fluorescent DNA stain, is a potent RNA polymerase inhibitor. 7-Aminoactinomycin D selectively binds to GC regions of the DNA. 7-Aminoactinomycin D also has antibacterial effects. Dec 19 2024
E7442 Pyrazosulfuron-ethyl Pyrazosulfuron-ethyl, one of the acetolactate synthase inhibiting herbicides in the sulphonylurea family, has been widely used to control weed growth in commercial cereal, soybean, and vegetable fields. Dec 19 2024
E2639 2′,7′-Dichlorofluorescein diacetate 2′,7′-Dichlorofluorescein diacetate (DCFH2-DA) is a cell-permeable fluorescent probe. 2′,7′-Dichlorofluorescein diacetate can be used to detect the generation of reactive oxygen intermediates and for assessing the overall oxidative stress in toxicological phenomenon. Dec 19 2024
E6012 Cetirizine Cetirizine is a second-generation, non-sedating selective antagonist of H1 histamine receptors. It has anti-inflammatory and anti-allergic properties and is used to treat perennial rhinitis and urticaria. Dec 19 2024
E7443 Cross-linked dextran G 25 Cross-linked dextran G 25 is a dextran chromatography medium. Cross-linked dextran G 25 separates from 1 to 5 kD (spherical proteins) and can be used for the separation of peptides as well as for the desalting and buffer replacement of large molecule proteins. Dec 19 2024
E7015 PF-543 PF-543 (Sphingosine Kinase 1 Inhibitor II) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy. Dec 19 2024
E7222 λ-Cyhalothrin λ-Cyhalothrin is a high efficiency, broad-spectrum type II synthetic pyrethroid insecticide containing α-cyano group. λ-Cyhalothrin is used to control a wide range of pests in a variety of applications. λ-Cyhalothrin is a neurotoxin that targets sodium channels in the membranes of neurons in the central nervous system. Dec 19 2024
E7444 (S)-MCPG (S)-MCPG ((+)-MCPG) is a potent group I/II metabotropic glutamate receptor (mGluRs) antagonist and the active isomer of (RS)-MCPG (HY-100371). (S)-MCPG can be used for the study of the function of mGluRs in spatial learning. Dec 19 2024
E7016 Ac-DEVD-AFC Ac-DEVD-AFC is a fluorogenic substrate (λex=400 nm, λem=530 nm). Dec 19 2024
E7223 Ac-YVAD-AFC Ac-YVAD-AFC is the the fluorometric peptide substrate of caspase-1, with λ excitation of 400 nm and λ emission of 505 nm. Dec 19 2024
E7445 Protein Kinase C (19-31) Protein Kinase C (19-31), a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31), is used as protein kinase C substrate peptide for testing the protein kinase C activity. Dec 19 2024
E2990 Radezolid Radezolid (RX-1741) is a oxazolidinone antibiotic. Radezolid is active against Staphylococcus, Chlamydia, and Legionella species, and remains active against Linezolid-resistant strains. Dec 19 2024
E7224 Human serum albumin Human serum albumin (HSA) is the most abundant protein in plasma and is a major determinant of plasma oncotic pressure. Human serum albumin exhibits antioxidant, anticoagulant, anti-inflammatory, anti-platelet aggregation activities as well as colloid osmotic action. Human serum albumin can block the inhibitory effect of GML on human T cells, providing protective function for T cells. Human serum albumin is also associated with cardiovascular diseases and can partially prevent the LPS (HY-D1056) induced oxidative stress, as well as the upregulation of NF-κB, NF-κB, and peroxynitrite (ONOO−) in the vascular wall, contributing to the reduction of blood pressure. Dec 19 2024
E7446 NKY80 NKY80 is a potent, selective and non-competitive adenylyl cyclase (AC) type V isoform inhibitor with IC50s of 8.3 µM, 132 µM and 1.7 mM for type V, III and II, respectively. NKY80 is a non-nucleoside quinazolinone and regulates the AC catalytic activity in heart and lung tissues. Dec 19 2024
E7017 Fluorescein Diacetate Fluorescein diacetate is a cell permeable esterase-substrate. Fluorescein diacetate can be used as a fluorogenic substrate for hGSTP1-1. Dec 19 2024
E7225 Vatalanib Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM. Dec 19 2024
E7447 EDANS EDANS (1,5-EDANS) (Standard) is an analytical standard for EDANS. This product is intended for research and analytical applications. EDANS (1,5-EDANS) is a novel quenched fluorogenic substrate for the analysis of retroviral proteases by resonance energy transfer. Dec 19 2024
E7018 DNase I, Bovine pancreas DNase I (EC 3.1.21.1) is an enzyme that degrade DNA, it plays a key role in the cleavage of extracellular DNA is crucial for limiting the inflammatory response and maintaining homeostasis. Exogenous deoxyribonuclease shows beneficial effects in inflammatory diseases and cancer. Dec 19 2024
E7226 Pirimiphos-methyl Pirimiphos-methyl is a rapid-acting organophosphorus insecticide and acaricide, causing inhibition of AChE in target organisms. Pirimiphos-methyl is often used for prevention and control of beetles, snout beetles, moths and Ephestia cautella during storage of agricultural grains. Dec 19 2024
E7448 [Pyr1]-Apelin-13 [Pyr1]-Apelin-13 is a highly potent, selective endogenous apelin receptor (APJ) agonist. Dec 19 2024
E7019 Teneligliptin Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM. Dec 19 2024
E7227 Myricetin 3-O-galactoside Myricetin 3-O-galactoside inhibits xanthine oxidase (XO) activity, lipid peroxidation and scavenges the free radical. Myricetin 3-O-galactoside inhibits lipid peroxidation with an IC50 of 160 μg/mL. Antioxidant activity. Dec 19 2024
E7449 Biotin Hydrazide Biotin Hydrazide is a carbonyl-reactive biotinylation reagent, which is a carbonyl probe. Dec 19 2024
E7020 Micafungin Micafungin (Mycamine; FK463) is an echinocandin antifungal drug which can inhibit 1,3-beta-D-glucan synthase. Dec 19 2024
E7228 Buparlisib Hydrochloride Buparlisib Hydrochloride (BKM120 Hydrochloride) is a pan-class I PI3K inhibitor, with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively. Dec 19 2024
E7450 DL-Tartaric acid DL-Tartaric acid is a non-racemic mixture of L- and D-tartaric acids with antioxidant activities. Dec 19 2024
E7021 Methicillin sodium salt Methicillin sodium salt (Meticillin sodium) is a β-lactam, semi-synthetic antibiotic related to penicillin antibiotic. Methicillin sodium salt inhibits penicillin-binding proteins involved in the synthesis of peptidoglycan. Methicillin sodium salt inhibits S. aureus with a MIC value of 2.1 μg/mL. Methicillin sodium salt can be used for the research of inflammation. Dec 19 2024
E7229 Pefloxacin Pefloxacin is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse) Target: DNA gyrase Pefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections. Dec 19 2024
E7451 Dehydroisoandrosterone 3-acetate Dehydroepiandrosterone 3-acetate is a testosterone/estrogen precursor and known modulator of vertebrate aggression. Dec 19 2024
E5192 Paraxanthine Paraxanthine, a caffeine metabolite, provides protection against Dopaminergic cell death via stimulation of Ryanodine Receptor Channels. Dec 19 2024
E7452 Endomorphin 1 Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties. Dec 19 2024
E7022 Danazol Danazol is a derivative of the synthetic steroid Ethisterone, which inhibits gonadotropin production and has a certain weak androgenic effect. Danazol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 19 2024
E7230 7β-Hydroxycholesterol 7β-Hydroxycholesterol is an oxysterol that derived by the oxidation of cholesterol. 7β-hydroxycholesterol is a powerful inducer of oxidative stress, inducing dysfunction of organelles (mitochondria, lysosomes and peroxisomes) that can cause cell death. Dec 19 2024
E7453 CTS-1027 CTS-1027 is a potent small molecule inhibitor of MMPs, with IC50s of 0.3 nM, 0.5 nM for MMP2, MMP13, respectively, and has > 1,000 fold selectivity over MMP1. Dec 19 2024
E7023 Phosphorylcholine chloride Phosphorylcholine chloride (Phosphocholine chloride) is an antigenic cell-surface component found on many commensal and pathogenic bacteria that reside in the upper airway. Dec 19 2024
E7231 Anthrone Anthrone is an organic compound commonly used as a dye and intermediate. It can be used to make products such as pigments, dyes and fluorescent whitening agents, and is widely used in certain industrial production fields such as textile manufacturing, soap making and paper making. In addition, this compound is also used as a reagent and catalyst in some organic synthesis reactions. Dec 19 2024
E7454 Thiazole Orange Thiazole Orange is an asymmetric anthocyanin dye that can be coupled with oligonucleotides (ONs) to prepare fluorescent hybridization probes. Thiazole Orange has been widely used in biomolecular detection and staining of DNA/ RNA in gels and can be used for reticulocyte analysis. Thiazole orange generates a significant fluorescence enhancement and high quantum yield when it binds with nucleic acids, especially RNA. Thiazole orange can permeate living cell membranes. Thiazole orange can use UV light for detection, but can also be detected with blue light. The excitation and emission of Thiazole orange are λex = 510 nm (488 nm and 470 nm also show strong excitation) and λem = 527 nm, respectively. Dec 19 2024
E6032 Levamisole Levamisole ((-)-Levamisole), an anthelmintic agent with immunomodulatory properties. Levamisole acts as a positive allosteric modulator (PAM) for the α3β2 (EC50=300 μM) and α3β4 (EC50=100 μM) subtype of nAChRs. Orally active. Dec 19 2024
E7232 1,2-DLPC 1,2-DLPC (1,2-Dilauroyl-sn-glycero-3-phosphocholine) is a ligand for LRH-1 agonists. 1,2-DLPC is a phospholipid used in the synthesis of liposomes. 1,2-DLPC enhances fat breakdown and apoptosis in fat cells through a TNFα-dependent pathway, while also inhibiting palmitate-induced insulin resistance through PPARα-mediated inflammation in muscle cells. Dec 19 2024
E7455 Ethyl docosa-4,7,10,13,16,19-hexaenoate Ethyl cis-4,7,10,13,16,19-Docosahexaenoate, the ethyl ester of Docosahexaenoate (DHA), is enriched in the ethyl ester fraction by the selective alcoholysis of fatty acid ethyl esters originating from tuna oil with lauryl alcohol. Dec 19 2024
E6030 Bazedoxifene Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer. Dec 19 2024
E7233 5(6)-FITC 5(6)-FITC (Fluorescein 5(6)-isothiocyanate) is an amine-reactive derivative of a fluorescent dye, characterized by high absorbance and excellent fluorescence quantum yield. The isothiocyanate group of FITC can react with various functional groups on proteins, including amines, thiols, imidazoles, tyrosines and carbonyls, enabling the labeling of proteins such as antibodies and lectins. 5(6)-FITC has a wide range of applications, including flow cytometry, immunofluorescence, protease assays and conjugation. The maximum excitation/emission wavelengths are 492/518 nm. Dec 19 2024
E7456 LH846 LH846 is a selective inhibitor of CKIδ, with an IC50 of 290 nM, and less potently inhibits CKIα and CKIε, with IC50s of 2.5 μM and 1.3 μM, respectively. Dec 19 2024
E7024 Amiodarone Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM. Dec 19 2024
E7234 Mirogabalin besylate Mirogabalin besylate is a selective and orally available ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively. Dec 19 2024
E7418 Noscapine Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier. Dec 19 2024
E7025 Talmapimod Talmapimod (SCIO-469) is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs. Dec 19 2024
E7235 Cucurbit[7]uril Cucurbit[7]uril is a cyclic organic molecule consisting of seven glycoluril units linked by methylene bridges. It has a rigid barrel-like structure with two identical inlets at both ends to selectively encapsulate guest molecules of appropriate size, shape, and polarity. Cucurbit[7]uril is known for its high binding affinity for a variety of organic and inorganic guests, including drugs, amino acids, peptides, and metal ions. This property makes them promising candidates for various applications in areas such as drug delivery, catalysis, and sensing. Dec 19 2024
P1249 Gastrin I, human Gastrin I, human is the endogenous peptide produced in the stomach, and increases gastric acid secretion via cholecystokinin 2 (CCK2) receptor. Dec 19 2024
E5525 Beta-Acetoxyisovalerylshikonin Beta-Acetoxyisovalerylshikonin is a naphthoquinone derivative isolated from Arnebia euchroma. Dec 19 2024
E5793 Oxidopamine hydrochloride Oxidopamine (6-OHDA) hydrochloride is an antagonist of the neurotransmitter dopamine. Oxidopamine hydrochloride is a widely used neurotoxin and selectively destroys dopaminergic neurons. Oxidopamine hydrochloride promotes COX-2 activation, leading to PGE2 synthesis and pro-inflammatory cytokine IL-1β secretion. Oxidopamine hydrochloride can be used for the research of Parkinson’s disease (PD), attention-deficit hyperactivity disorder (ADHD), and Lesch-Nyhan syndrome. Dec 19 2024
E7236 Agarose,Low melting point Agarose,Low melting point is a kind of agarose, a kind of polysaccharide that can be derived from seaweed. It is commonly used in molecular biology and biochemistry to isolate and purify DNA and RNA fragments. Agarose,Low melting point is a low melting point agarose, which is suitable for the recovery of large DNA fragments and enzymatic reactions in gels and other applications. In addition, it has been used in various techniques, such as pulsed field gel electrophoresis and capillary electrophoresis for analyzing genetic material. Dec 19 2024
E7026 OVA Peptide (323-339) OVA Peptide (323-339) represents a T and B cell epitope of Ovalbumin (Ova), which is important in the generation and development of immediate hypersensitivity responses in BALB/c mice. Dec 19 2024
E7237 DBCO-PEG4-NHS ester DBCO-PEG4-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. DBCO-PEG4-NHS ester is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups. Dec 19 2024
S8263 KT5720 KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2+ concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases. Dec 19 2024
E7238 1-Dodecylimidazole 1-Dodecylimidazole (N-Dodecylimidazole) is a lysosomotropic detergent and a cytotoxic agent. 1-Dodecylimidazole causes cell death by its acid-dependent accumulation in lysosomes, disruption of the lysosomal membrane, and releaseof cysteine proteases into the cytoplasm. 1-Dodecylimidazole has hypocholesterolaemic activity and broad-spectrum antifungal activity. Dec 19 2024
E6038 Pitavastatin Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects. Dec 19 2024
E7239 Cuprizone Cuprizone is a copper chelating agent that forms a deep blue copper ketone complex with copper (II). The copper ketone reaction can be used in colorimetric tests for the presence of trace copper. Cuprizone can be used to induce some schizophrenia-like behavior in mice. Cuprizone acts on copper enzymes, including SOD1, cytochrome oxidase, and DβH, thereby causing oxidative stress and increasing DA levels in certain brain regions such as the medial prefrontal cortex (PFC). Dec 19 2024
E1400 Kainic acid Kainic acid is a potent excitotoxic agent. Kainic acid hydrate also is an agonist for a subtype of ionotropic glutamate receptor. Kainic acid induces seizures. Dec 19 2024
E7240 7,4'-Dihydroxyflavone 7,4'-Dihydroxyflavone (7,4'-DHF) is a flavonoid, which can be isolated from Glycyrrhiza uralensis. 7,4'-Dihydroxyflavone is eotaxin/CCL11 inhibitor and CBR1 inhibitor (IC50=0.28 μM). 7,4'-Dihydroxyflavone has the ability to consistently suppress eotaxin production and prevent dexamethasone (Dex)‐paradoxical adverse effects on eotaxin production. 7,4'-Dihydroxyflavone (7,4'-DHF) inhibits MUC5AC gene expression, mucus production and secretion via regulation of NF-κB, STAT6 and HDAC2.7,4'-Dihydroxyflavone (7,4'-DHF) decreases phorbol 12-myristate 13-acetate (PMA) stimulated NCI-H292 human airway epithelial cell MUC5AC gene expression and mucus production with IC50 value of 1.4 µM. Dec 19 2024
E7027 Iptacopan Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G). Dec 19 2024
E7241 PHA-767491 PHA-767491 is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively. Dec 19 2024
E7028 Hematoporphyrin dihydrochloride Hematoporphyrin dihydrochloride (Hematoporphyrin IX dihydrochloride), a photosensitizer, is a substrate for affinity chromatography of heme-binding proteins. Hematoporphyrin dihydrochloride can induce apoptosis in U87 glioma cells and decrease tumor growth in vivo when exposed to red light. Dec 19 2024
E7242 Ralfinamide Ralfinamide (FCE-26742A) is an orally available Na+ blocker derived from α-aminoamide, with function of suppressing pain. Dec 19 2024
E7029 2-PMPA 2-PMPA is a potent and selective inhibitor of glutamate carboxypeptidase II (GCPII) with an IC50 of 300 pM. Dec 19 2024
E7243 N-Desethyl Sunitinib N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively. Dec 19 2024
E7030 5-Methyltetrahydrofolic acid 5-Methyltetrahydrofolic acid (5-Methyl THF) is the main circulating form of folic acid in the body and is involved in a variety of biochemical reactions. 5-Methyltetrahydrofolic acid regulates cardiovascular function by increasing the production of endothelin-1 (ET-1) in low-density lipoprotein-treated endothelial cells and can be used in the study of cardiovascular diseases. Dec 19 2024
E7244 Lathosterol Lathosterol is a cholesterol-like molecule. Serum Lathosterol concentration is an indicator of whole-body cholesterol synthesis. Dec 19 2024
E7031 Nafamostat Nafamostat, an anticoagulant, is a synthetic serine protease inhibitor. Nafamostat has anticancer and antivirus effect. Nafamostat induce apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1). Nafamostat can be used in the development of the pathological thickening of the arterial wall. Dec 19 2024
E7245 BRAF inhibitor BRAF inhibitor is a B-Raf inhibitor with anti-tumor activity extracted from patent WO/2011103196 A1, Compound P-0850. Dec 19 2024
E7032 Ac-DEVD-AMC Ac-DEVD-AMC is a fluorescent substrate of caspase-3/caspase-7. When treating Ac-DEVD-AMC with cell lysate, Ac-DEVD-AMC releases amino-4-methylcoumarin (AMC) for fluorescence detection, with an excitation wavelength of 380 nm and an emission wavelength of 460 nm. Dec 19 2024
E7246 SAMS SAMS peptide is a specific substrate for the AMP-activated protein kinase (AMPK). Dec 19 2024
E7033 Eptifibatide Eptifibatide is a cyclic heptapeptide, acts as a competitive antagonist for the activated platelet glycoprotein IIb/IIIa receptor, with anti-platelet activity. Dec 19 2024
E7247 IR-820 IR-820 (New Indocyanine Green) is an infrared blood pool contrast agent. IR-820 also is normally used as a laser and near-infrared dye to detect and quantify diseased tissue in live animals. Dec 19 2024
E7034 Indinavir Indinavir (MK-639 free base) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir is also a SARS-CoV 3CLpro inhibitor. Dec 19 2024
E7248 Glyoxalic acid Glyoxalic acid (NSC 27785) is an organic compound that is both an aldehyde and a carboxylic acid. Dec 19 2024
E7249 Ulinastatin Ulinastatin (Uristatin) is a trypsin and serine protease inhibitor. Ulinastatin is the main protein binding inhibitor of various trypsin, chymotrypsin, and various pancreatic proteases. Ulinastatin shows neuroprotective, anti-inflammatory, anti-apoptotic, anti-oxidant effects. Dec 19 2024
E7035 4,6-Dioxoheptanoic acid 4,6-Dioxoheptanoic acid is a potent inhibitor of heme biosynthesis. Dec 19 2024
E7250 Taurohyodeoxycholic acid sodium Taurohyodeoxycholic acid (THDCA) sodium is the taurine-conjugated form of the secondary bile acid hyodeoxycholic acid. Taurohyodeoxycholic acid can also reduce the activity and expression of myeloperoxidase TNF-α and IL-6, as well as colonic damage in TNBS-induced ulcerative colitis mouse model. Dec 19 2024
E5126 Juglanin Juglanin, a occurring flavonoid that can be isolated from crude Polygonum aviculare, is a JNK acticator, with anti-inflammatory, anti-oxidant and anti-tumor activities. Juglanin can induce apoptosis and autophagy on human breast cancer cells. Dec 19 2024
E1417 Sertindole Sertindole (Lu 23-174) is an orally active 5-HT2A, 5-HT2C, dopamine D2, and αl-adrenergic receptors antagonist. Sertindole shows antipsychotic activity and anti-proliferative activity to multiple cancer cells. Dec 19 2024
E7036 Ditiocarb sodium Ditiocarb sodium (Sodium diethyldithiocarbamate) is an accelerator of the rate of copper cementation. Sodium diethyldithiocarbamate reduces the incidence of HIV infection, and also enhances adjuvant immunoresearch of high risk breast cancer. Dec 19 2024
E7251 SLIGRL-NH2 SLIGRL-NH2 (Protease-Activated Receptor-2 Activating Peptide) is an agonist of Protease-Activated Receptor-2 (PAR-2). Dec 19 2024
E7037 Aflatoxin B1 0 Dec 19 2024
E4962 Ferric citrate Ferric citrate (Iron(III) citrate), an orally active iron supplement, is an efficacious phosphate binder. Ferric citratee can be used for iron deficiency anemia and chronic kidney disease (CKD) research. Dec 19 2024
E7038 Z-LEHD-FMK Z-LEHD-FMK is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK exhibits the neuroprotective effect in a rat model of spinal cord trauma. Dec 19 2024
E7252 α-L-Fucosidase, Microorganism α-L-Fucosidase, Microorganism (EC 3.2.1.51) is an enzyme that catalyzes the chemical reaction. Serum activity of α-L-Fucosidase, Microorganism, a lysosomal enzyme present in all mammalian cells, has been proposed as a marker of hepatocellular carcinoma (HCC). Dec 19 2024
E1058 Triacsin C Triacsin C (WS 1228A), a natural intracellular long-chain acyl-CoA synthetases (ACSL) inhibitor, is from Streptomyces aureofaciens. Triacsin C inhibits TAG accumulation into lipid droplets (LD) by suppressing ACSL activity. Triacsin C is found to be highly effective against rotavirus replication. Dec 19 2024
E7253 Creatinine-d3 Creatinine-d3 is a deuterium labeled Creatinine. Creatinine is a break-down product of creatine phosphate in muscle[1]. Dec 19 2024
E7039 27-Hydroxycholesterol 27-Hydroxycholesterol (27-OHC) is a selective estrogen receptor modulator and an agonist of the liver X receptor. Dec 19 2024
E7254 Zinc Gluconate Zinc Gluconate has the potential for the research of common cold, cancer, and a nutrition supplement as a food additive. Dec 19 2024
E7255 Rupatadine Rupatadine (UR-12592) is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine can be used for the research of allergic rhinitis and urticaria. Dec 19 2024
E7040 Glycol chitosan Glycol chitosan is a chitosan derivative with ethylene glycol branches. Glycol chitosan enhances membrane permeability and leadkage in Glycine max Harosoy 63W cells. Glycol chitosan is biocompatible and biodegradable. Glycol chitosan inhibits E. coli, S. aureus and S. enteritidis growths with MIC values of 4 μg/mL, 32 μg/mL and <0.5 μg/mL, respectively. Dec 19 2024
E7256 Calf thymus DNA Calf thymus DNA (DNA from calf thymus) is high quality double-stranded template DNA isolated from the thymus of male and female calves. Calf thymus DNA can be used for the research of the interaction between DNA and agents. Dec 19 2024
E7041 Desmosterol Desmosterol is a molecule similar to cholesterol. Desmosterol is the immediate precursor of cholesterol in the Bloch pathway of cholesterol biosynthesis. Desmosterol, as an endogenous metabolite, used to study cholesterol metabolism. Dec 19 2024
E7257 Menaquinone-7 Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs (orally active), is originally discovered as the anti-hemorrhagic factors. Menaquinone-7 inhibits osteoclast bone resorption in vitro and stimulates bone formation in femoral tissue of aged female rats. Menaquinone-7 has a well-researched potential in the prevention of aging-induced bone degeneration. Menaquinone-7 is also a pharmacological option for activating Gla matrix protein and intervening in the progression of calcific aortic stenosis (CAVS). Dec 19 2024
E7042 SMIP004 SMIP004 is a SKP2 E3 ligase inhibitor, which downregulates SKP2 and to stabilise p27. SMIP004 is a cancer cell selective apoptosis inducer of human prostate cancer cells. Dec 19 2024
E7258 Polymyxin B Polymyxin B is an antibiotic. Polymyxin B inhibits Gram-negative infections by binding to the LPS of the bacterial wall with high affinity. Polymyxin B neutralizes the effect of endotoxin. Polymyxin B induces bacterial death by increasing its permeability. Polymyxin B is used in endotoxemia research. Dec 19 2024
E7043 Penicillin G Penicillin G is a potent penicillinantibiotic. Penicillin G can be used for bacterial infection. Penicillin G has potent activity against all Gram-positive bacteria and Gram-negative cocci. Dec 19 2024
E7044 DSPC DSPC (1,2-Distearoyl-sn-glycero-3-phosphorylcholine) is a cylindrical-shaped lipid. DSPC is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system. Dec 19 2024
E6037 Perindopril Perindopril erbumine is an angiotensin-converting enzyme inhibitor. Perindopril erbumine modulates NFκB and STAT3 signaling and inhibits glial activation and neuroinflammation. Perindopril erbumine can be used for the research of Chronic Kidney Disease and high blood pressure. Dec 19 2024
E7045 iRGD peptide iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of agents by first binding to αv-integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties. Dec 19 2024
E7259 Nelociguat Nelociguat (BAY60-4552) is a nitric oxide sensitive soluble guanylate cyclase stimulator. Dec 19 2024
E7046 TRAP-6 TRAP-6 (PAR-1 agonist peptide), a peptide fragment, is a selective protease activating receptor 1 (PAR1) agonist. TRAP-6 activates human platelets via the thrombin receptor. TRAP-6 shows no activity at PAR4. Dec 19 2024
E7260 Tolrestat Tolrestat is a potent, orally active aldose reductase inhibitor with IC50 of 35 nM. Dec 19 2024
E7047 β-Amyloid (1-40) β-Amyloid (1-40) is a primary protein in plaques found in the brains of patients with Alzheimer's disease. Dec 19 2024
E7261 Chlorotoxin Chlorotoxin is a 36 amino-acid peptide from the venom of the Israeli scorpion Leiurus quinquestriatus with anticancer activity. Chlorotoxin is a chloride channel blocker. Dec 19 2024
E1799 Streptonigrin Streptonigrin (Bruneomycin), a natural product produced by Streptomyces flocculus, possesses both anti-tumor and anti-bacterial activity. Streptonigrin acts as a pan-PAD inhibitor with IC50s of 48.3±34.2 µM, 26.1±0.3 µM, 0.43±0.03 µM, and 2.5±0.4 µM for PAD1, PAD2, PAD3, and PAD4, respectively. Dec 19 2024
E7048 Pronase E (Activity ≥ 4000 U/mg) Pronase E (Activity ≥ 4000 U/mg) is a mixture of proteolytic enzymes that is obtained from Streptomyces griseus and could digest protein into individual amino acids. Dec 19 2024
E7262 Darifenacin Darifenacin (UK-88525) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin inhibits tumor growth in colorectal cancer cells and has anti-tumor effects. Dec 19 2024
E7049 Fexofenadine Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research. Dec 19 2024
E7263 Elastase, Porcine pancreas Elastase, Porcine pancreas (EC 3.4.21.36) is a single polypeptide chain of 240 amino acid residues, derived from pig pancreas. Elastase, Porcine pancreas is a serine protease that can hydrolyze proteins and polypeptide. Elastase from porcine pancreas can induce emphysema in hamsters. Dec 19 2024
E7050 CC-401 CC-401 is a potent inhibitor of all three forms of JNK with Ki of 25 to 50 nM. Dec 19 2024
E7264 Cyclic GMP sodium Cyclic GMP sodium (cGMP) is an important regulator of short-term changes in smooth muscle tone and longer-term responses to chronic drug research or proliferative signals, it is in response to atrial natriuretic peptide (ANP) or nitric oxide (NO). Cyclic GMP sodium interacts with cation channels to regulate ion transport or activate the cyclic GMP-dependent protein kinase to result in protein phosphorylation. Dec 19 2024
E7051 Tempo Tempo is a nitric oxide radical and a selective scavenger of ROS in mitochondria. Tempo is also an organocatalyst that disproportionates superoxide and oxidizes primary alcohols to aldehydes in a catalytic cycle. Tempo has mutagenic and antioxidant effects and can induceDNA strand breaks. Tempo also exerts cytotoxic and mutagenic properties in mouse lymphoma cells. Dec 19 2024
E7265 Davunetide Davunetide is an eight amino acid snippet derived from activity-dependent neuroprotective protein (ADNP), a neurotrophic factor that exists in the mammalian CNS. Davunetide possesses neuroprotective, neurotrophic and cognitive protective roperties. Davunetide, a microtubule-stabilizing peptide, interacts with and stabilises neuron-specific βIII-tubulin in vitro. Davunetide penetrates the blood-brain barrier and is non-toxic. Davunetide inhibits Aβ aggregation and Aβ-induced neurotoxicity. Dec 19 2024
E7052 2-(Pyridyldithio)ethylamine hydrochloride 2-(Pyridyldithio)ethylamine hydrochloride is a novel disulfide intercalating cross-linking reagent. Dec 19 2024
E7266 Aurintricarboxylic acid Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway. Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM. Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM. Dec 19 2024
E7053 Neomycin Neomycin is an aminoglycoside antibiotic. Neomycin can be used for the research of external or internal bacterial infections, is primarily administered in veterinary medicine as a sulfate salt. Dec 19 2024
E7267 Astressin Astressin is a potent corticotropin releasing factor (CRF) antagonist. Dec 19 2024
E1035 GW-1100 GW-1100 is a selective GPR40 antagonist with a pIC50 of 6.9. Dec 19 2024
E7268 β-N-methylamino-L-alanine hydrochloride β-N-methylamino-L-alanine hydrochloride (BMAA hydrochloride) is a neurotoxin produced by cyanobacteria. β-N-methylamino-L-alanine hydrochloride could cause amyotrophic lateral sclerosis (ALS) and possibly other neurodegenerative diseases. Dec 19 2024
E6036 Fluvoxamine Fluvoxamine (DU-23000) is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor. Dec 19 2024
E7269 Retrorsine Retrorsine is a naturally occurring toxic pyrrolizidine alkaloid. Retrorsine can bind with DNA and inhibits the proliferative capacity of hepatocytes. Retrorsine can be used for the research of hepatocellular injury. Dec 19 2024
E7054 PAβN dihydrochloride PAβN dihydrochloride (MC-207110 dihydrochloride) is an efflux pump inhibitor. Dec 19 2024
E7270 Atosiban acetate Atosiban acetate (RW22164 acetate;RWJ22164 acetate) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research. Dec 19 2024
E7055 Polydatin Polydatin (Piceid), extracted from the roots of Reynoutria japonica, a widely used traditional Chinese remedies, possesses anti-inflammatory activity in several experimental models. Polydatin (Piceid) inhibits G6PD and induces oxidative and ER stresses. Dec 19 2024
E7271 Enniatin B1 Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes. Enniatin B1 crosss the blood-brain barrier. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation. Dec 19 2024
E7056 Tacalcitol Tacalcitol (1,24(R)-Dihydroxyvitamin D3; 1. Dec 19 2024
E7272 Chlorothalonil Chlorothalonil is a broad-spectrum foliar fungicide with oral activity. Chlorothalonil can be used to combat fungal diseases in vegetable and crop leaves. Chlorothalonil can alter the microbial community in the soil. Chlorothalonil inhibits spermatogenesis. Chlorothalonil can cause intestinal epithelial barrier dysfunction and fetal toxicity. Dec 19 2024
E5076 Tomatidine Tomatidine acts as an anti-inflammatory agent by blocking NF-κB and JNK signaling. Tomatidine activates autophagy either in mammal cells or C elegans. Dec 19 2024
E7273 Dehydrothio-p-toluidine Dehydrothio-p-toluidine (DHPT) is a chemical intermediate used in dyestuff production. Dehydrothio-p-toluidine shows inhalation toxicity in acute and subchronic conditions. Dec 19 2024
E7057 Tebipenem Tebipenem is an orally available carbapenem antibiotic, shows broad-spectrum activity against Gram-positive and -negative bacteria, except for Pseudomonas aeruginosa. Dec 19 2024
E7274 NADP NADP is a coenzyme involved in cellular electron transfer reactions in biological metabolism, which is alternately oxidized (NADP+) and reduced (NADPH), and can maintain cellular redox homeostasis and regulate many biological events, including cellular metabolism. NADPH is a universal electron donor that provides reducing ability for synthetic metabolic reactions and redox balance. NADPH plays a multifunctional role in regulating inflammation, redox homeostasis, and synthetic metabolism processes. Dec 19 2024
E0648 AH 6809 AH 6809 is an antagonist of EP and DP receptor, with Kis of 1217, 1150, 1597, and 1415 nM for the cloned human EP1, EP2, EP3-III, and DP receptor respectively. AH 6809 has a Ki of 350 nM for mouse EP2 receptor. Dec 19 2024
E7275 N-1-Naphthylphthalamic acid N-1-Naphthylphthalamic acid (Alanap 1) is a modulator of polar auxin transport that competes with auxin (indole-3-acetic acid, IAA) for membrane binding sites. N-1-Naphthylphthalamic acid also disrupts maize leaf initiation, KNOX protein regulation, and leaf margin formation. Dec 19 2024
E7058 DM4 DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody agent conjugate. Dec 19 2024
E7276 Ercalcitriol Ercalcitriol (1α,25-Dihydroxy Vitamin D2) is an active metabolite of vitamin D2. Dec 19 2024
E7059 Alcian Blue 8GX Alcian Blue 8GX is a commonly used phthalocyanine dye that binds to glycoproteins and glycosaminoglycans. Alcian Blue 8GX has a wide range of applications in biological staining, including proteins in brain tumors and DNA in cells and tissues. Dec 19 2024
E7277 DiSC3(5) DiSC3(5) is a fluorescent probe commonly used as a tracer dye to evaluate mitochondrial membrane potential. The excitation/emission wavelength of DiSC3(5) is up to 622/670 nm. DiSC3(5) can inhibit the respiratory system associated with mitochondrial NAD, and the IC50 value is 8 μM. DiSC3(5) in the presence of Na+/K+-ATPase inhibitor ouabain 2 can induce membrane hyperpolarization of Ehrlich ascites tumor cells. Dec 19 2024
E7060 AQC AQC (6-Aminoquinolyl-N-hydroxysccinimidyl carbamate) is a reagent used for amino acid or protein sequence analysis by HPLC with fluorescence detection. AQC reacts with primary and secondary amino acids to yield fluorescent derivates, allowing amino acid detection at under-picomolar levels. Dec 19 2024
E7278 L-Methionine-DL-sulfoximine L-Methionine-DL-sulfoximine (MSX; MSO), a highly specific and irreversible inhibitor of Glutamine synthetase (GS), is also a potent convulsant which metabolically and morphologically primarily affects astroglia. L-Methionine-DL-sulfoximine has been employed to inhibit the Gln-dependent ammonia-stimulated neuronal toxicity in vitro, potentiating Gln deficit-dependent depression. L-Methionine-DL-sulfoximine tremendously increases the rate of release of fixed nitrogen in cyanobacteria. L-Methionine-DL-sulfoximine is a promising candidate for research in biofertilizers and convulsive seizures (CS). Dec 19 2024
E7061 Tarenflurbil Tarenflurbil ((R)-Flurbiprofen) is the R-enantiomer of the racemate NSAID Flurbiprofen, Tarenflurbil ((R)-Flurbiprofen) inhibits the binding of [3H]9-cis-RA to RXRα LBD with IC50 of 75 μM. Tarenflurbil can be used for Alzheimer's disease research. Dec 19 2024
E7279 Inosinic acid Inosinic acid is an endogenous metabolite. Inosinic acid is used as umami tastant and dietary supplement. Dec 19 2024
E7062 Olverembatinib Olverembatinib (GZD824) is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib has antitumor activity. Olverembatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 19 2024
E7280 Xanthosine 5'-monophosphate sodium salt Xanthosine 5'-monophosphate sodium salt (5'-Xanthylic acid sodium salt) is an intermediate in purine metabolism. Xanthosine 5'-monophosphate sodium salt can be used for genetic code, nucleic acid structure, and DNA, RNA and protein synthesis research. Dec 19 2024
E7063 Endoxifen (Z-isomer) Endoxifen Z-isomer is the most important Tamoxifen metabolite, inducing an anti-estrogenic effect in breast cancer cells expressing ERα. Endoxifen Z-isomer inhibits hERG. This effect is concentration-dependent, with an IC50 value of 1.6 μM. Dec 19 2024
E7281 7-Methylguanosine 7-Methylguanosine is a novel cNIIIB nucleotidase inhibitor with IC50 value of 87.8 ± 7.5 µM. Dec 19 2024
E1419 Talnetant Talnetant (SB 223412) is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant can be used in schizophrenia-related studies. Dec 19 2024
E7282 N6-Isopentenyladenosine N6-Isopentenyladenosine (Riboprine), an RNA modification found in cytokinins, which regulate plant growth/differentiation, and a subset of tRNAs, where it improves the efficiency and accuracy of translation. N6-Isopentenyladenosine, an end product of the mevalonate pathway, is an autophagy inhibitor with an interesting anti-melanoma activity. Dec 19 2024
E7064 Tyr-Gly-Gly-Phe-Met-OH Tyr-Gly-Gly-Phe-Met-OH regulates human immune function and inhibits tumor growth via binding to the opioid receptor. Dec 19 2024
E7283 Vitamin K2 Vitamin K2 is an endogenous metabolite. Dec 19 2024
E7065 PCPA methyl ester hydrochloride PCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride), a reversible tryptophan hydroxylase inhibitor, is a serotonin (5-HT) synthesis inhibitor. PCPA methyl ester hydrochloride crosses the blood brain barrier and reduces 5-HT central availability. Dec 19 2024
E7284 SB-222200 SB-222200 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant NK-3 receptor antagonist. SB-222200 is developed for central nervous system (CNS) disorders. Dec 19 2024
E7066 N-Acetyl-L-cysteine ethyl ester N-Acetyl-L-cysteine ethyl ester is an esterified form of N-acetyl-L-cysteine (NAC). N-Acetyl-L-cysteine ethyl ester exhibits enhanced cell permeability, and produce NAC and cysteine. N-Acetyl-L-cysteine ethyl ester increases circulating hydrogen sulfide (H2S) and can be used as an H2S producer. N-Acetyl-L-cysteine ethyl ester has the potential to substitute NAC as a mucolytic agent, and as a GSH-related antioxidant. Dec 19 2024
E7285 Licarbazepine Licarbazepine (BIA 2-005; GP 47779)?is a?voltage-gated sodium channel?blocker?with?anticonvulsant?and?mood-stabilizing?effects. Dec 19 2024
E7067 UDP-GlcNAc disodium UDP-GlcNAc Disodium Salt (UDP-α-D-N-Acetylglucosamine Disodium Salt) is a donor substrate of O-GlcNAc transferase (OGT). Dec 19 2024
E7286 1,4-Dicaffeoylquinic acid 1,4-Dicaffeoylquinic acid (1,4-DCQA) is a phenylpropanoid from Xanthii fructus, inhibits LPS-stimulated TNF-α production. Dec 19 2024
E7068 Novobiocin Novobiocin (Albamycin) is a potent and orally active antibiotic. Novobiocin also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin shows anti-orthopoxvirus activity. Dec 19 2024
E7287 Neurokinin A Neurokinin A (Substance K), a peptide neurotransmitter of the tachykinin family, acts via the NK-2 receptor. Neurokinin A acts as a major mediator in human airway and gastrointestinal tissues. Dec 19 2024
E7069 2-Thenoyltrifluoroacetone 2-Theoyltrifluoroacetone is a chelating agent and mitochondrial electron transfer chain inhibitor, with a IC50 value of 51.5 μM. 2-Thermoyltrifluoroacetone can chelate with various metal ions and has cytotoxicity and anti-tumor activity, which is expected to play an important role in the treatment of mitochondrial dysfunction related diseases[1][2][3]. Dec 19 2024
E1996 Salinomycin sodium salt Salinomycin sodium salt (Salinomycin sodium), an antibiotic potassium ionophore, is a potent inhibitor of Wnt/β-catenin signaling. Salinomycin sodium salt (Salinomycin sodium) acts on the Wnt/Fzd/LRP complex, blocks Wnt-induced LRP6 phosphorylation, and causes degradation of the LRP6 protein. Salinomycin sodium salt (Salinomycin sodium) shows selective activity against human cancer stem cells. Dec 19 2024
E7070 DiBAC4(3) DiBAC4(3) is a voltage-sensitive fluorescent dye (λex=490 nm, λem=505 nm). Dec 19 2024
E7288 Denatonium benzoate Denatonium benzoate (THS-839) is known as the most bitter compound and is commonly used as a deterrent (bittering agent) to activate different types of bitter taste receptors (TAS2Rs) with oral activity. Denatonium benzoate can enhance insulin secretion, has anti-inflammatory effects, and promotes allergy susceptibility . Dec 19 2024
E7071 Neuromedin N Neuromedin N is a potent modulator of dopamine D2 receptor agonist binding in rat neostriatal membranes. Dec 19 2024
E7289 Linseed oil Linseed oil is a biochemical reagent that can be used as a biological material or organic compound for life science related research. Dec 19 2024
E7072 CY7-SE CY7-SE is a CY dye. CY, short for Cyanine, is a compound consisting of two nitrogen atoms connected by an odd number of methyl units. Cyanine compounds have the characteristics of long wavelength, adjustable absorption and emission, high extinction coefficient, good water solubility and relatively simple synthesis. CY dyes are of en used for the labeling of proteins, antibodies and small molecular compounds. For the labeling of protein antibodies, the combination can be completed through a simple mixing reaction. Below, we introduce the labeling method of protein antibody labeling, which has certain reference significance. Dec 19 2024
E7290 Chlorhexidine (digluconate) Chlorhexidine digluconate is a chlorophenyl biguanide with broad antibacterial action against both Gram (+) and (-) bacteria and fungi. Chlorhexidine digluconate is a broad-spectrum antiseptic and disinfectant. Chlorhexidine digluconate is effective to prevent and control infectious diseases of the mouth by killing bacteria in saliva and tongue. Chlorhexidine digluconate is a cytotoxic agent and induces cell necrosis and apoptosis. Dec 19 2024
E7073 Rigosertib Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle. Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM. Dec 19 2024
E7291 N-tert-Butyl-α-phenylnitrone N-tert-Butyl-α-phenylnitrone is a nitrone-based free radical scavenger that forms nitroxide spin adducts. N-tert-Butyl-α-phenylnitrone inhibits COX2 catalytic activity. N-tert-Butyl-α-phenylnitrone has potent ROS scavenging, anti-inflammatory, neuroprotective, anti-aging and anti-diabetic activities, and can penetrate the blood-brain barrier. Dec 19 2024
E7074 Sulfo-NHS-LC-Biotin sodium Sulfo-NHS-LC-Biotin sodium is an amine-reactive biotinylation reagent that can be used for antibody labeling. Dec 19 2024
E7292 Beta-glucuronidase (Escherichia coli) Beta-glucuronidase is an important lysosomal enzyme involved in the degradation of glucuronate-containing glycosaminoglycan. Dec 19 2024
E7075 Secalciferol Secalciferol ((24R)-24,25-Dihydroxyvitamin D3) is the major active metabolite of Vitamin D. Secalciferol activates vitamin D receptor (VDR) with an EC50 value of 150 nM. Secalciferol is involved in a wide range of biological functions such as calcium homeostasis, cellular differentiation and proliferation processes, as well as other functions related to the immune system, which is promising for research of rickets, osteomalacia, hypercalcemia and autoimmune disorders. Dec 19 2024
E7293 Terazosin Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin works by relaxing blood vessels and the opening of the bladder. Terazosin has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment. Dec 19 2024
E7076 BTZ043 BTZ043 is an inhibitor of decaprenyl-phosphoribose-epimerase (DprE1), with MICs of of 2.3 nM and 9.2 nM for M. tuberculosis H37Rv and Mycobacterium smegmatis, respectively. Dec 19 2024
E4953 Citalopram Citalopram is a racemate mixture of the active S(+)-enantiomer (Escitalopram; HY-14258) and R(-)-enantiomer. Citalopram is an orally active selective serotonin reuptake inhibitor (SSRI). Citalopram is an antidepressant and enhances serotoninergic neurotransmission. Dec 19 2024
E7077 DSRM-3716 DSRM-3716 (5-Iodoisoquinoline) is a potent and selective SARM1 NADase inhibitor with an IC50 of 75 nM. DSRM-3716 is selective against other NAD+-processing enzymes, receptors, and transporters. DSRM-3716 provides robust axon protection. Dec 19 2024
E7294 TFLLR-NH2 TFLLR-NH2 is a selective PAR1 agonist with an EC50 of 1.9 μM. Dec 19 2024
E7078 N2,N2-Dimethylguanosine N2,N2-Dimethylguanosine is an urinary nucleoside, a primary degradation product of tRNA. Dec 19 2024
E7079 Ensitrelvir Ensitrelvir (S-217622) is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM). Dec 19 2024
E7295 Dabsyl chloride Dabsyl chloride is an amine derivatizing agent, able to give rise to stable products that can be easily monitored spectrophotometrically at 460 nm; Dabsyl chloride also used for labeling amino acids. Dec 19 2024
E7080 Dihomo-γ-linolenic acid Dihomo-γ-linolenic acid (DGLA) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system. Dec 19 2024
E7296 Amine-PEG3-Biotin Amine-PEG3-Biotin is a signal amplification label containing a biotin group and a terminal primary amine group. Dec 19 2024
E7081 Purpurin 18 Purpurin 18, a derivative of chlorophyll and a type of dihydroporphyrin, is used to produce photosensitizers. Purpurin 18 photodynamic therapy can induce cell apoptosis and has anti-tumor activity. Dec 19 2024
E7297 Tris(4,7-diphenyl-1,10-phenanthroline)ruthenium(II) dichloride Tris(4,7-diphenyl-1,10-phenanthroline)ruthenium(II) dichloride is an oxygen-sensitive fluorescent indicator widely used as a probe for luminescence detection and quantitative oxygen determination. Dec 19 2024
E7082 5(6)-Carboxyfluorescein 5(6)-Carboxyfluorescein (5(6)-FAM) is an amine-reactive pH-sensitive green fluorescent probe. 5(6)-Carboxyfluorescein (5(6)-FAM) can be used to label proteins, peptides and nucleotides. 5(6)-Carboxyfluorescein can be used for the detection of tumour areas in vivo. Dec 19 2024
E7298 NSC-87877 NSC-87877 is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively. NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26). Dec 19 2024
E4965 Dinoprost Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour. Dec 19 2024
E7299 Veratridine Veratridine (3-Veratroylveracevine) is a plant neurotoxin, a voltage-gated sodium channels (VGSCs) agonist. Veratridine inhibits the peak current of Nav1.7, with an IC50 of 18.39 µM. Veratridine regulates sodium ion channels mainly by activating sodium ion channels, preventing channel inactivation and increasing sodium ion flow. Dec 19 2024
E7083 BTS BTS (N-Benzyl-p-toluenesulfonamide) is a potent and selective inhibitor of skeletal muscle myosin II subfragment 1 (S1) ATPase activity, with an IC50s of ~5 μM for actin- and Ca2+-stimulated myosin S1 ATPase. BTS specifically inhibits the contraction of fast skeletal muscle fibers. Dec 19 2024
E7300 Sulfanitran Sulfanitran is an antibacterial and anticoccidial agent used in poultry feeds. Sulfanitran also is a multidrug resistance protein 2 (MRP2) stimulator that can increase the affinity of MRP2 for estradiol-17-β-D-glucuronide (E217βG). Dec 19 2024
E7084 C6 Ceramide C6 Ceramide (C6-Cer) is a short-chain, cell-permeable ceramide pathway activator with anticancer activity. C6 Ceramide-mediated miR-29b expression participates in the progression of multiple myeloma through suppressing the proliferation, migration and angiogenesis of endothelial cells by targeting Akt signal pathway. C6 Ceramide exhibits multiple anti-cancer properties including cell cycle arrest, Apoptosis, inhibition of tumor growth and enhances the effects of chemotherapy in drug-resistant cancer cells. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects. Dec 19 2024
E7301 Atrasentan Atrasentan (ABT-627) is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA. Dec 19 2024
E7085 Laurdan Laurdan is a membrane-permeable fluorescent probe that displays spectral sensitivity to the phospholipid phase of the cell membrane to which it is bound. Quantitation of generalized polarization (GP) of Laurdan can be used to identify phospholipid phase. Dec 19 2024
E7302 Nolatrexed dihydrochloride Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of thymidylate synthase, interacts at the folate cofactor binding site of the enzyme, with a Ki of 11 nM for human thymidylate synthase. Nolatrexed dihydrochloride (AG 337) induces cell cycle arrest in S phase of cancer cells. Anti-cancer activity. Dec 19 2024
E7086 Kanamycin Kanamycin (Kanamycin A) is an orally active antibacterial (gram-negative/positive bacteria) agent, inhibits translocation and causes misencoding by binding to the 70 S ribosomal subunit. Kanamycin shows good inhibitory activity to both M. tuberculosis (sensitive and drug-resistant ) and K. pneumonia, which can be used in studies of tuberculosis and pneumonia. Dec 19 2024
E7303 Telotristat ethyl Telotristat ethyl (LX1032) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production. Dec 19 2024
E4721 Ammonium tetrathiomolybdate Ammonium tetrathiomolybdate is a copper chelator and also is a class of sulfide donor. Ammonium tetrathiomolybdate has neuroprotection effects. Ammonium tetrathiomolybdate can be used for the research of brain ischemia. Dec 19 2024
E7304 Xanthine oxidase, Microorganism Xanthine oxidase, Microorganism (XO) is a xanthine oxidoreductase enzyme that generates reactive oxygen species (ROS), catalyzes the oxidation of hypoxanthine to xanthine, and further catalyzes the oxidation of xanthine to uric acid. Dec 19 2024
E2927 WST-1 WST-1 is a kind of water-soluble tetrazolium salt. WST induces the intracellular mitochondrial dehydrogenase to conduct NADH-dependent enzyme digestion reaction, releasing the water-soluble methyl benzene product. WST-1 can be used for the detection of cell proliferation and cytotoxicity, via the determination of the light absorption value at 450 nm. Dec 19 2024
E7305 Penconazole Penconazole is a typical triazole fungicide, and mainly applied on apples, grapes, and vegetables to control powdery mildew. Penconazole inhibits sterol biosynthesis in fungi. Penconazole decrease AChE activity in the cerebrum and cerebellum of rats. Dec 19 2024
S7866 Fumonisin B1 Fumonisin B1 is a mycotoxin produced from Fusarium moniliforme. Fumonisin B1 is a potent inhibitor of sphingosine N-acyltransferase (ceramide synthase) and disrupts de novo sphingolipid biosynthesis. Fumonisin B1 is the most abundant and toxic fumonisin. Dec 19 2024
E1776 Benzo[a]pyrene Benzo[a]pyrene shows lung carcinogenicity in animal models, and it is frequently used in chemoprevention studies. Dec 19 2024
E7087 Fluorescein-5-maleimide Fluorescein-5-maleimide (N-(5-Fluoresceinyl)maleimide) is a fluorescent dye. Fluorescein-5-maleimide can be used to detect the redox state of thiols in eukaryotic cells. Fluorescein-5-maleimide can label peptides and is used to detect negatively charged nanoparticles. Fluorescein-5-maleimide can also label actin to explore its interaction with cardiac myosin-binding protein C (cMyBP-C), which helps in developing small molecule modulators for heart failure. Fluorescein-5-maleimide can screen mutant proteins that contain cysteine residues. The excitation wavelength of Fluorescein-5-maleimide is 494 nm, and the emission wavelength is 519 nm. Dec 19 2024
E7306 Benzalkonium chloride Benzalkonium chloride is a potent anti-microbial agent, used as a preservative in eye drops. Dec 19 2024
E7088 Acetyl Coenzyme A trisodium Acetyl-coenzyme A (Acetyl-CoA) trisodium is a membrane-impermeant central metabolic intermediate, participates in the TCA cycle and oxidative phosphorylation metabolism. Acetyl-coenzyme A trisodium, regulates various cellular mechanisms by providing (sole donor) acetyl groups to target amino acid residues for post-translational acetylation reactions of proteins. Acetyl Coenzyme A trisodium is also a key precursor of lipid synthesis. Dec 19 2024
E7307 Dulaglutide Dulaglutide (LY2189265) is a glucagon-like peptide-1 (GLP-1) receptor agonist. Dulaglutide can be uesd for the research of type 2 diabetes (T2D) . Dec 19 2024
E7089 Cefepime Cefepime (BMY-28142) is a broad-spectrum and cross the blood-brain barrier cephalosporin. Cefepime shows antibacterial effects against both Gram-positive and Gram-negative aerobic bacteria. Cefepime induces neurotoxicity. Dec 19 2024
E7308 Calcium N5-methyltetrahydrofolate Calcium N5-methyltetrahydrofolate(NSC173328) is the calcium salt of levomefolic acid, which has been proposed for treatment of cardiovascular disease and advanced cancers such as breast and colorectal cancers. Dec 19 2024
E7090 Coenzyme Q0 Coenzyme Q0 (CoQ0) is a potent, oral active ubiquinone compound can be derived from Antrodia cinnamomea. Coenzyme Q0 induces apoptosis and autophagy, suppresses of HER-2/AKT/mTOR signaling to potentiate the apoptosis and autophagy mechanisms. Coenzyme Q0 regulates NFκB/AP-1 activation and enhances Nrf2 stabilization in attenuation of inflammation and redox imbalance. Coenzyme Q0 has anti-angiogenic activity through downregulation of MMP-9/NF-κB and upregulation of HO-1 signaling. Dec 19 2024
E7309 Nociceptin Nociceptin, a heptadecapeptide, is the endogenous ligand of the nociceptin receptor, acting as a potent anti-analgesic. Dec 19 2024
E7091 Pirodavir Pirodavir is a potent, broad-spectrum picornavirus inhibitor, and is highly active against both group A and group B rhinovirus serotypes.Pirodavir is very potent in a virus yield reduction assay (IC90=2.3 nM). Dec 19 2024
E7310 Fosfomycin calcium Fosfomycin (MK-0955) calcium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin calcium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria. Dec 19 2024
S6989 Digitoxin Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure . Dec 19 2024
E7092 Arg-Gly-Asp-Ser Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1. Dec 19 2024
E7311 Ammonium bicarbonate,AR,99% Ammonium bicarbonate is a bioactive chemical. Dec 19 2024
E7093 5(6)-CFDA 5(6)-CFDA is a common aliphatic luciferin-line organism. CFDA conducts free diffusion into cells, and then it is hydrolyzed into carboxyl fluorescein (CF) by intracellular non-specific lipase. CF containing portion contains an additional negative charge so that it is better retained in cells, compared to fluorescein dyes. Dec 19 2024
E7312 Complete Freund's adjuvant (CFA) Complete Freund's adjuvant (CFA) is an immunoadjuvant emulsified with antigen by its discoverer Jules T. Freund to enhance an animal's immune response to an antigen. Complete Freund's adjuvant (CFA) is also an inducer of the Th1 immune response and a ligand of TLRs. Complete Freund's adjuvant (CFA) contains heat-killed inactive tuberculosis bacilli and consists of a paraffin oil-in-water emulsion. Complete Freund's adjuvant (CFA) stimulates a strong and durable immune response and can be used to induce persistent inflammatory pain models in mice, experimental autoimmune myocarditis (EAM) models, and more. Incomplete Freund's adjuvant (IFA) (HY-153808A) is another type of Freund's Adjuvant that stimulates a weaker immune response. Dec 19 2024
E7094 5-TAMRA-SE 5-TAMRA-SE is an amine-reactive fluorescent agent, and its conjugate produces bright, pH-insensitive orange-red fluorescence with good photostability. Dec 19 2024
E7313 TLR4-IN-C34-C2-COOH TLR4-IN-C34-C2-COO is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis. Dec 19 2024
E7095 BS-181 BS-181 is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880, 3000 and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 has the potential for the research of cancer therapy. Dec 19 2024
E7314 α-CGRP(human) α-CGRP(human) is a regulatory neuropeptide of 37 amino acids. α-CGRP(human) is widely distributed in the central and peripheral nervous system. α-CGRP(human) is a potent vasodilator. Dec 19 2024
E7096 Insulin(cattle) Insulin cattle is a two-chain polypeptide hormone produced in vivo in the pancreatic β cells. Insulin cattle has often been used as growth supplement in culturing cells. Dec 19 2024
E7315 Catalase, Aspergillus niger Catalase, Aspergillus niger is a key enzyme in the metabolism of H2O2 and reactive oxygen species (ROS), and its expression and localization is markedly altered in tumors. Free oxygen radical scavenger. Dec 19 2024
E7097 Cyclic-di-GMP Cyclic-di-GMP is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP can be used in cancer research. Dec 19 2024
E7316 Cholecystokinin Octapeptide, desulfated Cholecystokinin Octapeptide, desulfated is a synthetic desulfated octapeptides of cholecystokinin (CCK). Dec 19 2024
E1407 α-Galactosylceramide α-Galactosylceramide (α-GalCer) is a synthetic glycolipid with antitumorial and immunostimulatory. α-Galactosylceramide is a very potent NKT cell agonist and binds effectively to CD1d. The complex of α-Galactosylceramide plus CD1d binds the NKT cell TCR (T cell antigen receptor). Dec 19 2024
E7317 Tetrac Tetrac (Tetraiodothyroacetic acid), a derivative of L-thyroxine (T4), is a thyrointegrin receptor antagonist. Tetrac blocks the actions of T4 and 3,5,3'-triiodo-L-thyronine (T3) at the cell surface receptor for thyroid hormone on integrin αvβ3. Tetra has anti-angiogenic and anti-tumor activities. Dec 19 2024
E5381 Xylose D-(+)-xylose (Xylose) is a natural compound that is catalyzed by xylose isomerase to form xylulose, which is a key step in the anaerobic ethanol fermentation of xylose. Dec 19 2024
E7098 Orexin A (human, rat, mouse) Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats. Dec 19 2024
E7318 GGTI298 GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 20 μM in vivo, respectively. Dec 19 2024
E5785 5-Fluorouridine 5-Fluorouridine, a metabolite of 5-fluorouracil (HY-90006), is a potent ribozyme self-cleavage inhibitor. 5-Fluorouridine incorporates into both total and poly A RNA and has antiproliferative activity. 5-Fluorouridine induces apoptosis. Dec 19 2024
E7319 Aureobasidin A Aureobasidin A (Basifungin) is a cyclic peptide antibiotic with oral activity. Aureobasidin A is an inhibitor of inositol phosphorylated ceramide synthetase AUR1. Aureobasidin A has antifungal and antiparasitic activity. Dec 19 2024
E7099 Hypotaurine Hypotaurine (2-aminoethanesulfinic acid), an intermediate in taurine biosynthesis from cysteine in astrocytes, is an endogenous inhibitory amino acid of the glycine receptor. Antioxidant. Dec 19 2024
E7320 Penicillic acid Penicillic acid is a polyketide mycotoxin produced by several species of Aspergillus and Penicillium. Penicillic acid exhibits cytotoxicity in rat alveolar macrophages (AM) in vitro. Penicillic acid inhibits Fas ligand-induced apoptosis by blocking self-processing of caspase-8. Dec 19 2024
E7100 Ellipticine Ellipticine (NSC 71795) is a potent antineoplastic agent; inhibits DNA topoisomerase II activities. Dec 19 2024
E7321 Diallyl Trisulfide Diallyl Trisulfide is an orally active anticancer agent that can be isolated from garlic. Diallyl Trisulfide has the ability to induce apoptosis and exhibits anticancer, anti-inflammatory, antioxidant, and antibacterial activities. Diallyl Trisulfide can be used to study a variety of cancers, including liver, colon and prostate cancer. Dec 19 2024
E7101 5-Aminolevulinic acid 5-Aminolevulinic acid (5-ALA) is a non-protein amino acid that plays a rate-limiting role in heme biosynthesis. Dec 19 2024
E7322 Valacyclovir Valacyclovir (Valaciclovir) is an orally active antiviral agent for herpes simplex, herpes zoster, and herpes B. Valacyclovir inhibits HSV-1 W (50=2.9 μg/ml). Valacyclovir is a proagent of Aciclovir (HY-17422) . Dec 19 2024
E7102 Triapine Triapine (3-AP; PAN-811) is a potent inhibitor of the M2 subunit of ribonucleotide reductase (RR), and is a potent radiosensitizer. Dec 19 2024
E7323 Fevipiprant Fevipiprant (QAW039, NVP-QAW039) is s an orally active, selective, reversible prostaglandin D2 (DP2) receptor antagonist with an Kd value of 1.14 nM. Fevipiprant has the potential for the research of bronchial asthma. Dec 19 2024
E1911 AY 9944 AY 9944 is a specific cholesterol biosynthesis inhibitor. AY 9944 inhibits the 7-dehydro cholesterol Δ7-reductase (DHCR7) enzyme with an IC50 of 13 nM. AY 9944 causes hypocholesterolemia and accumulation of 7DHC. At high doses, AY 9944 inhibits also in cultured embryos sterol Δ7-Δ8 isomerase, which causes the accumulation of cholest-8-en-3β-ol. Dec 19 2024
E7324 Maxacalcitol Maxacalcitol (22-Oxacalcitriol), a vitamin D3 (HY-15398) analog, is an orally active VDR agonist. Maxacalcitol has a limited calcemic effect. Maxacalcitol has the potential for psoriasis and hyperparathyroidism research. Dec 19 2024
E7103 Ertapenem Ertapenem (MK-0826) is a broad spectrum and long acting β-lactam antibiotic. Ertapenem has a broad-spectrum anti-anaerobic activity against a variety of anaerobes with a mode MIC of 0.12 μg/mL. Ertapenem can be used for the research of severe infections caused by bacteria in the skin, lungs, stomach, pelvis, and urinary tract. Dec 19 2024
E7325 9,10-Anthracenediyl-bis(methylene)dimalonic acid 9,10-Anthracenediyl-bis(methylene)dimalonic acid (ABMDMA) is a biological dye and indicator used to detect singlet oxygen generation (SOG). 9,10-Anthracenediyl-bis(methylene)dimalonic acid is water-soluble derivative of anthracene. 9,10-Anthracenediyl-bis(methylene)dimalonic acid can be photobleached by singlet oxygen to its corresponding endoperoxide. This reaction can be monitored spectrophotometrically by recording the decrease of absorbance at 400 nm. Dec 19 2024
E7104 Deoxycorticosterone Deoxycorticosterone is a steroid hormone produced by the adrenal gland that possesses mineralocorticoid activity and acts as an aldosterone precursor. Deoxycorticosterone is an agonist for O. mykiss mineralocorticoid receptor (rtMR) transcription with EC50 of 0.16 nM. Deoxycorticosterone could acts as an immune stimulator in fish. Dec 19 2024
E7326 Sitafloxacin Sitafloxacin (DU6859a) is a potent, orally active fluoroquinolone antibiotic. Sitafloxacin shows antichlamydial activity and antibacterial activities against a broad range of gram-positive and gram-negative bacteria, including anaerobic bacteria, as well as against atypical pathogens. Sitafloxacin can be used for the research of respiratory tract infection and urinary tract infection. Dec 19 2024
E7105 Coumestrol Coumestrol, a phytoestrogen present in soybean products, exhibits activities against cancers, neurological disorders, and autoimmune diseases. It suppresses proliferation of ES2 cells with an IC50 of 50 μM. Dec 19 2024
E7327 Isotetrandrine Isotetrandrine is a bioactive component in Stephania tetrandra. Dec 19 2024
E5306 Demethylsuberosin Demethylsuberosin (7-Demethylsuberosin) is a coumarin compound isolated from Angelica gigas Nakai, and has anti-inflammatory activity. Dec 19 2024
E7328 2,2'-Bipyridine 2,2'-Bipyridine is the unique molecular scaffold of the bioactive natural products. 2,2'-Bipyridine is extensively used as the core structure of many chelating ligands by acting as a bridge in the arrangement of the catalytic center. 2,2'-Bipyridine shows robust redox stability and hyperglycemic activity. Dec 19 2024
E4882 Octreotide Octreotide (SMS 201-995) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide (SMS 201-995) can bind to the somatostatin receptor and mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production. Octreotide (SMS 201-995) has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly. Dec 19 2024
E5043 Rehmannioside A Rehmannioside A is a neuroprotective agent that can be isolated from Rehmanniae radix. Rehmannioside A can inhibit the release of proinflammatory mediators from microglia and promote M2 polarization in vitro, thereby protecting co-cultured neurons from apoptosis by inhibiting NF-κB and MAPK signaling pathways. Rehmannioside A can be used in spinal cord injury research. Dec 19 2024
E7106 Procainamide Procainamide (Procaine amide) is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1), which reactivates the expression of tumor suppressor factors by demethylating tumor suppressor genes. Procainamide induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide relaxes airway smooth muscle by activating potassium channels. Procainamide can be used in cancer and arrhythmia research. Dec 19 2024
E7329 8-Bromo-cAMP 8-Bromo-cAMP (8-Br-Camp), a cyclic AMP analog, is an activator of cyclic AMP-dependent protein kinase (PKA). 8-Bromo-cAMP has anti-proliferative and apoptotic effects against cancer cells. Dec 19 2024
E7107 Quercetin 3-O-β-D-glucofuranoside Quercetin 3-O-β-D-glucofuranoside is an effective antioxidant and an eosinophilic inflammation suppressor. Dec 19 2024
E7330 Biotin-PEG4-NHS ester Biotin-PEG4-NHS ester is a biotin-labeled, PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Dec 19 2024
E7108 Kaempferol 3-O-β-D-glucuronide Kaempferol 3-O-β-D-glucuronide (Kaempferol-3-glucuronide) is a metabolite of kaempferol that can be taken orally and has anti-inflammatory properties. Kaempferol 3-O-β-D-glucuronide can activate AKT/GSK3β phosphorylation and improve glucose metabolism. Dec 19 2024
E7331 Bismuth subgallate Bismuth subgallate, a hemostatic agent, acts on coagulation factor XII (Hageman factor), leading to the activation of the coagulation cascade and improving early formation of a fibrin clot. Dec 19 2024
E7109 PKI(5-24) PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor. Dec 19 2024
E7332 Parathyroid Hormone (1-34), bovine Parathyroid Hormone (1-34), bovine is a potent parathyroid hormone (PTH) receptor agonist. Parathyroid Hormone (1-34), bovine increases calcium and inorganic phosphate levels in vivo. Parathyroid Hormone (1-34), bovine can be used for th reseach of osteoporosis. Dec 19 2024
E7110 2'-Deoxycytidine hydrochloride 2'-Deoxycytidine hydrochloride is composed of the purine nucleoside guanine linked by its N9 nitrogen to the C1 carbon of deoxyribose. Dec 19 2024
E7333 Semaglutide Semaglutide, a long-acting GLP-1 analogue, is a glucagon-like peptide-1 (GLP-1) receptor agonist. Semaglutide has the potential for type 2 diabetes treatment. Dec 19 2024
E5781 2',3'-cGAMP 2',3'-cGAMP (2'-3'-cyclic GMP-AMP) is a endogenous cGAMP in mammalian cells. 2',3'-cGAMP binds to STING with a high affinity and is a potent inducer of interferon-β (IFNβ). 2',3'-cGAMP is produced in mammalian cells in response to DNA in the cytoplasm. Dec 19 2024
E7111 Picaridin Picaridin (Lcaridin) is a broad spectrum arthropod repellent. The repellent and deterrent activities of Picaridin involve olfactory sensing in mosquitoes, and ticks, via their interactions with odorant receptor proteins. Dec 19 2024
E7334 Cyclo(RGDyK) Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM. Dec 19 2024
E7112 Buformin hydrochloride Buformin hydrochloride (1-Butylbiguanide hydrochloride), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin hydrochloride decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin hydrochloride also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al). Dec 19 2024
E7335 L-γ-Glutamyl-p-nitroanilide L-γ-Glutamyl-p-nitroanilide Monohydrate is a glutamic acid derivative. Dec 19 2024
E7113 4-P-PDOT 4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity). Dec 19 2024
E7336 Tuftsin Tuftsin is a tetrapeptide. Tuftsin is a macrophage/microglial activator. Dec 19 2024
E7114 Biotin-azide Biotin-azide (N-(3-Azidopropyl)biotinamide) is a form of biotin with a terminal azide group. Biotin-azide can be used to prepare various biotinylated conjugates via Click Chemistry. Biotin-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. Dec 19 2024
E7337 CLP290 CLP290 is an orally available activator of the neuron-specific K+-Cl? cotransporter KCC2, displays potential for treatment of a wide range of neurological and psychiatric indications. CLP290 can significantly lower blood arginine-vasopressin (AVP) and glucose levels in STZ (HY-13753) rats. Dec 19 2024
E7115 TUG-770 TUG-770 is a potent, selective and orally active GPR40/FFA1 agonist with an EC50 of 6 nM for human FFA1. TUG-770 shows a high selectivity for FFA1 over FFA2, FFA3, FFA4, PPARγ, other receptors, transporters, and enzymes. TUG-770 can be uesd for type 2 diabetes research. TUG-770 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 19 2024
E4978 (S)-Rasagiline (S)-Rasagiline (TVP1022) is the relatively inactive S-enantiomer form of Rasagiline. Rasagiline is a highly potent selective irreversible MAO inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively. (S)-Rasagiline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 19 2024
E7116 Deoxynivalenol Deoxynivalenol, an orally active mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors. Dec 19 2024
E7338 Sodium copper chlorophyllin B Sodium copper chlorophyllin B exerts antiviral activities against Influenza virus and HIV with IC50s of 50 to 100 μM for both of them. Dec 19 2024
E7117 1-Methyladenosine 1-Methyladenosine is an RNA modification that can serve as a tumor marker, with elevated levels in the body associated with cancer development. Following 1-methyladenosine methylation, upregulation of PPARδ expression regulates cholesterol metabolism and activates Hedgehog signaling pathway, driving liver tumorigenesis. Dec 19 2024
E7339 6-TAMRA-SE 6-TAMRA-SE (6-TAMRA-NHS ester) is a fluorescent dye carrying the amine reactive group. 6-TAMRA-SE is one of the traditional fluorophores used for automated DNA sequencing. Dec 19 2024
E5794 Ionomycin calcium Ionomycin calcium (SQ23377 calcium) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin calcium (SQ23377 calcium) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin calcium (SQ23377 calcium) also induces the activation of protein kinase C (PKC). Dec 19 2024
E7340 Dabigatran (ethyl ester) Dabigatran ethyl ester is an emerging oral anticoagulant which is a direct inhibitor of thrombin activity. Dec 19 2024
E7118 Uridine triphosphate Uridine triphosphate (UTP) is a pyrimidine nucleoside triphosphate that is used as a substrate to synthesize RNA or as an energy source in metabolic reactions. Uridine triphosphate activates membrane-bound P2Y2 receptors. Dec 19 2024
E7341 Tofogliflozin Tofogliflozin(CSG-452) is a potent and highly specific sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2. Dec 19 2024
E7119 Fagomine Fagomine is a mild glycosidase inhibitor. The Ki of the iminosugar Fagomine is 4.8 μM, 39 μM, and 70 μM for Amyloglucosidase (A.niger), β-Glucosidase (bovine), and Isomaltase (yeast), respectively. Dec 19 2024
E7342 Enocyanin Enocyanin is an anthocyanin extracted from grapes. Enocyanin shows inhibitory effect on the leucine aminopeptidase, acid phosphatase, γ-glutamyl transpeptidase and esterase activity. Dec 19 2024
E7120 Sobetirome Sobetirome (GC-1) is a thyroid hormone receptor β (TRβ)-specific agonist which bind selectively to TRβ-1 with an EC50 of 0.16 μM. Dec 19 2024
E7343 γ-Tocotrienol γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a novel radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment. Dec 19 2024
E7121 Elacestrant Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER+ breast cancer cell lines in vitro and in vivo. Dec 19 2024
E7344 Aurantiamide acetate Aurantiamide acetate (TMC-58A) is a selective and orally active cathepsin inhibitor isolated from?Portulaca oleracea L. Aurantiamide acetate has anti-inflammatory activities and can be used for the study of ?inflammatory?diseases. Dec 19 2024
E1693 Ryanodine Ryanodine is a cell permeant ryanodine receptor modulator. Ryanodine can either stimulate or inhibit Ryanodine-mediated Ca2+ release depending on its concentrations. Poisonous diterpenoid found in Ryania speciosa. Dec 19 2024
E7345 Balaglitazone Balaglitazone is a selective partial PPARγ agonist with an EC50 of 1.351 μM for human PPARγ. Dec 19 2024
E7122 Guanosine 5'-diphosphate disodium salt Guanosine 5'-diphosphate (GDP) disodium salt, a purine nucleoside diphosphate, is interconverted to guanosine by the action of exonucleotidase and phosphorylation of nucleoside to guanine. Guanosine 5'-diphosphate disodium salt activates adenosine 5'-triphosphate-sensitive K+ channel and is used to study the kinetics and characteristics of GTPases such as those associated with G-protein coupled receptors (GPCR). Guanosine 5'-diphosphate disodium salt is a potential iron mobilizer, which prevents the Hepcidin (HY-P70400)-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Elevated levels of guanosine 5’-diphosphate are associated with the pathogenesis of neurological diseases. Guanosine 5'-diphosphate disodium salt Dec 19 2024
E7346 NVP-BSK805 NVP-BSK805 is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively. Dec 19 2024
E7123 Seocalcitol Seocalcitol is a vitamin D analog, binds vitamin D receptor protein from human osteosarcoma MG-63 cells with Kd of 0.27 nM. Dec 19 2024
E7347 S-Nitroso-N-acetyl-DL-penicillamine S-Nitroso-N-acetyl-DL-penicillamine (SNAP) is a nitric oxide donor and acts as a stable inhibitor of platelet aggregation. Dec 19 2024
E7124 Ercalcidiol 0 Dec 19 2024
E5257 Epmedin C Epmedin C, a natural product, has estrogen-like effects for ovariectomized mice. Dec 19 2024
E7125 Vitamin D4 Vitamin D4 (22-Dihydroergocalciferol) is a Vitamin D derived from fungi. The precursor of Vitamin D4 is 22,23-dihydroergosterol. Dec 19 2024
E7348 Moracin C Moracin C, a natural product, is an anti-inflammatory agent. Moracin C inhibits LPS-activated reactive oxygen species (ROS) and nitric oxide (NO) release from cells. Dec 19 2024
E7126 Licochalcone C Licochalcone C could inhibit α-glucosidase, with IC50s of <100 nM and 92.43 μM for α-glucosidase and protein tyrosine phosphatase 1B (PTP1B), respectively. Dec 19 2024
E5267 Sanggenon C Sanggenon C, a flavonoid, exerts protective effects against cardiac hypertrophy and fibrosis via suppression of the calcineurin/NFAT2 pathway. Sanggenon C inhibits mitochondrial fission to induce apoptosis by blocking the ERK signaling pathway. Sanggenon C inhibits inducible nitric oxide synthase expression in RAW264.7 cells, and TNF-α-stimulated cell adhesion and VCAM-1 expression, by suppressing NF-κB activity. Sanggenon C possesses antioxidant, anti-inflammatory and antitumor activities. Dec 19 2024
E7349 T-1105 T-1105, a structural analogue of T-705, is a novel broad-spectrum viral polymerase inhibitor. T-1105 inhibits the polymerases of RNA viruses after being converted to ribonucleoside triphosphate (RTP) metabolite. T-1105 has antiviral activity against various RNA viruses. T-1105 can be formed by nicotinamide mononucleotide adenylyltransferase. Dec 19 2024
E7127 Vasopressin Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis, and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of corticotropin releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors. Dec 19 2024
E7350 4-Aminobenzamidine dihydrochloride 4-Aminobenzamidine (p-Aminobenzamidine) dihydrochloride is a strong trypsin inhibitor, also acting as a relatively weak urokinase type plasminogen activator (uPA) inhibitor (Ki=82 μM). 4-Aminobenzamidine can inhibit growth of a human prostate tumor in SCID mice. Dec 19 2024
E5621 Eriocalyxin B Eriocalyxin B is an ent-Kaurene diterpenoid isolated from Chinese herb Isodon eriocalyx. Eriocalyxin B has anti-cancer and anti-infammatory activities. Eriocalyxin B induces cell apoptosis. Dec 19 2024
E7351 KRCA-0008 KRCA-0008 is a selective ALK/Ack1 inhibitor with IC50s of 12 and 4 nM for ALK and Ack1, respectively. KRCA-0008 can be used for the research of cancer. Dec 19 2024
E7128 NPPB NPPB is a blocker of the outwardly rectifying chloride channel (ORCC). Dec 19 2024
E7352 3-Methyl-2-oxovaleric acid 3-Methyl-2-oxovaleric acid is a neurotoxin, an acidogen, and a metabotoxin, and also an abnormal metabolite that arises from the incomplete breakdown of branched-chain amino acids. Dec 19 2024
E4614 Coelenterazine h Coelenterazine h (2-Deoxycoelenterazine), a coelenterazine derivative, is a luminescent substrate for RLuc8. Coelenterazine h is more sensitive to Ca2+, thus providing a valuable tool for measuring small changes in Ca2+ concentrations. Dec 19 2024
E7353 Gamma-glutamylcysteine Gamma-glutamylcysteine (γ-Glutamylcysteine), a dipeptide containing cysteine and glutamic acid, is a precursor to glutathione (GSH). Gamma-glutamylcysteine is a cofactor for glutathione peroxidase (GPx) to increase GSH levels. Dec 19 2024
E7129 Lasalocid sodium Lasalocid sodium (Lasalocid-A sodium) is an antibacterial agent. Dec 19 2024
E5542 Gypenoside A Gypenoside A is a natural compound isolaated from Gynostemma pentaphyllum Makino. Dec 19 2024
E7130 D-Glucose 6-phosphate D-Glucose 6-phosphate is a glucose sugar phosphorylated at the hydroxy group on carbon 6. Dec 19 2024
E7354 Dimethyl succinate Dimethyl succinate is a biochemical reagent that can be used as a biological material or organic compound for life science related research. Dec 19 2024
E7131 L-Homocysteine L-Homocysteine, an amino acid, is a homocysteine that has L configuration. Homocysteine is an essential intermediate in normal mammalian metabolism of methionine. L-Homocysteine induces upregulation of Cathepsin V that mediates vascular endothelial inflammation in hyperhomocysteinaemia. Dec 19 2024
E7355 Bremelanotide Bremelanotide (PT-141) is an analogue of α-melanocyte-stimulating hormone (α-MSH). Bremelanotide activates the mPOA and other hypothalamic and limbic regions of the brain involved in sexual behavior. Bremelanotide can be used for researching hypoactive sexual desire disorders. Dec 19 2024
E7132 5-CFDA 5-CFDA is a common aliphatic luciferin-line organism. CFDA conducts free diffusion into cells, and then it is hydrolyzed into carboxyl fluorescein (CF) by intracellular non-specific lipase. CF containing portion contains an additional negative charge so that it is better retained in cells, compared to fluorescein dyes. Dec 19 2024
E7356 Thiophanate-Methyl Thiophanate-Methyl is a systematic fungicide. Dec 19 2024
E7133 HCGRP-(8-37) HCGRP-(8-37) is a human calcitonin gene-related peptide (hCGRP) fragment and also an antagonist of CGRP receptor. Dec 19 2024
E7357 δ-Tocotrienol δ-Tocotrienol is a Vitamin E in vegetables, fruits, seeds, nuts, grains and oils. Vitamin E has become well known for its role as an antioxidant, in lowering cholesterol and other lipids, as a neuroprotective and anticancer agent, and in cardiovascular disease protection. Dec 19 2024
E7134 Osteogenic Growth Peptide, OGP Osteogenic Growth Peptide, OGP is a short, naturally occurring 14-mer growth factor peptide found in serum at μM concentrations. Dec 19 2024
E7358 Epothilone D Epothilone D (KOS 862) is a potent microtubule stabilizer. Dec 19 2024
E7135 Meldonium dihydrate Meldonium (MET-88) dihydrate functions as a cardioprotective agent by cpmpetetively inhibiting γ-butyrobetaine hydroxylase (BBOX) and carnitine/organic cation transporter type 2 (OCTN2). Mildronate dihydrate exhibits IC50 values of 34-62 μM for human recombinant BBOX and an EC50 of 21 μM for human OCTN2. Meldonium dihydrate is a fatty acid oxidation inhibitor. Dec 19 2024
E7359 A-674563 A-674563 is an orally active Akt1 inhibitor with a Ki of 11 nM. Dec 19 2024
E7136 Mal-β-CD Mal-β-CD is a cellular cholesterol modifier which can form soluble inclusion complex with cholesterol. Dec 19 2024
S7376 Bay 60-7550 Bay 60-7550 is a potent and selective PDE2 inhibitor with a Ki of 3.8 nM. Dec 19 2024
E7137 Protease-Activated Receptor-2, amide Protease-Activated Receptor-2, amide (SLIGKV-NH2) is a highly potent protease-activated receptor-2 (PAR2) activating peptide. Dec 19 2024
E7360 Zearalanone Zearalenone is a nonsteroidal estrogenic mycotoxin produced by Fusarium species, which colonizes several grains. Zearalenone has low acute toxicity and carcinogenicity. Due to its agonistic effect on the estrogen receptor, Zearalenone exhibits distinct estrogenic and anabolic properties in several animal species, resulting in severe effects on the reproductive system. Dec 19 2024
E7138 5-TAMRA 5-TAMRA can produce bright, pH-insensitive orange-red fluorescence (excitation and emission extremes of 546/579) and has good photostability. Dec 19 2024
E7361 (±)-Huperzine A (±)-Huperzine A, an active Lycopodium alkaloid extracted from traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD). Dec 19 2024
E7139 Gastric mucin Gastric mucin is a large glycoprotein which is thought to play a major role in the protection of the gastrointestinal tract from acid, proteases, pathogenic microorganisms, and mechanical trauma. Dec 19 2024
E7362 Virginiamycin M1 Virginiamycin M1 (Pristinamycin IIA; Ostreogrycin A), produced by Streptomyces virginiae, is an polyunsaturated macrocyclic lactone antibiotic and acts as a component of Virginiamycin (HY-112665). Virginiamycin M1 alone is against Staphylococcus aureus with a MIC of 0.25 μg/mL. Dec 19 2024
E7140 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC (POPC), a phospholipid, is a major component of biological membranes. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC is used for the preparation of liposomes and studying the properties of lipid bilayers. Dec 19 2024
E7363 Canthaxanthin Canthaxanthin is a red-orange carotenoid with various biological activities, such as antioxidant, antitumor properties. Dec 19 2024
E7141 Lysozyme Lysozyme (Muramidase) is a conserved antimicrobial protein. Lysozyme exerts its bactericidal effect by hydrolyzing bacterial cell wall peptidoglycan (PG). Lysozyme plays an important role in limiting bacterial growth on mucosal surfaces and other sites, not only controlling potential pathogens but also limiting overgrowth of microbiota to prevent dysbiosis. Extracellular lysozyme can also degrade polymeric PG into soluble fragments, activate NOD receptors in mucosal epithelial cells, and lead to the secretion of chemokines and activating factors by neutrophils and macrophages. Dec 19 2024
E7364 2'-Deoxy-2'-fluorocytidine 2'-Deoxy-2'-fluorocytidine, an nucleoside analog, is a potent inhibitor of Crimean-Congo hemorrhagic fever virus (CCHFV) replication. 2′-deoxy-2′-fluorocytidine can act synergistically with T705 to increase the potency of both compounds antiviral effects on CCHFV replication. Dec 19 2024
E7142 CGP-42112 CGP-42112 (CGP-42112A) is a potent Angiotensin-II subtype 2 receptor(AT2 R) agonist. Dec 19 2024
E7365 3-Epiursolic Acid 3-Epiursolic Acid is a triterpenoid that can be isolated from Eriobotrya japonica, acts as a competitive inhibitor of cathepsin L (IC50, 6.5 μM; Ki, 19.5 μM), with no obvious effect on cathepsin B. Dec 19 2024
E6008 Miglustat hydrochloride Miglustat (N-Butyldeoxynojirimycin) hydrochloride is an orally active and reversible ceramide glucosyltransferase inhibitor. Miglustat hydrochloride can be used for the research of type I gaucher disease. Dec 19 2024
E1666 TPPB TPPB is a cell-permeable benzolactam-derived protein kinase C (PKC) activator with a Ki of 11.9 nM. Dec 19 2024
E7143 DTE DTE (Dithioerythritol) is a sulfur-containing sugar derived from the corresponding 4-carbon monosaccharide erythrose; an epimer of dithiothreitol (DTT). Dec 19 2024
E7366 Veliparib dihydrochloride Veliparib (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Kis of 5.2 nM and 2.9 nM in cell-free assays, respectively. Dec 19 2024
E7144 PAR-4 Agonist Peptide, amide PAR-4 Agonist Peptide, amide (PAR-4-AP; AY-NH2) is a proteinase-activated receptor-4 (PAR-4) agonist, which has no effect on either PAR-1 or PAR-2 and whose effects are blocked by a PAR-4 antagonist. Dec 19 2024
E7367 Beaucage reagent Beaucage reagent is found to be potent in causing DNA cleavage. Dec 19 2024
E7145 Borrelidin Borrelidin (Treponemycin) is a bacterial and eukaryal threonyl-tRNA synthetase inhibitor which is a nitrile-containing macrolide antibiotic isolated from Streptomyces rochei. Borrelidin is an inhibitor of Cdc28/Cln2 of the budding yeast, with an IC50 of 24 μM. Borrelidin is a potent angiogenesis inhibitor, with an IC50 of 0.8 nM. Borrelidin induces apoptosis in the tube-forming cells. Borrelidin has strong antimalarial activities, with IC50s of 1.9 nM and 1.8 nM against K1 and FCR3 strains of Plasmodium falciparum, respectively. Dec 19 2024
E7368 Light green SF yellowish Light green SF yellowish (Acid Green 5) is a triarylmethane dye. Light green SF yellowish is a highly selective mitochondrial stain. Light green SF yellowish is usually available as a disodium salt and has a maximum absorption value as 629 nm. Light green SF yellowish can be used as a histological stain for collagen and a critical component of Papanicolaou stains. Dec 19 2024
E7146 VIP(6-28)(human, rat, porcine, bovine) VIP(6-28)(human, rat, porcine, bovine) is an effective antagonist of the actions of exogenous vasoactive intestinal peptide (VIP) on cAMP. Dec 19 2024
E7369 Zaprinast Zaprinast (M&B 22948) is a selective inhibitor of cGMP-selective Phosphodiesterase (PDE5). Zaprinast causes a significant increase in cGMP levels in myocytes. Zaprinast is a G protein-coupled receptor 35 (GPR35) agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects. Dec 19 2024
E1518 DPQ DPQ is a potent PARP-1 inhibitor. DPQ can reduce the N-methyl-d-aspartate (NMDA)-induced PARP activation, restoring ATP to near control levels and significantly attenuating neuronal injury in the severe NMDA exposure model. DPQ can be used for researching neuroprotection. Dec 19 2024
E7370 Chromium(III) acetate Chromium(III) acetate (Chromic acetate) is an AMPK inhibitor that promotes lipogenesis by inhibiting AMPK phosphorylation. Chromium(III) acetate has low toxicity in mammals, with an LD50 of 2365 mg/kg in rats. Dec 19 2024
E7371 Bifenthrin Bifenthrin is a synthetic pyrethroid insecticide. Bifenthrin prolongs the opening time of Nav1.8 sodium channels, leading to membrane depolarization and conductance block in the insect nervous system, thereby disrupting neural function. Bifenthrin was effective in inhibiting A. gambiae (LD50=0.15 ng/mg) and C. quinquefasciatus (LD50=0.16 ng/mg). Bifenthrin has good lethality against susceptible and resistant mosquitoes and is very effective in inhibiting blood sucking and can be developed as a mosquito-removal netting material. Dec 19 2024
E7147 Senktide Senktide is a tachykinin NK3 receptor agonist. Dec 19 2024
E7372 N,N-Dimethylacetamide N,N-Dimethylacetamide (DMAc) is an organic solvent with blood-brain transmissibility and an FDA-approved drug excipient. N, N-dimethylacetamide exerts anti-inflammatory activity by inhibiting the NF-κB signaling pathway. N, N-dimethylacetamide can be used in studies of weight gain caused by a high-fat diet and neuroinflammation in Alzheimer's disease. Dec 19 2024
E7148 SB-269970 SB-269970 is a potent, selective and brain-penetrant 5-HT7 receptor antagonist with a pKi of 8.3. SB-269970 exhibits >50-fold selectivity against other 5-HT receptors. Dec 19 2024
P1233 β-Amyloid (1-42), (rat/mouse) β-Amyloid (1-42), (rat/mouse) is a 42-aa peptide, shows cytotoxic effect on acute hippocampal slices, and used in the research of Alzheimer's disease. Dec 19 2024
E7149 Nitrilotriacetic acid Nitrilotriacetic acid is an aminotricarboxylic acid. Nitrilotriacetic acid can be used as a chelating agent, forming coordination compounds with metal ions. Dec 19 2024
E7373 Ketone monoester Ketone monoester is an orally available ketone monoester that serves as a source of nutritional ketones. Ketone monoester increases plasma beta-hydroxybutyrate, acetoacetate, blood glucose, blood sodium, and blood creatinine levels in mouse models. Ketone monoester has the potential to improve athletic performance and endurance in animals. Ketone monoester partially prevents myasthenia in septic mice. Ketone monoester may also be used to study Parkinson's disease or diabetes. Dec 19 2024
E7150 Tirbanibulin dihydrochloride Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Dec 19 2024
E7374 Idarubicin Idarubicin is an orally active and potent anthracycline antileukemic agent. Idarubicin inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription. Idarubicin shows induction of DNA damage. Idarubicin inhibits DNA synthesis and of c-myc expression. Idarubicin inhibits the growth of bacteria and yeasts. Dec 19 2024
E7151 Mephenytoin Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate. Dec 19 2024
E7375 Phenanthrene Phenanthrene is an orally active polycyclic aromatic hydrocarbon (PAH) that induces inflammation, oxidative stress, and apoptosis. Additionally, phenanthrene is commonly used to detect or assess PAH pollution in the environment. Dec 19 2024
E7152 Neurotensin(8-13) Neurotensin (8-13) is an active fragment of Neurotensin. Neurotensin(8-13) results in a decrease in cell-surface NT1 receptors (NTR1) density. Dec 19 2024
E7376 Fluorene Fluorene, a polycyclic aromatic hydrocarbon (PAH), is a precursor to other fluorene compounds. Fluorene and its derivative can be used as a precursor to fluorene-based dyes. Dec 19 2024
E7153 C2 Ceramide C2 Ceramide (Ceramide 2) is the main lipid of the stratum corneum and a protein phosphatase 1 (PP1) activator. C2 Ceramide activates PP2A and ceramide-activated protein phosphatase (CAPP). C2 Ceramide induces cells differentiation, autophagy and apoptosis, inhibits mitochondrial respiratory chain complex III. C2 Ceramide is also a skin conditioning agent that protects the epidermal barrier from water loss. Dec 19 2024
E7377 Acenaphthylene Acenaphthylene is a polycyclic aromatic hydrocarbon (PAH). PAHs are derived naturally from coal and tar deposits, and produced by incomplete combustion of organic matter. Dec 19 2024
E7154 C16-Ceramide C16-Ceramide is a natural small molecule activating p53 through the direct and selective binding. Dec 19 2024
E7378 Chrysene Chrysene is a high molecular weight (HMW), polycyclic aromatic hydrocarbon (PAH) known for its recalcitrance and carcinogenic properties. Dec 19 2024
E7155 Prolylleucine Prolylleucine is a dipeptide containing branched-chain amino acids. Prolylleucine can affect the circadian rhythms and behaviour of animals. Dec 19 2024
E5720 Isocurcumenol Isocurcumenol, an estrogen receptor alpha (ERα) inhibitor isolated from Curcuma zedoaria Rhizomes, possesses anti-tumor acticity, with IC50 values of 99.1μg/mL and 178.2 μg/mL in DLA and KB cells, respectively. Dec 19 2024
E7156 CE3F4 CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively. Dec 19 2024
E7379 Amifostine thiol dihydrochloride Amifostine thiol (WR-1065) dihydrochloride can protect normal tissues from the toxic effects of certain cancer agents and activate p53 through a JNK-dependent signaling pathway. Dec 19 2024
E7157 FSLLRY-NH2 FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor. Dec 19 2024
E7380 Pafuramidine Pafuramidine (DB289) is an orally active proagent of Furamidine (HY-110137A). Pafuramidine is a potent anti-parasitic agent, can be used to research trypanosomiasis, Pneumocystis pneumonia and malaria. Dec 19 2024
E7158 Brilliant Blue FCF Brilliant Blue FCF is an aromatic hydrocarbon, a synthetic dye produced from petroleum and used as a colorant for food and other substances. The solution has a maximum absorption at 628 nm. Dec 19 2024
E7381 Collagenase, Type I Collagenase, Type I is a microbially derived matrix metalloproteinases (MMPs) and zinc peptidase. Collagenase, Type I breaks down collagens 1, 3, 7, 8, 10, gelatin, proteoglycans, aggrecan. Dec 19 2024
E5071 3-Acetyl-beta-boswellic acid 3-Acetyl-beta-boswellic acid is a boswellic acid isolated from Boswellia serrata gum resin. Dec 19 2024
E7159 Remdesivir O-desphosphate acetonide impurity Remdesivir O-desphosphate acetonide impurity is an impurity of Remdesivir. Remdesivir (GS-5734), a nucleoside analogue with effective antiviral activity and is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro. Dec 19 2024
E7382 5-Methoxy-DL-tryptophan 5-Methoxy-DL-tryptophan is an endogenous metabolite. Dec 19 2024
E7160 Diltiazem Diltiazem is an orally active L-type Ca2+ channel blocker. Diltiazem shows antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris. Dec 19 2024
E7383 Lucidin Lucidin (NSC 30546) is a natural component of Rubia cordifolia. Dec 19 2024
E1695 9-cis-Retinoic acid 9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities. Dec 19 2024
E7384 Sulfamethoxazole-d4 Sulfamethoxazole-d4 is a deuterium labeled Sulfamethoxazole (Ro 4-2130). Sulfamethoxazole is a sulfonamide bacteriostatic antibiotic[1]. Dec 19 2024
E7161 Fibronectin Fibronectin, a glycoprotein present in blood as well as in cells, is a biomarker of tissue injury. Fibronectin binds to membrane-spanning receptor proteins called integrins. Fibronectin also binds to other extracellular matrix proteins such as collagen, fibrin, and heparan sulfate proteoglycans. Dec 19 2024
E4753 NNK NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser70 and c-Myc at Thr58 and Ser62 through activation of both ERK1/2 and PKCα. NNK induces survival and proliferation of human lung cancer cells. NNK can be used for lung cancer mice model structure. Dec 19 2024
E7385 1,4-DPCA 1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM. Dec 19 2024
E7162 CTAP CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction. Dec 19 2024
E7386 Fructose Fructose is a simple ketonic monosaccharide found in many plants, where it is often bonded to glucose to form the disaccharide sucrose. Dec 19 2024
E7163 [Des-Arg9]-Bradykinin [Des-Arg9]-Bradykinin is a Bradykinin (B1) receptor agonist that displays selectivity for B1 over B2 receptors. Dec 19 2024
E7387 Metalaxyl Metalaxyl is a fungicide agent that inhibits the protein synthesis in fungi. Metalaxyl against downy mildews and soil-borne diseases by Phytium ssp. and Phytophthora ssp.. Dec 19 2024
E7164 β-Endorphin, human β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioid receptor, with preferred affinity for μ-opioid receptor and δ-opioid receptor; β-Endorphin, human exhibits antinociception activity. Dec 19 2024
E7388 (S)-2-Allylglycine (S)-2-Allylglycine is a peptide derivative. Dec 19 2024
E7165 4-Diethylaminobenzaldehyde 4-Diethylaminobenzaldehyde is a reversible aldehyde dehydrogenases (ALDHs) inhibitor, with a Ki of 4 nM for ALDH1. 4-Diethylaminobenzaldehyde displays potent anti-androgenic effect (IC50= 1.71μM). Dec 19 2024
E7389 Tetrahydrofolic acid Tetrahydrofolic acid (L-5,6,7,8-Tetrahydrofolic acid) is the biologically active vitamin B9 folate derivative. Tetrahydrofolic acid is a donor of one-carbon groups for amino acids, nucleic acids, and lipids. Tetrahydrofolic acid serves as an acceptor of free formaldehyde, producing 5,10-methylenetetrahydrofolate-Tetrahydrofolic acid. Dec 19 2024
E7166 Tafluprost acid Tafluprost acid (AFP-172), an active metabolic form of Tafluprost, is a selective prostanoid FP receptor agonist. Tafluprost acid shows a high affinity for human prostanoid FP receptor with Ki and EC50 values of 0.4 nM and 0.53 nM, respectively. Tafluprost acid has 126 times weaker binding affinity for prostanoid EP3 receptor (IC50=67 nM) than for the prostanoid FP receptor. Tafluprost acid can be used in the research of glaucoma. Dec 19 2024
E7390 1-Palmitoyl-sn-glycero-3-phosphocholine 1-Palmitoyl-sn-glycero-3-phosphocholine is an abundant lysophosphatidylcholine. 1-Palmitoyl-sn-glycero-3-phosphocholine exhibits proinflammatory activity. 1-Palmitoyl-sn-glycero-3-phosphocholine can be used in the study of atherosclerosis. Dec 19 2024
E4948 Latanoprost acid Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor. Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes. Dec 19 2024
E7391 Flutrimazole Flutrimazole is an imidazole antifungal with dual anti-inflammatory and antifungal activity. Flutrimazole shows scarce transdermal penetration. Flutrimazole has the advantageous in the research of topical fungal infections with an inflammatory component. Dec 19 2024
E7167 Cefaclor Cefaclor is a well-absorbed orally active cephalosporin antibiotic. Cefaclor can specifically bind to specific for penicillin-binding protein 3 (PBP3). Cefaclor can be used for the research of depression and kinds of infections caused by bacteria, such as respiratory tract infections, bacterial bronchitis, pharyngitis and skin infections. Dec 19 2024
E7392 1-Benzylimidazole 1-Benzyl-1H-imidazole is a biochemical reagent that can be used as a biological material or organic compound for life science related research. Dec 19 2024
E7168 Ciglitazone Ciglitazone is a potent and selective PPARγ agonist (EC50=3 μM). Ciglitazone inhibits proliferation and differentiation of th17 cells. Ciglitazone is a hypoglycemic agent orally active in the obese-hyperglycemic animal models. Ciglitazone induces apoptosis accompanied by activation of p38 MAPK and nuclear translocation of apoptosis inducing factor (AIF) in opossum kidney (OK) renal epithelial cells. Dec 19 2024
E7393 Pymetrozine Pymetrozine is a feeding inhibitor of Homoptera, in preventing transmission of cauliflower mosaic caulimovirus by the aphid species Myzus persicae (Sulzer). Dec 19 2024
E7169 Lansoprazole sulfone Lansoprazole sulfone (AG-1813) is an orally active and selective inhibitor of H+, K+-ATPase. Lansoprazole sulfone can significantly stimulates gastric acid secretion by inhibiting H+, K+-ATPase. Lansoprazole sulfone has potential applications in duodenal ulcer, gastric ulcer, gastroesophageal reflux disease and Zolinger Ellison disease. Dec 19 2024
E7394 Methotrexate metabolite Methotrexate metabolite (DAMPA) is an active metabolite of Methotrexate. Methotrexate is a Folic acid (HY-16637) antagonist, widely used as an immunosuppressant. Methotrexate metabolite is an antimalarial agent that inhibits parasite growth under physiological folic acid conditions, with IC50 values of 446 nM and 812 nM against folic acid-sensitive strains and highly resistant strains, respectively. Methotrexate metabolite exhibits pharmacokinetic characteristics of rapid clearance and extensive metabolism, with a mean clearance rate of 1.9 l/kg/h and a mean terminal half-life of 51 minutes. Methotrexate metabolite is promising for research in the field of inflammation. Dec 19 2024
E5056 4-Allylcatechol 4-Allylcatechol (4-Allylpyrocatechol) is a xylan isolated from the root of Piper taiwanense. 4-Allylcatechol has a strong inhibitory activity against collagen-induced platelet aggregation (IC50=5.3 μM). In addition, 4-Allylcatechol has anti-tuberculosis activity against Mycobacterium tuberculosis H37Rv (MIC=27.6 μg/mL). Dec 19 2024
E7170 KAT8-IN-1 KAT8-IN-1 is a lysine (K) acetyltransferase 8 (KAT8) inhibitor, with IC50s of 141 μM (KAT8), 221 μM (KAT2B), 106 μM (KAT3B), respectively. KAT8 inhibits histone acetyltransferases (HATs), and could result in disease states, such as cancer or inflammatory diseases. Dec 19 2024
E7395 Salcaprozate sodium Salcaprozate sodium (SNAC), an oral absorption promoter, and has the potential as a delivery agent for oral forms of heparin and insulin. Salcaprozate sodium could increase passive transcellular permeation across small intestinal epithelia based on increased lipophilicity arising from non-covalent macromolecule complexation. Dec 19 2024
E7171 PIK-75 PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 induces apoptosis. Dec 19 2024
E7396 5-Hydroxypyrazine-2-Carboxylic Acid 5-Hydroxypyrazine-2-Carboxylic Acid, a metabolite of anti-tuberculosis drug pyrazinamide (PZA). Dec 19 2024
E7172 6-FAM 6-FAM (6-Carboxyfluorescein) is an isomer of carboxyfluorescein and is mainly used for sequencing and labeling of nucleic acids. Dec 19 2024
E7397 Falcarindiol Falcarindiol, an orally active polyacetylenic oxylipin, activates PPARγ and increases the expression of the cholesterol transporter ABCA1 in cells. Falcarindiol induces apoptosis and autophagy. Falcarindiol has anti-inflammatory, antifungal, anticancer and antidiabetic properties. Falcarindiol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Dec 19 2024
E7173 5-ROX 5-ROX (5-Carboxy-X-rhodamine), a rhodamine dye, exhibits strong fluorescence property in aqueous buffer with the λexit of 580 nm (ε=3.6×104 M-1 cm-1), and λemit of 604 nm (=0.94). Dec 19 2024
E7398 Ezetimibe phenoxy glucuronide Ezetimibe phenoxy glucuronide (Ezetimibe glucuronide) is the active metabolite of Ezetimibe. Antihyperlipoproteinemic activity. Ezetimibe is a potent cholesterol absorption inhibitor. Dec 19 2024
E7174 D-α-Tocopherol Succinate D-α-Tocopherol Succinate (Vitamin E succinate) is an antioxidant tocopherol and a salt form of vitamin E. D-α-Tocopherol Succinate inhibits Cisplatin (HY-17394)-induced cytotoxicity. D-α-Tocopherol Succinate can be used for the research of cancer. Dec 19 2024
E7399 Ajmalicine Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity. Dec 19 2024
E7175 Gramicidin A Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α). Dec 19 2024
E7400 Furafylline Furafylline is a potent and selective inhibitor of human cytochrome P450IA2 with an IC50 of 0.07 μM. Dec 19 2024
E7176 Glucose oxidase Glucose oxidase is used in the food and beverage industry as a preservative and stabilizer and is commonly derived from the fungus Aspergillus niger. Glucose oxidase can react with intracellular glucose and oxygen (O2) to produce hydrogen peroxide (H2O2) and gluconic acid, which can cut off the nutrition source of cancer cells and consequently inhibit their proliferation. Dec 19 2024
E7401 (S)-b-aminoisobutyric acid (S)-b-aminoisobutyric acid is a non-protein amino acid originating from the catabolism of thymine and valine. Dec 19 2024
E7000 Ponatinib hydrochloride Ponatinib hydrochloride (AP24534 hydrochloride) is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively. Dec 19 2024
E7402 Ac-IETD-AFC Ac-IETD-AFC is a fluorogenic substrate of caspase-8, caspase-3, caspase-10, and granzyme B. Dec 19 2024
E7177 5(6)-TAMRA 5(6)-TAMRA is a fluorescent dye molecule widely used as a label for peptides and proteins. Dec 19 2024
E7403 Ac-LEHD-AFC Ac-LEHD-AFC is a fluorescent substrate for caspase-9, can be used to assess the activity of caspase. Dec 19 2024
E7178 Polystyrene Polystyrene can form Polystyrene microplastics (PS-MPs), a hazardous material with potential toxicity. Polystyrene microplastics is harm to zebrafish heart and induces male reproductive toxicity in mice. MCE provides Polystyrene products in solution packaging. Dec 19 2024
E5557 Noreugenin Noreugenin, 5,7-dihydroxy-2-methyl-4H-chromen-4-one, is a new chromone from Aloe arborescens. (Amaryllidaceae). Dec 19 2024
E7179 n-Octyl β-D-glucopyranoside n-Octyl-β-d-glucopyranoside is a non-ionic detergent, it can be widely used in the research of biotechnical, biochemical applications, solubilization and crystallization of membrane proteins. n-Octyl-β-d-glucopyranoside can completely inhibit cavitation-induced cell lysis in vitro. Dec 19 2024
E7404 N-dodecanoyl-L-Homoserine lactone N-dodecanoyl-L-Homoserine lactone (C12-HSL) is a quorum sensing (QS) signaling molecule. N-dodecanoyl-L-Homoserine lactone (C12-HSL) aptamers blocks qurom sensing and inhibits biofilm formation in Pseudomonas aeruginosa. Dec 19 2024
E7180 Ponceau 4R Ponceau 4R is a synthetic colorant that can be used for food coloring. Ponceau 4R is a strawberry red azo dye that can be used in a variety of foods, usually synthesized from aromatic hydrocarbons, and is stable to light, heat, and acids. Dec 19 2024
E7405 TMB TMB is a non-toxic, non-mutagenic, colorless dye that is also used as a chromogenic agent in enzyme detection systems based on horseradish peroxidase (HRP). TMB can function as a photoacoustic probe for reactive oxygen and nitrogen species (ROS/RNS), reacting with hypochlorite, hydrogen peroxide, singlet oxygen, and nitrogen dioxide to produce blue oxidation products. TMB can detect the singlet oxygen produced by the outer membrane of Escherichia coli ATCC 25922. Dec 19 2024
E7181 Myelin Basic Protein Myelin Basic Protein (MHP4-14), a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM). Myelin Basic Protein is not phosphorylated by cyclic AMP-dependent protein kinase, casein kinases I and II, Ca2+/calmodulin-dependent protein kinase II, or phosphorylase kinase, and can be routinely used for the assay of protein kinase C with low background in the crude tissue extracts. Dec 19 2024
E7406 Tulobuterol Tulobuterol (C-78 free base) is a long-acting β2-adrenoceptor agonist, which reduces the frequency of exacerbations of chronic obstructive pulmonary disease and bronchial asthma. Tulobuterol is also a sympathomimetic agent used as a transdermal patch, and increases normal diaphragm muscle strength. Dec 19 2024
E7182 Dehydroepiandrosterone sulfate sodium salt Dehydroepiandrosterone sulfate sodium salt (DHEAS) is the most abundant circulating steroid in human. Dehydroepiandrosterone sulfate sodium salt (DHEAS) affects steroid hormone biosynthesis on a molecular level resulting in an increased formation of pregnenolone. Dec 19 2024
E7407 Adrenomedullin (AM) (22-52), human Adrenomedullin (AM) (22-52), human, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist, and also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat. Dec 19 2024
E7183 N-Nitrosodibutylamine N-Nitrosodibutylamine (N-Nitroso-di-n-butylamine) is a nitrosamine enriched in the drinking water. Dec 19 2024
E7184 NBD-Cl NBD-Cl is a nonfluorescent reagent which becomes highly fluorescent after reaction with thiol or amino groups. Dec 19 2024
E7185 5(6)-ROX 5(6)-ROX is a nucleic acid fluorescent label which can be used as a reference dye for real-time polymerase chain reaction. Dec 19 2024
E7408 Sodium laureth sulfate Sodium laureth sulfate (Sodium lauryl polyoxyethylene ether sulfate) is an anionic active agent with excellent decontamination, emulsification, dispersion, wetting, antifungal and other properties. Dec 19 2024
E7186 Sacubitril Sacubitril (AHU-377) is a potent and orally active NEP (neprilysin) inhibitor with an IC50 of 5 nM. Sacubitril is a component of the heart failure medicine LCZ696. Sacubitril can be used for the research of heart failure, hypertension and COVID-19. Dec 19 2024
E7409 Dimethyl biphenyl-4,4'-dicarboxylate Dimethyl biphenyl-4,4'-dicarboxylate (Biphenyl dimethyl dicarboxylate) is a hepatoprotectant obtained from Schizandra fructus and may induce a signal transduction similar to that associated with IFN. Dec 19 2024
E5742 Marein Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC50 of 100 µM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects. Dec 19 2024
E7187 Hydroxyphenyllactic acid Hydroxyphenyllactic acid is an antifungal metabolite. Dec 19 2024
E7410 Boc-L-Ala-OH Boc-L-Ala-OH (Boc-Ala-OH) shows excellent affinity with ATP. Boc-L-Ala-OH contains an amino acid moiety, and an acylamide bond like that of the peptide and protein. Dec 19 2024
E7188 c-di-AMP c-di-AMP (Cyclic diadenylate) is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP (Cyclic diadenylate) is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP (Cyclic diadenylate) acts as a potent mucosal adjuvant stimulating both humoral and cellular responses. Dec 19 2024
E7411 Boc-L-Leu-OH Boc-L-Leu-OH is a leucine derivative. Dec 19 2024
E7189 EGNHS EGNHS is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs. Dec 19 2024
E7412 Thermolysin, Bacillus thermoproteolyticus rokko Thermolysin, Bacillus thermoproteolyticus rokko (EC 3.4.24.27) (TML) is a thermostable neutral metalloproteinase enzyme secreted by the Gram-positive bacteria Bacillus thermoproteolyticus. Thermolysin catalyzes the hydrolysis of peptide bonds containing hydrophobic residues.Optimal pH: 8.0. Considerably stable from pH 5 to 9.5. Optimal temperature : 70 °C Dec 19 2024
E5782 Remodelin Remodelin is a potential inhibitor of the acetyltransferase NAT10. It enhances nuclear shape and cellular fitness in both progeric cells and cells depleted of Lamin A/C by inhibiting NAT10. Remodelin exhibits anti-proliferation activity and significantly inhibits tumour growth and tumour cell proliferation in the PDX model of HNSCC. Dec 19 2024
E7190 SHU 9119 SHU 9119 is a potent human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist; with IC50 values of 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively. Dec 19 2024
E7413 Reactive Blue 4 Reactive Blue 4 is an anthraquinone dye, as a single colorimetric chemosensor for sequential determination of multiple analytes with different optical responses in aqueous media. Reactive Blue 4 is phytotoxic, cytotoxic and genotoxic. Reactive Blue 4 . Dec 19 2024
E7191 Ditolylguanidine Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor) with Ki values of 69 and 21 nM for σ1 and σ2 receptors, respectively. Ditolylguanidine effectively inhibits the growth of small cell lung cancer cells. Ditolylguanidine can be used for the research of lung cancer. Dec 19 2024
E7414 MG-115 MG-115 is a potent and reversible proteasome inhibitor, with Kis of 21 nM and 35 nM for 20S and 26S proteasome, respectively. MG-115 specifically inhibit the chymotrypsin-like activity of the proteasome, induces p53-dependent apoptosis. Dec 19 2024
E7192 Endothelin-3, human, mouse, rabbit, rat Endothelin-3, human, mouse, rabbit, rat is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB. Dec 19 2024
E1254 L-AP4 L-AP4 (L-APB) is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively. Dec 19 2024
E7193 Win 18446 Win 18446 is an orally active testes-specific enzyme ALDH1a2 inhibitor, with an IC50 of 0.3 μM. Win 18446 reversibly inhibits spermatogenesis in many species and inhibits Retinoic acid (HY-14649) biosynthesis from Retinol (HY-B1342) within the testes. Dec 19 2024
E5709 Karanjin Karanjin is an orally active furanoflavonoid which can be isolated from several Leguminosae. Karanjin exhibits evident anti-diabetic, anti-cancer, anti-inflammatory, antioxidant, anticolitis, anti-ulcer, anti-Alzheimer properties and multiple insect repellent/insecticidal, acaricide properties, suggesting the potential of Karanjin to be applied to relevant research. Dec 19 2024
E7194 Peroxidase, Horseradish Peroxidase, Horseradish actively involves in oxidizing reactive oxygen species, innate immunity, hormone biosynthesis and pathogenesis of several diseases. Dec 19 2024
E7415 Dimethoate Dimethoate is an effective systemic insecticide for use on plants, has shown promise as a chemotherapeutic agent for control of cattle grubs and certain other insect pests of farm animals, and has high contact toxicity to house-flies and many other insects. Dec 19 2024
E7195 N-Acetyl-D-cysteine N-Acetyl-D-cysteine has antioxidant activities and scavenges ROS through the reaction with its thiol group, but cannot enter the glutathione metabolic pathway. Dec 19 2024
E7416 α-Amyrin α-Amyrin is a pentacyclic triterpenoid compound with oral activity. α-Amyrin activates the ERK and GSK-3β signaling pathways. α-Amyrin can be used in the study of metabolic syndrome induced by high fructose diet and cognitive dysfunction caused by low cholinergic neurotransmission. Dec 19 2024
E7196 Reverse T3 Reverse T3 is a thyroid hormone that can be generated by deiodination of the prohormone thyroxine. Reverse T3 inhibits the increase of sodium current generated by other thyroid hormone analogs in neonatal rat myocytes. Dec 19 2024
E7417 Ligandrol Ligandrol (LGD-4033) is a novel nonsteroidal, oral SARM that binds to androgen receptor with high affinity (Ki of 1 nM) and selectivity. Dec 19 2024
E5022 1-Caffeoylquinic acid 1-Caffeoylquinic acid is an effective NF-κB inhibitor, shows significant binding affinity to the RH domain of p105 with Ki of 0.002 μM and binding energy of 1.50 Kcal/mol. 1-Caffeoylquinic acid has anti-oxidative stress ability. 1-Caffeoylquinic acid inhibits PD-1/PD-L1 interact. Dec 19 2024
E7419 Neuromedin B Neuromedin B (NMB) is a member of Bombesin (BN)-like peptide family in mammals. Dec 19 2024
E7197 Docetaxal Docetaxal (10-Acetyl docetaxel) is an analog of Docetaxel (HY-B0011), with anticancer activity. Docetaxel is a microtubule disassembly inhibitor, with antimitotic activity. Dec 19 2024
E7420 Limaprost Limaprost (OP1206) is a PGE1 analogue and a potent and orally active vasodilator. Limaprost increases blood flow and inhibits platelet aggregation. Limaprost pain relief, has antianginal effects, and can be used for ischaemic symptoms research. Dec 19 2024
E7198 Cyclosporin H Cyclosporin H is a selective and potent inhibitor of FPR-1 (formyl peptide receptor 1). Cyclosporin H, a viral transduction enhancer, increases lentiviral transduction up to 10-fold in human cord blood-derived hematopoietic stem and progenitor cells (HSPCs). Cyclosporin H displays an additive effect when combined with Rapamycin (HY-10219) or Prostaglandin E2 (HY-101952). Cyclosporin H lacks immunosuppressant activity of Cyclosporin A. Dec 19 2024
E7421 Diisopropyl phthalate Diisopropyl phthalate (DiPP) is a phthalate diester. Phthalate esters can be widely used as the polymeric additives to increase plastic flexibility in industrial application. Dec 19 2024
E7199 Transferrins Transferrin, a blood-plasma glycoprotein, is a target ligand for transferrin receptor. Transferrins can bind to and mediate the transport of iron. Dec 19 2024
E7422 2-Amino-3-(2-chlorophenyl)propanoic acid 2-Amino-3-(2-chlorophenyl)propanoic acid is a phenylalanine derivative. Dec 19 2024
E7001 Pilocarpine Pilocarpine is a selective M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist. Dec 19 2024
E7200 Ceramides Mixture Ceramides Mixture is an endogenous ceramide and consists of hydroxy and non-hydroxy fatty acid-containing ceramides. Ceramides Mixture is a main lipid component of the permeability barrier in epidermis. Ceramides Mixture is involved in the regulation of growth inhibition, cell cycle arrest, and modulation of telomerase activity. Dec 19 2024
E7423 Cetrorelix Acetate Cetrorelix Acetate (SB-75 acetate) is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM. Dec 19 2024
E4968 Oseltamivir Oseltamivir (GS 4104) is an orally active influenza virus neuraminidase inhibitor (NAI). Oseltamivir inhibits influenza A/H3N2, A/H1N2, A/H1N1, and B viruses with mean IC50s of 0.67, 0.9, 1.34 and 13 nM, respectively. Dec 19 2024
E7201 Ceftriaxone Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis. Dec 19 2024
E7424 T-2 Toxin 0 Dec 19 2024
E5685 Carboxyatractyloside tripotassium Carboxyatractyloside (Gummiferin) tripotassium is a toxic natural product, acts as an inhibitor of ADP/ATP carrier, inhibits mitochondrial ADP/ATP transport from the inner mitochondria to the inner mitochondria. Carboxyatractyloside tripotassium can be used for the study of cellular energy metabolism and mitochondrial biology. Dec 19 2024
E7425 Alagebrium chloride Alagebrium chloride (ALT711) is an advanced glycation end product (AGE) inhibitor. Dec 19 2024
E7002 Uric acid sodium Uric acid sodium (Monosodium urate), scavenger of oxygen radical, is a very important antioxidant that help maintains the stability of blood pressure and antioxidant stress. Uric acid sodium can remove reactive oxygen species (ROS) such as singlet oxygen and peroxynitrite, inhibiting lipid peroxidation. Dec 19 2024
E7202 5-FAM 5-FAM (5-Carboxyfluorescein) is a green fluorescent reagent used for in situ labeling peptides, proteins and nucleotides. 5-FAM is a single isomer with Ex/Em of 490 nm/520 nm. Dec 19 2024
E7426 Nitromide Nitromide is an anti-parasitic agent. Dec 19 2024
E7003 Vosilasarm Vosilasarm (RAD140) is a potent, orally active, nonsteroidal selective androgen receptor modulator (SARM) with a Ki of 7 nM. Vosilasarm shows good selectivity over other steroid hormone nuclear receptors. Dec 19 2024
E7203 Cross-linked dextran G 50 Cross-linked dextran G 50 is a gel filtration medium. Cross-linked dextran G 50 can be used in gel permeation chromatography for fractionation of the glycopeptide mixture (Sphere protein separation range: 1.5K-30K Da; Polysaccharide separation range: 500-10K Da). Dec 19 2024
E7427 Dehydroaripiprazole Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole. Dec 19 2024
E7004 Vonoprazan Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H+,K+-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan can be used for eradication of Helicobacter pylori. Dec 19 2024
E7204 Faropenem Faropenem is a potent and orally active beta-lactam antibiotic. Faropenem demonstrates broad-spectrum in vitro antimicrobial activity against many gram-positive and -negative aerobes and anaerobes. Faropenem is resistant to hydrolysis by nearly all beta-lactamases, including extended-spectrum beta-lactamases and AmpC beta-lactamases. Faropenem is developed as an oral proagent, faropenem medoxomil, for the research of respiratory tract infections. Dec 19 2024
E5523 (5R,6E)-5-Hydroxy-1,7-diphenyl-6-hepten-3-one (5R,6E)-5-Hydroxy-1,7-diphenyl-6-hepten-3-one is the methylene chloride extract of Alpinia nutans, has antioxidant activity. Dec 19 2024
E4848 Toremifene Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively. Dec 19 2024
E7205 6-TAMRA 6-TAMRA has been a widely used fluorophore for preparing bioconjugates, especially fluorescent antibody and avidin derivatives used in immunochemistry. Dec 19 2024
E7428 Chromomycin A3 Chromomycin A3 is an aureolic acid-type antitumor antibiotic. Chromomycin A3 forms dimeric complexes with divalent cations, such as Mg2+, which strongly binds to the GC rich sequence of DNA to inhibit DNA replication and transcription. Chromomycin A3 has a variety of utilities as a staining agent for human sperm chromatin, autophagy inducing agent, and apoptosis inhibitor. Dec 19 2024
E7005 Umifenovir Umifenovir is a potent, orally active broad-spectrum antiviral agent with activity against a number of enveloped and non-enveloped viruses. Umifenovir is used as an anti-influenza virus agent. Umifenovir could effectively inhibit the fusion of virus with host cells. Umifenovir is an efficient inhibitor of SARS-CoV-2 in vitro. Umifenovir shows anti-inflammatory activity. Dec 19 2024
E7206 Norvancomycin hydrochloride Norvancomycin hydrochloride is suitable for endocarditis, osteomyelitis, pneumonia, sepsis or soft tissue infections caused by Staphylococcus aureus (including methicillin-resistant strains and multi-drug-resistant strains). Dec 19 2024
E7429 (R,S)-Anatabine (R,S)-Anatabine is a a minor tobacco alkaloid found in the Solanaceae family of plants that can be used as a specific marker for the detection of tobacco use. Dec 19 2024
E7006 Taurocholic acid Taurocholic acid (N-Choloyltaurine) has marked bioactive effects such as an inhibitory potential against hepatic artery ligation induced biliary damage by upregulation of VEGF-A expression. Taurocholic acid has immunoregulation effect. Dec 19 2024
E7207 5(6)-Aminofluorescein 5(6)-Aminofluorescein (5(6)-AFM) is a a precursor for synthesis of 5(6)-FITC (HY-15941). 5(6)-FITC is an amine-reactive derivative of fluorescein dye. Dec 19 2024
E7430 Hydroxyethyl cellulose Hydroxyethyl cellulose is a non-ionic, modified cellulose polymer used as a thickening agent for aqueous cosmetic and personal care formulations. Dec 19 2024
E7208 Saclofen Saclofen is an orally available competitive GABAB receptor antagonist with an IC50 of 7.8 μM, but it has a weaker antagonistic effect on GABAB1b and GABAB2 heterodimer recombinant receptors. Saclofen can inhibit the binding of baclofen (HY-B007) to rat cerebellar membranes and block the phase shifts in circadian rhythms caused by baclofen. Saclofen has also shown anti-inflammatory and analgesic effects in rats. Dec 19 2024
E7431 LEP(116-130)(mouse) LEP(116-130)(mouse) is a synthetic leptin peptide fragment. Dec 19 2024
E7007 Suc-Leu-Leu-Val-Tyr-AMC Suc-Leu-Leu-Val-Tyr-AMC is a fluorogenic substrate. Dec 19 2024
E7209 N6-(2-Hydroxyethyl)adenosine N6-(2-Hydroxyethyl)adenosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc. Dec 19 2024
E7432 Monoethyl fumarate Monoethyl fumarate is the monoethyl ester form of fumaric acid. Monoethyl fumarate is a kind of effective preservative and polymerization agent for macromolecular material. Dec 19 2024
E7008 ONPG ONPG is a colorimetric and spectrophotometric substrate for detection of β-galactosidase activity. Dec 19 2024
E7210 Enzalutamide carboxylic acid Enzalutamide carboxylic acid (MDV3100 carboxylic acid) is an inactive metabolite of Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist. Dec 19 2024
E7433 C-Phycocyanin C-phycocyanin (C-PC) is a protein pigment which is also widely used as an excellent nutrient supplement for human beings. Dec 19 2024
E5779 4-Azido-L-phenylalanine 4-Azido-L-phenylalanine is an unnatural amino acid, which is used as an effective vibrational reporter of local protein environments. 4-Azido-L-phenylalanine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. Dec 19 2024
E7211 Phosphatidylcholines,soya Phosphatidylcholines,soya is a phosphatidylcholine from soybean used in the preparation of liposomes. Phosphatidylcholines,soya can be used as a vehicle in animal agent administration. Dec 19 2024
E4908 Clemizole hydrochloride Clemizole hydrochloride is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. Clemizole hydrochloride is an inhibitor of TRPC5 channel. The IC50 of Clemizole hydrochloride for RNA binding by NS4B is 24 nM, whereas its EC50 for viral replication is 8 μM. Dec 19 2024
E7009 D-Glucose-13C6 D-Glucose-13C6 is a stable isotope-labeled counterpart of D-glucose (HY-B0389). D-Glucose-13C6 can be used as a metabolic tracer to trace glucose-related synthetic catabolism or as synthesis ingredient, minimal media reagent, and internal standard. Dec 19 2024
E7212 7-Desmethyl-agomelatine 7-Desmethyl-agomelatine is a metabolite of Agomelatine. Agomelatineis a potent agonist at melatonin receptors (MT1 and MT2), and also is an antagonist of 5-HT2C. Dec 19 2024
E7434 Illudin S Illudin S, a cytotoxic Illudin, is a natural sesquiterpene with strong anti-tumour and antiviral activities. Illudin S has genotoxic activities. Illudin S blocks the G1-S phase interface of the cell cycle in human leukemia cells. Dec 19 2024
S7468 SR 11302 SR 11302 is an activator protein-1 (AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibits AP-1 activity without activating the transcription of retinoic acid response element (RARE). Dec 19 2024
E7213 TAPI-1 TAPI-1 is a TACE (ADAM17) inhibitor and blocks the shedding of several cell surface proteins. TAPI-1 is also a metalloproteinase (MMP) inhibitor. Dec 19 2024
E7435 Galactose Oxidase, Dactylium dendroides Galactose Oxidase, Dactylium dendroides (GOase) from fungus is often used in biochemical studies. Galactose oxidase is a type II copper metalloenzyme, and it containing a single polypeptide. Galactose oxidase catalyzes two-electron oxidation of primary alcohols to their corresponding aldehydes, coupling with the reduction of dioxygen to hydrogen peroxide. Dec 19 2024
E4737 Potrasertib Potrasertib (IMP7068, WEE1-IN-10) is a potent and selective inhibitor of WEE1 Kinase. It displays antitumor activity and is well-tolerated in patients with advanced solid tumors. Dec 18 2024
S8593 VX-984 VX-984 (M9831) is an orally active, potent, selective, and ATP-competitive inhibitor of DNA-PK. VX-984 effectively suppresses non-homologous end joining (NHEJ) and increases DNA double-strand breaks (DSBs). It enhances the cytotoxic effects of ionizing radiation (IR) in various cancer cell lines, including non-small cell lung cancer (NSCLC) cell lines, in vitro. Additionally, VX-984 reduces DNA-PKcs autophosphorylation. Dec 18 2024
E1462 P62-mediated mitophagy inducer P62-mediated mitophagy inducer (PMI) is a P62-mediated activator of mitophagy that functions independently of parkin recruitment or mitochondrial membrane potential (ΔΨm) collapse. It remains effective even in cells lacking a fully functional PINK1/Parkin pathway. PMI stabilizes Nrf2 and enhances p62 expression, thereby activating mitophagy. Dec 18 2024
E6024 Selumetinib sulfate Selumetinib sulfate (AZD6244 sulfate, ARRY-142886 sulfate) is an oral, non-ATP-competitive inhibitor of MEK1/2, with an IC50 of 14 nmol/L against purified MEK1. It exhibits an anti-tumor effect in the HT-29 xenograft model and is used to treat cancer and inflammation. Dec 18 2024
E4781 OPN expression inhibitor 1 Dec 16 2024
E1974 MS8709 MS8709 (EX-A11295) is a first-in-class G9a/GLP proteolysis targeting chimera (PROTAC) degrader, that induces G9a/GLP degradation in a concentration, time, and ubiquitin-proteasome system (UPS)-dependent manner, and does not alter the mRNA expression of G9a/GLP over other methyltransferases. It displays superior cell growth inhibition in prostate, leukemia, and lung cancer cells over parent G9a/GLP inhibitors. Dec 16 2024
E4771 Aprocitentan Aprocitentan (ACT-132577) is a pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual antagonist of ETA/ETB with IC50 values of 3.4 nM and 987 nM, and pA2 values of 6.7 and 5.5, respectively. Dec 16 2024
E1984 JBJ-09-063 hydrochloride JBJ-09-063 hydrochloride is a mutant-selective allosteric inhibitor of EGFR with IC50 values of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S, respectively. JBJ-09-063 hydrochloride significantly inhibits the phosphorylation of EGFR, Akt, and ERK1/2. Dec 16 2024
E1863 Inixaciclib Inixaciclib (NUV-422) is a potent inhibitor of CDK2, CDK4, and CDK6. It inhibits the growth of glioma cell lines in vitro and exhibits antitumor activity in GB xenograft models, PDX models of HR+ HER2- metastatic breast cancer resistant to CDK4/6 inhibitors and prostate cancer resistant to anti-androgens. Dec 12 2024
E1941 ACT-1016-0707 ACT-1016-0707 (LPA1 receptor antagonist 2) is an orally active and selective antagonist of LPA1 Receptor, with IC50 of 3.1 nM for hLPAR1 in tango assay. It has the potential to treat fibrotic diseases. Dec 12 2024
E4738 LYMTAC-2 LYMTAC-2 is a lysosomal-targeting chimera (LYMTAC) designed to degrade membrane-associated proteins by leveraging lysosomal membrane proteins (LMPs) like RNF152, LAPTM4a, and LAPTM5. It forms a ternary complex with its target protein, such as KRASG12D, and facilitates relocalization to the lysosome, leading to ubiquitin-dependent degradation. It has the potential to study membrane protein regulation and develop strategies to overcome resistance in KRAS-driven signaling pathways. Dec 12 2024
E4612 iCARM1 iCARM1 (CARM1-IN-6) is a potent and selective inhibitor of protein arginine methyltransferase CARM1 (PRMT4) with an IC50 of 12.3 μM. It potently suppresses breast cancer cell growth both in vitro and in vivo and can be used in cancer research. Dec 12 2024
E6011 Agomelatine hydrochloride Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. It is also a selective antagonist of 5-HT2C receptors with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively. Blockade of these receptors enhances adrenergic and dopaminergic transmission in the frontocortical regions. Dec 12 2024
E1921 NRL-1049 NRL-1049(BA 1049) is a small molecule selective inhibitor of ROCK2 with an IC50 of 0.59 µM. It exhibits potent efficacy in preserving the blood-brain barrier (BBB) and suppresses seizures after brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice. Dec 12 2024
E4782 17-OH PREG (17a-Hydroxypregnenolone) 17-OH PREG (17a-Hydroxypregnenolone) is a pregnenolone metabolite and DHEA precursor. It is formed through CYP17A1 hydroxylase and 17,20-lyase activities. It is the most relevant steroid for the study of elevated plasma levels linked to type II 3β-hydroxysteroid dehydrogenase deficiency. Dec 12 2024
E5775 Exatecan Exatecan (DX-8951), is a water-soluble derivative of camptothecin. It acts as an inhibitor of DNA topoisomerase I with an IC50 value of 1.906 μM. It demonstrates potent antitumor effects and triggers apoptotic cell death after treatment in human pancreatic cancer cells. Dec 11 2024
E4997 BAY 2927088（Sevabertinib） BAY 2927088（Sevabertinib) is the first non-covalent, potent, oral, selective, and reversible inhibitor of tyrosine kinase that potently inhibits mutant HER2 and mutant EGFR in preclinical models. It targets Exon 20 insertions in non-small-cell lung carcinoma (NSCLC) patients. Dec 11 2024
E5777 Tris(benzyltriazolylmethyl)amine Tris(benzyltriazolylmethyl)amine (TBTA) is a ligand used as a biochemical tool for labeling proteins and enzymes. It dramatically enhances the Copper(II) acetate (Cu(OAc)2)-accelerated azide-alkyne cycloaddition (AAC) reactions involving nonchelating azides. Dec 11 2024
E5767 Ovalbumins Ovalbumin is a major glycoprotein found in egg whites, serving as a nutrient reserve for developing embryos and used in the food industry. It also induces a Th2 immune response in sensitized individuals, characterized by the production of cytokines like IL-4, IL-5, and IL-13, leading to airway inflammation, hyper-responsiveness (AHR), and immune cell infiltration, key features in asthma models. Dec 11 2024
P1246 ODN 1826 sodium ODN 1826 sodium (CpG 1826 sodium) is a synthetic CpG oligodeoxynucleotide and agonist of TLR9 signaling pathway, that induces G1-phase arrest and apoptosis in A20 lymphoma cells while stimulating NO and iNOS production in mouse models, as part of its immunostimulatory activity. Dec 11 2024
S9740 U0126 U0126 is a highly potent and selective inhibitor of the dual-specificity kinases MEK1 and MEK2, with IC50 values of 72 nM and 58 nM, respectively. It also acts as a strong antioxidant, protecting cells from oxidative stress-induced cell death. Dec 05 2024
E4702 SRX3177 SRX3177 is a potent triple inhibitor targeting CDK4/6, PI3K, and BRD4, with IC50 values of 33 nM for BRD4 BD1, 89 nM for BRD4 BD2, 79 nM for PI3Kα, 83 nM for PI3Kδ, 3.18 μM for PI3Kγ, <2.5 nM for CDK4, and 3.3 nM for CDK6. By simultaneously inhibiting these key pathways, SRX3177 disrupts cancer cell signalling and exhibits significant cytotoxic effects in tumors. Dec 05 2024
E4621 BHPI BHPI is a potent noncompetitive inhibitor of estrogen receptor α (ERα), which disrupts the protective estrogen–ERα-mediated activation of the unfolded protein response (UPR), leading to sustained UPR activation. It specifically inhibits the growth of drug-resistant ERα-positive breast and ovarian cancer cells and induces significant tumor regression in a mouse xenograft model of breast cancer. Dec 05 2024
E4785 BAP1-IN-1 BAP1-IN-1 is a small-molecule inhibitor of BRCA1 associated protein 1 (BAP1) catalytic activity in vitro with an IC50 of 0.1-1 μM. It exhibits a potential therapeutic target for leukemia. Dec 05 2024
E1939 ART899 ART899, a derivative of ART558 is a potent, specific allosteric inhibitor of DNA polymerase theta (Polθ), specifically inhibits Polθ MMEJ activity with IC50 of 180 nM. It specifically radiosensitizes tumor cells and have a potent stand-alone antitumor effect in cancer cells. Dec 05 2024
E4774 4-DAMP 4-DAMP (4-diphenyl-acetoxy-N-methyl-piperidine) (4-DAMP methiodide) is a selective antagonist of M3 type muscarinic acetylcholine receptors (M3-mAChR) with a pKi of 9.3. It also has a high affinity for the closely-related M5 receptor with a pKi of 8.9. It is routinely used to study the regulation and functions of the M3 receptor. Dec 05 2024
E4732 FDW028 FDW028 is a highly potent and selective inhibitor of FUT8. FDW028 demonstrates strong anti-tumor effects by promoting defucosylation and inducing lysosomal degradation of B7-H3 via the chaperone-mediated autophagy (CMA) pathway. Additionally, FDW028 suppresses the AKT/mTOR signaling pathway. FDW028 exhibits potent anti-Metastatic colorectal cancer (mCRC) activities. Dec 02 2024
E4880 Labetalol Labetalol (AH5158, Sch-15719W free base) is an orally active and selective competitive antagonist of α1-adrenergic receptors and non-selective β-adrenergic receptors. Labetalol, an anti-hypertensive agent is used in the research of cardiovascular diseases. Dec 02 2024
E1896 BMS-502 BMS-502 is a potent dual inhibitor of diacylglycerol kinase (DGK) α and ζ with IC50 values of 4.6 nM and 2.1 nM, respectively. BMS-502 also exhibits an EC50 value of 340 nM in the mouse cytotoxic T cell IFN-γ assay (mCTC). BMS-502 can be used in tumor immunity-related research. Dec 02 2024
E6005 Saxagliptin hydrochloride Saxagliptin hydrochloride (BMS-477118 hydrochloride) is a potent, selective, reversible, competitive, and orally active inhibitor of dipeptidyl peptidase-4 (DPP-4). It exhibits 400-950 fold selective inhibition of DPP-4 than DPP-8. Saxagliptin hydrochloride is used in the research of type 2 diabetes mellitus research. Dec 02 2024
E1664 GNE-987 GNE-987 is a BRD4-degradating PROTAC consisting of BRD4B1 and BRD4B2 (BRD4 bromodomains 1 and 2) and the VHL E3-ubiquitin ligase. It exhibits BRD4 degradation activity with DC50 of 0.03 nM for the EOL-1 AML cell line. GNE-987 inhibits cell proliferation and induces apoptosis by promoting the rapid and sustained degradation of BRD4 and inhibiting its downstream targets. It also demonstrates potent antitumor activity in AML cell lines. Dec 02 2024
E6006 Deferasirox (Fe3+ chelate) Deferasirox (Fe3+ chelate) (Exjade) is an oral tridentate iron chelator used for reducing transfusional chronic iron overload. It exhibits efficacy in iron-overloaded patients with anemias, thalassemia, sickle cell disease and myelodysplastic syndromes. It is also an orally effective antitumor agent against solid tumors. Nov 29 2024
E4884 Icotinib Hydrochloride Icotinib hydrochloride (BPI-2009H) is a highly potent and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 5 nM, utilized in the treatment of non-small cell lung cancer (NSCLC). Nov 29 2024
E5768 Indolelactic acid Indolelactic acid (Indole-3-lactic acid), a metabolite of tryptophan (Trp), plays a role in immune cell differentiation and cytokine production by activating aryl hydrocarbon receptors (AhR). This regulation supports immune responses and aids in anti-inflammatory and anti-allergic activities. It also plays an important role in the balance of Th17/Treg cells by reprogramming CD4+ Th cells into CD4+CD8+ Treg cells and inhibiting the polarization of Th17 cells. Nov 29 2024
A2167 Anti-mouse CD3-InVivo Anti-mouse CD3-InVivo reacts with mouse CD3, a transmembrane cell-surface protein that belongs to the immunoglobulin superfamily.CD3 is expressed on T lymphocytes, NK-T cells, and to varying degrees on developing thymocytes. Nov 29 2024
E1814 Resigratinib Resigratinib (KIN-3248) is a potent, kinome selective, irreversible, orally bioavailable, small-molecule inhibitor of pan-FGFR. It exhibits dose-dependent tumor inhibition in FGFR driven cholangiocarcinoma, gastric, and bladder cancer xenograft models. Nov 27 2024
E4792 Atorvastatin calcium hydrate Atorvastatin calcium hydrate (Totalip) is a potent inhibitor of the HMG-CoA reductase . It is used as a potent hypolipidemic agent to reduce the elevated total-cholesterol, low-density lipoprotein (LDL), apolipoprotein B (apo B), and triglyceride (TG) levels, and to increase the high-density lipoprotein cholesterol (HDL-C) level in patients with primary hypercholesterolemia and mixed dyslipidemia. Nov 27 2024
E4994 JNJ-75276617 JNJ-75276617 (Bleximenib, Menin-MLL inhibitor 24) is an orally bioavailable, potent inhibitor of menin targeting the menin-KMT2A selective protein-protein interaction. It also acts as an inhibitor of menin-mixed-lineage leukemia 1 (menin-MLL). JNJ-75276617 displays highly potent antiproliferative activity across several acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) cell lines and patient samples. Nov 25 2024
E4800 BML-284 BML-284 (Wnt Agonist) is a potent and cell-permeable activator of Wnt signaling that induces TCF-dependent transcriptional activity with an EC50 value of 0.7 µM. BML-284 also acts as an agonist of β-catenin that effectively activates direct Wnt-β-catenin signaling to induce adipocyte dedifferentiation while circumventing the apoptotic effect in the hypertonic treatment. Nov 25 2024
E4719 XYL-1 XYL-1 is a highly potent inhibitor of PARP7 with and IC50 of 0.6 nM. It could enhance the type-Ⅰinterferon signaling in vitro, and can be a potential candidate for developing cancer immunotherapy agents. Nov 25 2024
E4637 PK 11195 PK 11195 (RP 52028) is a translocator protein (TSPO) ligand, a potent and selective antagonist of peripheral benzodiazepine receptorwith high affinity Ki of 3.1 nM in cerebellum and 4.1 nM in spinal cord. It is also an antagonist of human constitutive androstane receptor (hCAR), and human pregnane X receptor (PXR). It displaces [3H] RO5-4864 from its binding sites across organs and also targets Leishmania in chemotherapy. Nov 25 2024
E4793 Bucladesine calcium Bucladesine calcium (Dibutyryl-cAMP Calcium Salt, DBcAMP calcium salt) is a cell-permeable analog of cyclic AMP. It serves as a potent activator of protein kinase A (PKA) and mimics the effects of endogenous cAMP. It also inhibits phosphodiesterase (PDE) activity, with the potential to treat congestive heart failure, wound healing, and inflammation. Nov 25 2024
E4681 PF-07799933 PF-07799933 (Claturafenib, ARRY-440) is a brain-penetrant, selective, pan-mutant inhibitor of BRAF. It exhibits broad inhibition of pERK levels in HT29 cells with an IC50 value of 1.6 nM. PF-07799933 treatment displays antitumor activity against BRAFV600- and non-V600-mutant cancers preclinically and in treatment-refractory patients. Nov 24 2024
E6015 Heparin (Lithium salt) Heparin Lithium salt is an anticoagulant that binds reversibly to antithrombin III (ATIII). Heparin Lithium salt is used as an anticoagulant for laboratory studies and in direct membrane-feeding assays. Nov 24 2024
E6009 Esomeprazole Esomeprazole ((S)-Omeprazole, (-)-Omeprazole) is a potent inhibitor of proton pump. It decreases acid production by inhibiting the H+, K+-ATPase enzyme in gastric parietal cells. Esomeprazole displays pharmacokinetic properties that make it more effective than omeprazole and has the potential for use in research of symptomatic gastroesophageal reflux disease. Nov 24 2024
E6013 Sivelestat sodium Sivelestat sodium (ONO-5046, Sodium sivelestat, LY544349 sodium) is a potent, specific, and intravenously active inhibitor of neutrophil elastase with an IC50 value of 44 nm. It is a useful agent for studying the roles of neutrophil elastase in animal disease models such as emphysema, adult respiratory distress syndrome, septic shock and disseminated intravascular coagulation in COVID-19. Nov 21 2024
E1628 BMS-911172 BMS-911172 is a brain penetrant, selective inhibitor of adaptor protein 2-associated kinase 1 (AAK1) with an IC50 value of 12 nM. BMS-911172 inhibits μ2 phosphorylation and has potential as a therapeutic agent in neuropathic pain research. Nov 21 2024
E4657 PFI-6 PFI-6 is a selective MLLT1/3 probe that targets the YEATS domain of MLLT1 (ENL/YEATS1) and MLLT3 (AF9/YEATS3) with IC50 values of 140 nM and 160 nM for MLLT1 and MLLT3, respectively. PFI-6 demonstrates increased affinity and selectivity for MLLT1/3 than other human YEATS domain proteins (YEATS2/4). Nov 20 2024
E4977 Zileuton sodium Zileuton sodium (A 64077 sodium) is a potent, selective, and specific inhibitor of 5-lipoxygenase, exhibiting inflammatory activities. Zileuton sodium prevents polyp formation efficiently by reducing tumor-associated and systemic inflammation in in vivo models. Zileuton sodium also acts as a potential chemo-preventive agent in patients that are at high risk of developing colon cancer. Nov 20 2024
E1563 GNE-7883 GNE-7883 is a potent and allosteric small-molecule inhibitor of pan-TEAD, that allosterically blocks the interactions between YAP/TAZ and all human TEAD paralogs through binding to the TEAD lipid pocket. It effectively reduces chromatin accessibility at TEAD motifs, suppresses cell proliferation in a variety of cell line models and achieves strong antitumor efficacy in vivo. Furthermore, it effectively overcomes KRAS G12C inhibitor resistance. Nov 17 2024
E1856 ARS-1323 ARS-1323 is the racemic mixture, containing ARS-1620, and a potent inhibitor of mutant KRAS G12C. It can be used in research for biochemical binding screens as companion imaging drugs (CID) for KRAS G12C. Nov 17 2024
E4791 Adezmapimod hydrochloride Adezmapimod hydrochloride (RWJ 64809 hydrochloride, SB 203580 hydrochloride) is an inhibitor of the MAPK family member termed as stress-activated protein kinase 2a(SAPK2a; also known as p38). It exhibits IC50 of SAPK2a/p38 and SAPK2b/p38β2 with IC50 values of 50 nM and 500 nM respectively and can be used in research of chronic inflammatory diseases, such as rheumatoid arthritis. Nov 17 2024
E4778 BODIPY 493/503 BODIPY 493/503 (Pyrromethene 546, BDP 493/503 lipid stain) is a fluorescent neutral lipophilic dye. It is used to facilitate quantification of neutral lipid content, a lipid droplet–associated protein by flow cytometry and observation of lipid droplets(LDs) by microscopy. Nov 17 2024
E1815 STX-478 STX-478 is a highly potent, mutant-selective, allosteric inhibitor of PI3Kα, that selectively targets prevalent mutant forms of PI3Kα. It demonstrates strong efficacy against common PI3Kα helical- and kinase-domain mutations, including the H1047R variant, with an IC50 value of 9.4 nmol/L. STX-478 exhibits 14-fold greater selectivity for mutant PI3Kα over the wild-type form. It spares metabolic dysfunction and improves therapeutic response in PI3Kα-Mutant Xenografts. Nov 14 2024
E4922 Allopurinol riboside Allopurinol riboside, a metabolite of allopurinol, competitively inhibits the action of purine nucleoside phosphorylase on inosine in vitro with a Ki value of 277 μM. It displays potent activities against parasites. Nov 14 2024
E1979 Irpagratinib Irpagratinib (ABSK011) is a potent inhibitor of FGFR4 with an IC50 of < 10 nM in biochemical assays. It effectively suppresses FGFR4 auto-phosphorylation and disrupts downstream signal transduction. It also strongly inhibits tumor growth and induces regression in subcutaneous xenograft models. Nov 14 2024
E4740 TAK-861 TAK-861 is a potent, orally bioavailable agonist of orexin receptor 2 (OX2R), with an EC50 of 2.5 nM in calcium mobilization assays. It induces dose-dependent membrane depolarization in histaminergic neurons within the mouse tuberomammillary nucleus (TMN) with an EC50 of 31.7 nM. Nov 14 2024
E6017 Ornidazole (Levo-) Ornidazole (Levo-) (Levornidazole, (S)-Ornidazole), the levo-isomer of ornidazole, is a third-generation nitroimidazole derivative. It exhibits antiprotozoal and antibacterial properties against anaerobic bacteria. Nov 14 2024
P1245 Bovine Serum Albumin Bovine serum albumin (BSA, Albumin bovine serum) is an efficient passivating agent that inhibits nonspecific protein binding in assays such as ELISA. It is used to coat hydrophobic substrates, enhancing anti-fouling properties and reducing immune system interactions. Nov 14 2024
E4976 Tegaserod Tegaserod is an orally active agonist of serotonin receptor 4 (5-HT4R) and also acts as an antagonist of 5-HT2B receptor with pKi values of 7.5, 8.4, and 7.0 for human recombinant 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Tegaserod has anti-tumor activity and is used in the research of irritable bowel syndrome (IBS). Nov 12 2024
E4983 Omadacycline hydrochloride Omadacycline hydrochloride (PTK0796 hydrochloride) is a first-in-class orally active member of the tetracycline class of antibiotics. Omadacycline inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit. Omadacycline hydrochloride exhibits broad-spectrum antibacterial activity against aerobic and anaerobic Gram-positive and Gram-negative bacteria, as well as atypical bacteria. Nov 12 2024
E1272 SRI-37330 HCl SRI-37330 HCl(EX-A5854), an anti-diabetic drug, is an orally bioavailable inhibitor of thioredoxin-interacting protein (TXNIP), with an IC50 of 0.64 μM for TXNIP expression in INS-1 cells. Its treatment inhibits glucagon secretion and function, decreases hepatic glucose production, and reverses hepatic steatosis. Nov 07 2024
E1758 Bersacapavir Bersacapavir(JNJ-6379, JNJ-56136379) is a potent capsid assembly modulator (CAM) that accelerates capsid assembly and induces the formation of morphologically intact viral capsids devoid of genomic material. It inhibits HBV replication with an EC50 of 54 nM in HepG2.117 cells. Nov 07 2024
E1510 Sonrotoclax Sonrotoclax(BGB-11417) is a highly potent, orally active and selective inhibitor of Bcl2. Sonrotoclax demonstrates increased potency along with in vitro and in vivo inhibitory activity against both WT Bcl-2 and the G101V mutant. Bcl-xL Sonrotoclax has effective cell killing effect against a variety of lymphoma and leukemia cell lines. Nov 05 2024
S5970 Selenomethionine Selenomethionine (Seleno-DL-methionine, DL-Selenomethionine) is a naturally occurring amino acid containing selenium. Selenomethionine (SeMet) can substitute for methionine (Met) during protein synthesis in a non-specific manner. Due to the significant differences in their redox properties, the incorporation of SeMet in place of Met may adversely impact protein function. Nov 05 2024
E4598 MEN1703(SEL24,SEL24-B489) MEN1703(SEL24-B489,SEL24, Pim/flt3 kinase inhibitor SEL24) is a potent, type I, orally active, dual inhibitor of PIM and FLT3-ITD, that exhibits Kd values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively. MEN1703 exhibits its broad therapeutic potential in treatment of acute myeloid leukemia. Nov 04 2024
E1841 Monlunabant Monlunabant(INV-202, (S)-MRI-1891) is a peripherally acting inverse agonist of the cannabinoid type-1 receptor (CB1R), with the potential to treat respiratory and renal complications associated with metabolic disorders. It improves lung compliance in a mouse model of asthma and reduces renal fibrosis in a streptozotocin-induced diabetic nephropathy mouse model. Oct 30 2024
E4990 1-Butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide 1-Butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide (BMIM TFSI) is a room-temperature ionic liquid with excellent ionic conductivity. Its solvation dynamics and conductivity are affected by proton concentration, which influences its performance in electrochemical applications. Oct 30 2024
S9881 M4205（IDRX-42） M4205 (IDRX-42) is an oral, selective inhibitor of KIT with broad activity against mutations in KIT exons 11, 13, and 17. It exhibits significant and dose-dependent antitumor activity in the xenograft model of GIST. Oct 30 2024
E4940 Chlorphenesin carbamate Chlorphenesin carbamate(Maolate, Rinlaxer, U 19646) is a centrally-acting muscle relaxant that inhibits motoneuron excitability. It is also used to treat pain and discomfort related to skeletal muscle trauma and inflammation. Oct 30 2024
E4924 Anagrelide Anagrelide(BL416201), an imidazoquinazoline derivative, is an inhibitor of phosphodiesterase type III (PDEIII) with IC50 of 36 nM, which acts as an antithrombotic and platelet-reducing agent. Oct 30 2024
E4955 Pitolisant Pitolisant(BF2.649, Tiprolisant) is a potent, selective antagonist of the non-imidazole histamine H3 receptor, with a Ki value of 0.16 nM and an EC50 of 1.5 nM as an inverse agonist. It enhances the activity of histaminergic neurons, promoting vigilance and cognitive function. It is useful in research on wakefulness, memory deficits, and cognitive disorders. Oct 30 2024
E4984 Avibactam free acid Avibactam free acid(NXL-104 free acid) is a potent, covalent, reversible, non–β-lactam Inhibitor of β-lactamase, inhibiting β-lactamase TEM-1 and CTX-M-15 with an IC50 of 8 nM and 5 nM, respectively. It is useful in research on Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium, Gram-negative infections. Oct 30 2024
E4975 Angiotensin II human TFA Angiotensin II human TFA(DRVYIHPF TFA, Ang II TFA) is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system that regulates blood pressure by activating AT1Rand AT2R, stimulating sympathetic activity, aldosterone production, and renal actions. It also promotes vascular cell growth, collagen synthesis, fibrosis, and induces apoptosis and capillary formation via a redox-sensitive pathway. Oct 30 2024
E1672 NMDI14 NMDI14(DA-66137) is an inhibitor of nonsense-mediated RNA decay (NMD). NMDI14 disrupts the SMG7-UPF1 interactions and inhibits NMD. NMDI14 increases the stability and expression of NMD targeted mRNAs. Oct 28 2024
E1819 Zavondemstat Zavondemstat(QC8222, TACH 101) is a small-molecule pan-inhibitor of histone lysine demethylase 4D (KDM4D) that selectively targets KDM4A-D with no effect on other KDM families. It exhibits potent antiproliferative activity in various cancer cell lines and organoid models. It displays antineoplastic activity and acts as a potential anticancer agent. Oct 27 2024
E4985 Avibactam sodium hydrate Avibactam sodium hydrate(NXL-104 hydrate) is a covalent and reversible non-β-lactam inhibitor of β-lactamase which inhibits β-lactamase activity with IC50 values of 8 nM for TEM-1 and 5 nM for CTX-M-15, respectively. Oct 27 2024
E1782 DSP5336 DSP5336 is an oral small molecule inhibitor of menin and MLL protein interaction. DSP5336 is undergoing clinical evaluation for its use in the treatment of patients with Relapsed or Refractory Acute Leukemia. Oct 27 2024
E1879 CBD3063 CBD3063(EX-A8428) is a selective, first-in-class inhibitor of Cav2.2-CRMP2 (ollapsin response mediator protein 2)interaction. It suppresses surface trafficking of Cav2.2, and N-type (Cav2.2) calcium currents. CBD3063 allosterically regulates Cav2.2 to achieve analgesia and pain relief without negative side effect profiles. Oct 27 2024
E4602 VLS-1488(KIF18A-IN-6 ) VLS-1488 (KIF18A-IN-6) is an oral inhibitor of KIF18A with an IC50 of 0.016 μM. KIF18A is a mitotic kinesin motor protein that localizes at the plus-end of kinetochore microtubule spindle fibers and is crucial for cell division in aneuploid cancer cells with high chromosomal instability (CIN). Oct 24 2024
E4979 Olprinone Hydrochloride Olprinone hydrochloride(Loprinone Hydrochloride, E-1020) is a potent inhibitor of phosphodiesterase (PDE) 3, with an IC50 value of 0.35 μM for PDE3, respectively. Olprinone Hydrochloride is used in the research of heart failure treatment due to its positive inotropic and vasodilatory effects. It also exhibits anti-inflammatory properties. Oct 24 2024
S7475 NU9056 NU9056 is a potent and selective inhibitor of Tip60 (KAT5) histone acetyltransferase with an IC50 value of 2 µM. NU9056 demonstrates over 16-fold selectivity for Tip60 compared to PCAF, p300, and GCN5 and effectively induces apoptosis in prostate cancer cells. Oct 24 2024
S9813 dTAG-13 dTAG-13(FKBP12 PROTAC dTAG-13) is an ortho-substituted, heterobifunctional selective degrader of FKBP12F36V that effectively engage FKBP12F36V and CRBN leading to rapid and selective CRBN-mediated degradation of FKBP12F36V.It can useful for target validation in the context of drug discovery. Oct 23 2024
E4650 Ladarixin Ladarixin(DF 2156A free base) is a small molecule, orally available, allosteric and non-competitive antagonist of dual CXCR1 and CXCR2. It is able to reduce the acute and chronic neutrophilic influx, and can be used in research of Asthma, Idiopathic Pulmonary Fibrosis, Influenza-A infection and COPD, cutaneous and uveal melanoma conditions. Oct 23 2024
E4697 RGT-018 RGT-018, is a potent and selective inhibitor of SOS1. It blocks the interaction of KRAS:SOS1 with an IC50 of 8 nM and inhibited KRAS signaling and the proliferation of KRAS-driven cancer cells. It may exhibit potent anticancer activity against NSCLC, colorectal cancer, and pancreatic cancer. Oct 23 2024
E4980 Verapamil Verapamil(Iproveratril,Dilacoran), is a phenylalkylamine derivative which is an antagonist of calcium influx and also an inhibitor P-gp and CYP3A4. It exhibits potency in treatment for angina, cardiac arrhythmias, cardiomyopathies and hypertension. Oct 23 2024
E4969 Avatrombopag hydrochloride Avatrombopag hydrochloride(AKR-501 hydrochloride, YM477 hydrochloride) is an orally administered second generation agonist of Thrombopoietin receptor(TpoR) with an EC50 value of 3.3 nM. It is used in the treatment of primary chronic immune thrombocytopenia (ITP). Oct 23 2024
E1881 NVS-STG2 NVS-STG2(HY-157214) is a potent, allosteric small molecule agonist of STING. It binds at the transmembrane domain (TMD) interface of STING, thereby acting as a molecular glue to promote STING oligomerization and contribute to its activation. It may be used in research of STING-related autoimmune diseases. Oct 23 2024
E4643 BIIB129 BIIB129, is a unique brain-penetrant covalent inhibitor of Bruton’s tyrosine kinase (BTK), with high kinome selectivity. It exhibits efficacy in targeting B-cell proliferation in the central nervous system (CNS), making it a promising immunomodulatory therapy for multiple sclerosis (MS). Oct 23 2024
E4714 Xanomeline Xanomeline(LY-246708) is a selective agonist of muscarinic type 1(M(1) receptor and muscarinic type 4 receptor(M(4). It increases neuronal excitability and inhibits behaviors induced by D-amphetamine and (-)-apomorphine. Oct 23 2024
E1600 AMG-193 AMG-193 is an orally active and MTA-cooperative inhibitor of PRMT5 with potent biochemical and cellular activity. AMG-193, in combination with MTA, selectively targets and inhibits the growth of MTAP-deficient tumor cells by suppressing PRMT5, with an IC50 of 0.107 μM, while sparing normal cells that possess wild-type MTAP. AMG-193 also exhibits antitumor activity. Oct 22 2024
E4873 Mebhydroline Mebhydroline acts as a selective antagonist of farnesoid X receptor (FXR). Mebhydrolin improves blood glucose balance in in vivo mice models by inhibiting hepatic gluconeogenesis through the FXR/miR-22-3p/PI3K/AKT/FoxO1 pathway and enhancing glycogen synthesis. It also acts as a specific antagonist of histamine H1 receptor. It has potential for its use in the treatment of Type 2 diabetes mellitus (T2DM). Oct 22 2024
E4987 (S)-Flurbiprofen (S)-Flurbiprofen (Esflurbiprofen), an active enantiomer of Flurbiprofen, acts as an inhibitor of cyclooxygenase (COX-2) with an IC50 value of 0.48 μM, respectively. It also helps in the significant reduction of the inflammatory mediator-induced CGRP release. Oct 22 2024
E4881 Ifenprodil Ifenprodil(Dilvax, RC 61-91) is a potent antagonist of N-methyl-D-aspartate (NMDA) receptor that selectively inhibits receptors containing the NR2B subunit. It exhibits potential for its use in the treatment of various neurological diseases. Oct 22 2024
E4971 Oclacitinib Oclacitinib(PF-03394197), an inhibitor of JAK is highly potent at inhibiting JAK1 with an IC50 value of 10 nM, respectively. Oclacitinib is highly potent against the JAK1 enzyme, displaying a 1.8-fold selectivity for JAK1 vs. JAK2 and a 9.9-fold selectivity toward JAK1 vs. JAK3. Oct 22 2024
E4938 Diphenylpyraline Diphenylpyraline(Allergen, Difenilpiralina; 4-Diphenylmethoxy-1-methylpiperidine), also known as 4-Diphenylmethoxy-1-methylpiperidine, is a first-generation antihistamine that acts as an antagonist of the histamine H1 receptor. It provides therapeutic antiallergic effects and has the potential to treat cocaine addiction. Oct 17 2024
E4814 Teneligliptin Hydrobromide Hydrate Teneligliptin Hydrobromide Hydrate(MP-513 hydrobromide hydrate) is a potent, competitive, and long-lasting inhibitor of DPP-4. It competitively inhibited rhDPP-4, human plasma, and rat plasma with IC50 values of 0.889, 1.75, and 1.35 nM respectively. It suppresses high glucose-mediated mitochondrial dysfunction and can be used for treatment of type 2 diabetes. Oct 17 2024
E1982 SOP1812 SOP1812( QN-302), is a tetra-substituted naphthalene diimide (ND) derivative and selective inhibitor of G-quadruplex (G4) transcription. It shows great affinity to hTERT G4 and HuTel21 G4 with KD values of 4.9 and 28.4 nM, respectively. It binds to G-quadruplex DNA in cancer gene promoters region and shows strong anti-proliferative and anti-tumor activity in pancreatic cancer models. Oct 17 2024
E4988 Vonoprazan Fumarate Vonoprazan Fumarate(TAK-438), is a potent, orally active inhibitor of proton pump, specifically a potassium-competitive acid blocker (P-CAB), inhibiting H+,K+-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. It exhibits potent antisecretory activity and can be used in research of acid-related disease. Oct 17 2024
E4709 MS-L6 MS-L6(Agn-PC-0N3ahi, NSC34338) is a potent inhibitor of OXPHOS, targeting electron transport chain complexes I (ETC-I), combining inhibition of NADH oxidation and uncoupling effect, on the respiratory chain. It exhibits potent antitumor efficacy. Oct 17 2024
E4628 BMS-986235 BMS-986235 (LAR-1219) is a selective, orally active and potent agonist of formyl peptide receptor 2 (FPR2), with EC50 values of 0.41 nM and 3.4 nM for hFPR2 and mFPR2, respectively. BMS-986235 therapy shows promising improvements in cardiac structure and function in a mouse model of heart failure, highlighting its potential for preventing the progression of heart failure. Oct 15 2024
E4703 Culmerciclib Culmerciclib (TQB3616) is a potent inhibitor of cyclin dependent kinase (CDK)4/6 and exhibits highly effective antineoplastic activity. TQB3616 exhibits significant synergistic antitumor activity in estrogen receptor (ER)-positive/HER2-negative or HER2-positive breast cancer when combined with endocrine therapy or Human Epidermal Growth Factor Receptor 2 (HER2) targeted therapy. Oct 15 2024
E4704 D34-919 D34-919 is potent inhibitor of the ALDH1A3-PKM2 interaction, and prevents the ALDH1A3-mediated enhancement of PKM2 tetramerization. D34-919 mediated in vitro and in vivo treatment enhances and restores chemoradiotherapy-induced apoptosis and sensitivity in glioblastoma (GBM) cells. Oct 15 2024
E1288 Inaxaplin Inaxaplin (VX-147) is an orally active inhibitor of apolipoprotein L1 (APOL1) function. Inaxaplin binds to APOL1 and is useful in the treatment of APOL1-associated kidney disease. Oct 15 2024
E4936 Larazotide acetate Larazotide acetate(AT-1001), a synthetic peptide, is an antagonist of zonulin. It functions as a gut permeability regulator for the treatment of celiac disease.  Oct 15 2024
E1633 BAY-805 BAY-805 is a potent, selective, and cell-active inhibitor that non-covalently targets the catalytic activity of USP21, a member of the ubiquitin-specific protease (USP) subfamily of deubiquitinating enzymes (DUBs). Oct 15 2024
A2165 Anti-mouse PD-1 (CD279)(29F.1A12)-InVivo Anti-mouse PD-1 (CD279)(29F.1A12)-InVivo reacts with mouse PD-1 (programmed death-1) also known as CD279. PD-1 is a 50-55 kDa cell surface receptor encoded by the Pdcd1 gene that belongs to the CD28 family of the Ig superfamily. Oct 12 2024
E4945 Pregnenolone monosulfate sodium Pregnenolone monosulfate sodium, a sodium salt form of pregnenolone monosulfate, is an active neurosteroid and a precursor of all steroid hormones. It functions act as a potent endogenous allosteric signal-specific inhibitor of CB1 receptors, reducing psychoactive effects associated with Δ9-tetrahydrocannabinol (THC). Oct 10 2024
E4652 ZX703 ZX703 is a proteolysis targeting chimera (PROTAC), that is a degrader of GPX4 through the ubiquitin-proteasome and the autophagy-lysosome with a DC50 of 0.315 µM. It induces the accumulation of lipid reactive oxygen species (ROS), thereby inducing ferroptosis cancer cells. Oct 10 2024
E1301 Imlunestrant Imlunestrant(LY3484356) is a potent, orally bioavailable selective estrogen receptor degrader (SERD) that functions as a pure antagonist of estrogen receptor alpha (ERα). It inhibits ER-dependent gene transcription and cell proliferation, resulting in sustained suppression of estrogen-driven growth in ER-positive cells. Oct 10 2024
E4715 SB-328437 SB-328437 is a non-peptide small molecule, potent and selective antagonist of CCR3 with an IC50 of 4.5 nM. It is important for eosinophil recruitment, a process that is thought to be crucial in the pathology of several inflammatory diseases including asthma, allergic rhinitis, and eczema. Oct 10 2024
E1967 ORIC-944 ORIC-944 is a potent and selective allosteric inhibitor of the polycomb repressive complex 2 (PRC2) via the embryonic ectoderm development (EED) subunit. It exhibits anti-tumor activity in vivo prostate cancer models. Oct 07 2024
E4947 Estrone sulfate sodium Estrone sulfate (Estrone 3-sulfate sodium salt, Premarin), an inactive form of estrogen, serves as a major circulating estrogen in the plasma. It is converted into the active form, estrone (E1), through the action of steroid sulfatase (STS. Estrone sulfate is commonly used in breast cancer research. Oct 07 2024
E4692 THZ-P1-2 THZ-P1-2 is an inhibitor of PI5P4K, which covalently binds to cysteines on a disordered loop in PI5P4Kα/β/γ. It inhibits PI5P4Kα kinase activity with an IC50 of 190 nM and disrupts autophagy by impairing autophagosome clearance and increasing TFEB nuclear localization. Oct 07 2024
E1831 FX-909 FX-909 is an orally available inverse agonist and inhibitor of the transcription factor (TF) peroxisome proliferator activated receptor gamma (PPARG, PPARγ) ), which exhibits anti-tumor activity in vivo. Oct 07 2024
E4958 cis-Bac430 Cis-Bac430 plays a role in mediating the movement of anti-tumor CD8+cells from the periphery to the tumor site,thus enhancing the anti-tumor effect of an immune checkpoint inhibitor. Sep 29 2024
E4886 HS-10296 hydrochloride HS-10296 hydrochloride(Almonertinib (hydrochloride), HS-10296 HCl) is an irreversible, third-generation inhibitor of EGFR tyrosine kinase that demonstrates high selectivity for EGFR-sensitizing mutations, T790M resistance mutation. It exhibits inhibitory activity against T790M, T790M/L858R, and T790M/Del19, with IC50 of 0.37 nM, 0.29 nM, and 0.21 nM, respectively. It also exhibits anti-tumor activity. Sep 28 2024
E1973 R16 R16(NSC29869, Nrf2-IN-3) is an inhibitor of NRF2 (nuclear factor erythroid 2-related factor 2) that selectively binds KEAP1 mutants and restores their NRF2-inhibitory function by repairing the disrupted KEAP1/NRF2 interactions. It significantly enhances the sensitivity of KEAP1-mutated tumor cells to cisplatin and gefitinib. Sep 28 2024
E1349 TNG908 TNG908 is a potent, selective, and brain-penetrant inhibitor of PRMT5 with an IC50 of 4 μM, acting through an MTA-cooperative mechanism. It also shows antitumor activity in a xenograft model. Sep 28 2024
E1842 Palazestrant Palazestrant(OP-1250) is an orally bioavailable complete antagonist of estrogen receptor (ER) that blocks ER activity. It exhibits antiproliferative and antitumor activity in ER-positive (ER+) breast cancer models. Sep 28 2024
E4893 Flecainide hydrochloride Flecainide hydrochloride, an antiarrhythmic drug, is a blocker of hydrophilic sodium channels with a pKa of 9.3. At pH 7.4. It also inhibits the ryanodine receptor (RyR2), reducing spontaneous calcium release from the sarcoplasmic reticulum. Sep 28 2024
E4862 Pimethixene Pimethixene(Calmixen, Pimetixene) is a highly potent and non-selective antagonist of the 5-HT2B receptor, with a pKi of 10.44. It also functions as an antihistamine and anticholinergic agent, and is a highly potent multi-target antagonist with antagonistic effects on multiple receptors. Sep 28 2024
E4900 Enalapril Enalapril(Eletriptan, Amprace, Vaseretic) is an inhibitor of angiotensin-converting enzyme (ACE), primarily used to treat hypertension, heart failure, and asymptomatic left ventricular dysfunction. It also attenuates frailty in aging mice. Sep 26 2024
E4954 Demeclocycline Demeclocycline(Demethylchlortetracycline (DMCT), Ledermycin) is a bacteriostatic antibiotic from the tetracycline class, that induces diuresis and can cause nephrogenic diabetes insipidus. It also manages the syndrome of inappropriate antidiuretic hormone secretion (SIADH) by restoring normal plasma sodium levels and permitting unrestricted water intake. Sep 26 2024
E4834 12-Crown-4 12-crown-4(EOCT, Ethylene oxide cyclic tetramer) is an effective phase-transfer catalyst and complexing agent for lithium, facilitating the dissolution of lithium bis(trifluoromethanesulfonyl)imide (LiTFSI) without requiring acetonitrile. It selectively binds to lithium ions and forms stable complexes, significantly improving electrolyte conductivity in lithium batteries, and positively influencing ion mobility and overall battery performance. Sep 25 2024
E4701 CMP-5 CMP5 is a potent and selective small molecule inhibitor of PRMT5. It is found to selectively block S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. It also exhibit potential for research into treatment for EBV+ lymphomas and other B-cell NHL subtypes. Sep 25 2024
E4687 NIBR-LTSi NIBR-LTSi is a selective small-molecule inhibitor of LATS kinase . It agonizes YAP signaling and promotes tissue regeneration in vitro and in vivo, supporting future research on the regenerative potential of the YAP/Hippo pathway. Sep 25 2024
E4680 MTX-531 MTX-531(NSC827271) is a first-in-class, potent and selective inhibitor of EGFR and PI3Kα with an IC50 of 14.7 nM and 6.4 nM, respectively. It may play a role in treating Head and Neck Squamous Cell Carcinoma (HSNCC), squamous lung cancers, and certain EGFR/PI3K-driven triple-negative breast cancers. Sep 25 2024
E4844 Valbenazine Valbenazine(Ingrezza, Mt-5199, NBI-98854, VBZ) is a potent inhibitor of vesicular monoamine transporter 2 (VMAT2) with a Ki of 110–190 nM. It is used to treat tardive dyskinesia and chorea associated with Huntington's disease. Sep 25 2024
E4675 Rezivertinib Rezivertinib(BPI-7711) is a potent third-generation inhibitor of EGFR tyrosine kinase, targeting both EGFR-sensitizing mutations and the EGFR T790M mutation. Additionally, it has excellent CNS penetration and has antitumor activity. Sep 25 2024
E4946 Tafenoquine Succinate Tafenoquine Succinate(WR 238605 Succinate, Etaquine, Krintafel) is an 8-aminoquinoline (8AQ) anti-malarial drug that kills both the liver and blood stages of the parasite, broadening its applicability for chemoprophylaxis to all species of malaria. It is specifically used for the prevention of Plasmodium vivax relapse. Sep 25 2024
E1993 BGB-16673 BGB-16673(BTK-IN-29) is an inhibitor of Bruton’s tyrosine kinase (Btk) and can be used in research for the treatment of autoimmune and inflammatory diseases. Sep 25 2024
E4941 Diflorasone diacetate Diflorasone diacetate(Florone), is a steroid anti-inflammatory drug, an inhibitor of TARC (thymus and activation regulated chemokine; CCL17) in the dinitrochlorobenzene (DNCB) model. It can be used in the treatment of allergic and inflammatory skin diseases such as atopic dermatitis and allergic contact dermatitis. Sep 25 2024
E4932 Amikacin Amikacin(BAY 41-6551, Lukadin) is a semisynthetic aminoglycoside, derived from kanamycin-A, that acts as an inhibitor of the Z ring formation, leading to the inhibition of cell division. It is used to treat serious infections caused by aerobic Gram-negative bacteria, mycobacteria, Nocardia, and life-threatening infections in neonates. Sep 25 2024
E4956 Ozanimod hydrochloride Ozanimod hydrochloride(Zeposia, RPC-1063 HCL) is a potent sphingosine 1-phosphate (S1P)receptor modulator and a selective agonist of S1P receptor subtypes 1 (S1P1) and 5 (S1P5) with EC50's of 1.03 nM and 8.6 nM, respectively. It can be used in the trearment of relapsing multiple sclerosis (MS). Sep 25 2024
E4923 AnaMorelin hydrochloride Anamorelin hydrochloride(RC-1291 HCL, ONO-7643) is a potent and selective agonist of ghrelin receptor with EC50 of 0.74 nM FLIPR assay. It has a significant appetite-enhancing activity and has the potential to treat cancer anorexia-cachexia syndrome. Sep 25 2024
E4907 Clomipramine Clomipramine(Hydiphen, Anafranil base) blocks the production of norepinephrine in the central nervous system and 5-HT reuptake, thereby exerting sedative and anticholinergic effects, with IC50 of 1.5 nM. Clomipramine is also a non-selective monoamine reuptake inhibitor that can affect the transmission of multiple neurotransmitters. Sep 25 2024
E1271 Zunsemetinib Zunsemetinib(ATI-450, CDD-450) is a selective inhibitor of p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) that mediates inflammatory responses. It reduces inflammation in cryopyrinopathy, alleviates arthritis, and potentially prevents tachyphylaxis. Sep 25 2024
E4921 Azelastine Azelastine(Azelastina; Astelin) is a potent antihistaminic and antiallergic drug, an antagonist of the histamine H1 receptor. It is also effective in treating allergic rhinitis, bronchial asthma, and SARS-CoV-2 and has shown potential in ameliorating aortic calcification, increasing apoA expression, and reducing apoB levels. Sep 25 2024
P1240 Etanercept Etanercept, a dimeric fusion protein, functions as an inhibitor of TNF by binding to TNF. It competitively blocks the attachment of both TNF-α and TNF-β to their cell surface receptors, thereby neutralizing TNF's biological activity. Etanercept has proven effectiveness in treating rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis. Sep 24 2024
E1491 Brigimadlin Brigimadlin(BI 907828) is a potent, orally active inhibitor of E3 ubiquitin-protein ligase MDM-2. Brigimadlin inhibits MDM-2's suppression of the tumor suppressor p53. It promotes apoptosis and enhances the transcription of p53 targets such as p21 and PUMA in BT48, BT67, and BT73 cells. Sep 23 2024
E4599 BGB-3245(Brimarafenib) BGB-3245(Brimarafenib, Brimarafenibum) is an inhibitor of Raf kinase. BGB-3245 displays potent effects against different RAF isoforms, including BRAF Class I/II/III mutations, BRAF fusions, and heterodimerization with CRAF in preclinical models. It also exhibits antineoplastic effects. Sep 23 2024
E4849 Terbutaline Terbutaline(Brican, Brethine), an active metabolite of bambuterol is an orally active agonist of β2-adrenergic receptor, that increases MKP-1 expression. Terbutaline is used in the treatment of obstructive lung diseases as a bronchodilator remedy. It also exhibits anti-inflammatory effects. Sep 23 2024
E4913 Calcifediol monohydrate Calcifediol monohydrate(25-hydroxy Vitamin D3 monohydrate), is an effective vitamin D receptor (VDR) ligand and VD supplement. It acts as an inhibitor of vitamin D receptor (VDR) Calcifediol is a prohormone of the vitamin D endocrine system (VDES) and is hydroxylated in the liver to produce the active form, calcitriol. Calcifediol can rapidly increase serum VD levels. Sep 23 2024
E4925 Amsacrine Amsacrine(m-AMSA; acridinyl anisidide) is an inhibitor of topoisomerase II. Amsacrine acts as an antineoplastic agent which intercalates into the DNA of tumor cells, it is also used in the treatment of acute myelogenous leukemia. Sep 23 2024
E4874 Lumateperone Tosylate Lumateperone tosylate(ITI-007) is an antagonist of 5-HT2A receptor. It also acts as a partial agonist of presynaptic D2 receptors, as an antagonist of postsynaptic D2 receptors, and as a modulator of dopamine D1 receptor. Lumateperone tosylate demonstrates anticancer activity. Sep 23 2024
E4957 Mozavaptan (hydrochloride) Mozavaptan hydrochloride(OPC 31260 HCl), a benzazepine derivative is a potent, selective, competitive, and orally active antagonist of vasopressin V2 receptor with an IC50 value of 14 nM. Mozavaptan hydrochloride shows ~85-fold selectivity for V2 receptor over V1 receptor. Mozavaptan hydrochloride has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment. Sep 23 2024
E4951 Eprosartan Eprosartan(Teveten, SK-108566) is a selective, competitive, nonpeptide and orally active antagonist of angiotensin II receptor. Eprosartan binds angiotensin II receptors with IC50 values of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively. Sep 23 2024
E1910 TASIN-30 TASIN-30 is a selective inhibitor of Emopamil binding protein (EBP) with EC50 values of 0.097 μM for EBP competition, respectively. TASIN-30 displays selectivity for EBP over DHCR24. Sep 23 2024
E4939 Sulfisoxazole acetyl Sulfisoxazole acetyl(N1-Acetylsulfisoxazole, Acetyl sulfafurazole), a sulfisoxazole derivative, is an orally active inhibitor of dihydropteroate synthase. Sulfisoxazole acetyl can be biotransformed primarily to sulfisoxazole, and partly to N(4)-acetyl sulfisoxazole (N4AS). Sulfisoxazole acetyl exhibits antibacterial action. Sep 23 2024
E4648 Pico145 Pico145(HC-608) is a selective inhibitor of TRPC1/4/5 channels. It inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC50 values of 0.349 and 1.3 nM, respectively. It exhibits no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8. Sep 23 2024
E1637 ALKBH5 inhibitor 1 (compound 3) ALKBH5 inhibitor 1 (compound 3) is an inhibitor of the RNA m6A Demethylase ALKBH5, with an IC50 value of 0.84 μM. It also exhibits potent antiproliferative activity. Sep 19 2024
E1785 PF-06952229 PF-06952229(UNII-1KKS7U3X86) is a selective, orally available inhibitor of the serine/threonine kinase TGF-β receptor 1 (TGF-β-R1). It inhibits pSMAD2 in both tumor and immune cells, reducing TGF-β signalling and reversing EMT in vitro. It modulates the tumor immune microenvironment and shows antitumor activity in mouse models. Sep 19 2024
E4700 ML-099 ML099(CID-888706) is a pan-activator of Ras-related GTPases. It enhances GTPase activity by increasing its affinity for guanine nucleotides through binding to an allosteric site between switch regions I and II. Sep 19 2024
E1972 AZD8421 AZD8421 is a potent and highly selective inhibitor of Cyclin-dependent Kinase 2 (CDK2), with an IC50 against CDK2 of 9nM with selectivity over CDK1, CDK4 and CDK6. It also exhibits an anti-proliferative effect, effectively inhibits Rb phosphorylation, and shows strong activity both as a monotherapy and in combination with CDK4/6 inhibitors in breast and ovarian cancer models. Sep 18 2024
E1834 iMDK iMDK is a potent inhibitor of PI3K. It also inhibits the growth factor MDK (also known as midkine or MK). iMDK use along with a MEK inhibitor suppresses tumor growth of non-small cell lung cancer (NSCLC), including KRAS-mutant NSCLC and squamous NSCLC. Sep 18 2024
E4930 Asenapine Asenapine(Org 5222, HSDB8061) is a multi-target receptor antagonist. It acts as an antagonist of serotonin receptors with pKi values of 8.4-10.5, adrenoceptors with pKi values of 8.9-9.5, dopamine receptors with pKi values of 8.9-9.4 and histamine receptors with pKi values of 8.2-9.0. Sep 18 2024
E4949 Eslicarbazepine Eslicarbazepine (BIA 2-194), an active metabolite of the prodrug eslicarbazepine acetate is an inhibitor of voltage-gated sodium channel (Nav). It acts by enhancing the slow activation of voltage-gated sodium channels, reducing their availability. Sep 18 2024
E4918 BecloMethasone Beclomethasone(Beclometasone) is a prototype agonist of glucocorticoid receptor. Beclomethasone and its derivatives display have higher binding affinity to glucocorticoid receptors in rat liver, thymus, and hypophysis. Sep 18 2024
E4964 ATP (disodium trihydrate) ATP disodium trihydrate, is the primary energy currency of the cell, essential for intracellular energy metabolism. It regulates extracellular biological processes, including cardiac function, neurotransmission, muscle contraction, vasodilation, bone and liver glycogen metabolism, and inflammation. It also plays a crucial role in initiating immune responses during infections. Sep 13 2024
E4661 dWIZ-2 dWIZ-2, is a molecular glue degrader of the WIZtranscription factor degrading WIZ with a DC50 of 32 nM. It also robustly induces fetal hemoglobin (HbF) in erythroblasts with an EC50 of 202 nM. Sep 13 2024
E4914 Cabozantinib hydrochloride Cabozantinib hydrochloride(XL184, BMS-907351 hydrochloride) is a potent small-molecule kinase inhibitor of c-MET and VEGFR2 with an IC50 of 1.3 nM, 0.035 nM respectively. It also inhibits RET, KIT, AXL, Tie2 and FLT3 with an IC50's of 5.2 nM, 4.6 nM, 7 nM, 14.3 nM, 11.3nM respectively. It can be promising agent for inhibiting tumor angiogenesis and metastasis in cancers with dysregulated MET and VEGFR signaling. Sep 13 2024
E4876 Lisinopril Lisinopril(MK-521) is a potent inhibitor of angiotensin-1 converting enzyme (sACE-1) with an IC50 of 1.9 nM. It demonstrates significant efficacy in the management of hypertension and heart failure, potentially improving cardiovascular outcomes. Sep 13 2024
E4960 L-Lysine hydrate L-Lysine hydrate is a first-limiting, essential amino acid with important roles in connective tissues and carnitine synthesis, energy production, growth in children, and maintenance of immune functions. It also ameliorates vascular calcification by modifying several key pathways and attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6. Sep 13 2024
E1302 Braco-19 trihydrochloride Braco-19 trihydrochloride(BRAC-O19, BRACO19 3HCl) is a G-quadruplex-stabilizing agent and an inhibitor of telomere/telomerase. It establishes antiviral activity against HIV-1 and anticancer effects by inhibiting telomerase capping and catalytic functions. Sep 13 2024
E1948 ZT-1a ZT-1a is a potent and selective, non-ATP-competitive inhibitor of STE20/SPS1-related proline-alanine-rich kinase (SPAK) with an IC50 of 44.3 μM. It can exhibit therapeutic potential for brain disorders linked to impaired ionic homeostasis in research. Sep 13 2024
E4677 PKUMDL-LC-101-D04 PKUMDL-LC-101-D04(GPX4-Activator-1d4) is a potent allosteric activator of Glutathione peroxidase 4 (GPX4) effectively suppressing ferroptosis and inflammation. It enhances GPX4 activity by 150% at 20 µM in a cell-free assay and 61 µM in cell extracts, also providing protection against cholesterol hydroperoxide (ChOOH)-induced damage. Sep 13 2024
E4639 FIDAS-5 FIDAS-5 is a potent and orally active inhibitor of methionine S-adenosyltransferase 2A (MAT2A) with an IC50 value of 2.1 μM, respectively. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 also demonstrates anticancer activity. Sep 12 2024
E4622 RP-102124 RP-102124 is a first-in-class allosteric inhibitor of multi-Rac with activity against oncogenic Rac1b. RP-102124 is orally bioavailable and exhibits dose-dependent inhibition of tumor growth in xenograft models. It exhibits potent inhibition of phenotypic characteristics of Rac signaling such as cell migration and cytoskeletal rearrangements. Sep 12 2024
E4916 Bestatin hydrochloride Bestatin hydrochloride is an inhibitor of aminopeptidase N and enkephalinase that elevates the levels of angiotensin II and angiotensin III. It also acts as a non-competitive inhibitor (α > 1) of porcine DPP-IV with a Ki value of 75 μM. It reduces DPP-IV activity, decreases cell viability, and increases DNA fragmentation in vitro. It has the potential to treat skin conditions like acne, psoriasis and keloids. Sep 12 2024
S5707 Aripiprazole lauroxil Aripiprazole lauroxil(Aristada) is an extended-release prodrug of aripiprazole designed for intramuscular injection. It acts as a dopamine-serotonin system stabilizer, with a potent partial agonist for dopamine D2 and serotonin 5-HT1A receptors while an antagonist for serotonin 5-HT2A receptors. Sep 12 2024
E4891 Fostemsavir Tris Fostemsavir Tris(BMS-663068 Tris) is a phosphonooxymethyl prodrug of BMS-626529, formulated as a tris(hydroxymethyl)aminomethane salt. It inhibits human immunodeficiency virus type 1 (HIV-1) by binding to the gp120 protein, preventing the virus from attaching to CD4+ T-cells. Sep 12 2024
E4910 Cariprazine Cariprazine(RGH-188, MP-214) acts primarily as a partial agonist at dopamine receptors, with pKi values of 10.07 for D3, 9.16 for D2L, and 9.31 for D2S receptors. It also acts as an antagonist forserotonin receptors, with pKi of 9.24, 8.59, 7.73, and 6.87 for5-HT2B,5-HT1A, 5-HT2A, and 5-HT2C receptors, respectively. Sep 12 2024
E4929 (S)-Clopidogrel (S)-Clopidogrel is an inhibitor of P2Y12 and exerts anticoagulant effects. It is metabolized into an active form that binds to the P2Y12 receptor, blocking ADP and preventing platelet aggregation. It also exhibits anti-inflammatory and antifibrotic properties in chronic kidney disease (CKD) and liver fibrosis. Sep 12 2024
E4897 Estramustine Estramustine(NSC-89201, LEO275) is used to treat hormone-resistant prostate cancer and stabilize microtubule dynamics. It acts as an anti-mitotic and anti-microtubule agent and disrupts microtubule disassembly. It inhibits the binding of MAPs 1 and 2 to taxol-stabilized microtubules, hinders microtubule assembly, and promotes the disassembly of MAP-2-associated microtubules. Sep 12 2024
E4920 Baclofen hydrochloride Baclofen hydrochloride is an agonist of the GABAB receptor that mimics the action of GABA, leading to slow presynaptic inhibition via the GABAB receptor. It improves the function of the ubiquitin-proteasome system (UPS) and enhances cell survival in both in vitro and in vivo models of Huntington's disease (HD). Sep 12 2024
E4961 Rutin (trihydrate) Rutin trihydrate is a bioflavonoid composed of the flavonol quercetin and the disaccharide rutinose. It exhibits anti-inflammatory and antiproliferative properties. It also acts as an antioxidant by scavenging reactive oxygen species (ROS). It lowers ROS levels, which in turn reduces oxidative stress in neurons, thereby controlling neuropathy (including auditory neuropathy) in patients with diabetes. Sep 12 2024
P1243 Fetuin, Fetal Bovine Serum Fetuin, Fetal Bovine Serum, a prevalent protein found in fetal bovine plasma, is the bovine equivalent of human α2HS glycoprotein (α2HS), commonly used as a supplement in various serum-free media. It inhibits trypsin activity and enhances cellular attachment, growth, and differentiation in culture systems. Sep 12 2024
E4597 Avitinib maleate Avitinib maleate(Abivertinib maleate, AC0010 maleate, AC0010MA) is a third-generation, irreversible, and orally active selective inhibitor of EGFR. It displays IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M, and wild-type EGFR. Avitinib maleate also acts as an inhibitor of BTK that induces apoptosis of BTK in mantle cell lymphoma. Sep 10 2024
E1969 ADT-007 ADT-007 is a potent and orally active pan-RAS inhibitor. ADT-007 effectively targets and suppresses the proliferation of cancer cells harboring mutated or hyper-activated wild-type RAS isozymes. ADT-007 exhibits potent anti-cancer effects. Sep 09 2024
S9911 Chlorin e6 Chlorin e6(Ce6, Phytochlorin) is a photosensitizer characterized by strong absorption peaks at 402 nm and 662 nm and intense fluorescence at 668 nm. It possesses antimicrobial and anticancer activities. It activates caspase-3 and induces apoptosis in cells, making it valuable for cancer research.Solutions are unstable and should be fresh-prepared. Sep 09 2024
E4651 HRS-4642 HRS-4642 is a selective inhibitor of KRAS G12D with a Kd value of 0.083 nM. It exhibits robust anti-cancer activity against KRAS G12D-mutant cancers both in vitro and in vivo. Sep 09 2024
E4615 GLPG0187 GLPG0187 is a broad-spectrum antagonist of integrin receptor. It inhibits αvβ1-integrin with an IC50 value of 1.3 nM. GLPG0187 also inhibits migrasome biogenesis without cytotoxicity. GLPG0187 exhibits potent antitumor activity. Sep 09 2024
E1701 Vanzacaftor Vanzacaftor(VX-121) is an orally active corrector of Cystic fibrosis transmembrane conductance regulator (CFTR). Vanzacaftor improves the processing and trafficking of CFTR protein and increases chloride transport in combination with Tezacaftor and Deutivacaftor. Sep 09 2024
E4919 Barnidipine hydrochloride Barnidipine hydrochloride(Mepirodipine hydrochloride; YM-09730-5) is an antagonist of L-type calcium (CaA). It displays a high affinity for [3H] initrendipine binding sites with a Ki value of 0.21 nmol/l. Barnidipine hydrochloride also acts as an antihypertensive agent. Sep 09 2024
E4903 Dalasetron Mesylate Hydrate Dolasetron Mesylate hydrate(MDL-73147EF hydrate) is an antagonist of serotonin 5-HT3 receptor. It is used in the treatment of patients with nausea and vomiting following chemotherapy. Sep 08 2024
E1827 ECC5004(AZD5004) ECC5004(AZD5004, GLP-1 agonist (Eccogene)) is a small molecule GLP-1 receptor agonist (GLP-1RA) used to treat digestive system diseases and endocrine and metabolic diseases. ECC5004 has the potential to be used to treat obesity, type 2 diabetes and metabolic dysfunction-associated steatohepatitis (MASH) disease. Sep 08 2024
E1971 Rezatapopt Rezatapopt(PC14586) is a first-in-class p53 reactivator. It selectively binds to the mutated p53 Y220C protein and restores its wild-type activity. It can also be used to inhibit solid tumor with p53 mutation. Sep 05 2024
E4686 DCZ0415 DCZ0415 is a potent inhibitor of TRIP13. DCZ0415 impairs nonhomologous end joining repair and inhibits NF-κB activity. It triggers anti-myeloma effects both in vitro, and in vivo, and primary cells obtained from myeloma patients resistant to drugs. Sep 05 2024
E1836 Cevidoplenib dimesylate Cevidoplenib dimesylate(SKI-O-703 dimesylate) is an orally available inhibitor of spleen tyrosine kinase (Syk) with potential anti-inflammatory and immunomodulating activities. It attenuates the progression of autoantibody-mediated autoimmune diseases by inhibiting both autoantibody-producing and autoantibody-sensing cells. Sep 05 2024
E1508 APG-2449 APG-2449 is an orally active inhibitor of ALK/ROS1/FAK. APG-2449 exerts potent and durable antitumor activity in human non-small-cell lung cancer (NSCLC) and ovarian tumor models. Sep 04 2024
E4662 CK-586 CK-586(CK-4021586) is an inhibitor of cardiac myosin used to treat obstructive hypertrophic cardiomyopathy (oHCM). It effectively reduces left ventricular outflow tract obstruction (LVOTO) in a dose-dependent manner. Sep 03 2024
E4695 OPB-171775 OPB-171775 functions as a molecular glue, promoting the formation of a complex between phosphodiesterase 3A (PDE3A) and Schlafen family member 12 (SLFN12). This interaction triggers multiple cellular stresses, ultimately leading to cell death. It also demonstrates significant anticancer activity in patient-derived xenograft (PDX) models of Gastrointestinal stromal tumor (GIST). Sep 03 2024
E4679 Bleximenib oxalate Bleximenib oxalate(Menin-MLL inhibitor 24 oxalate) is an inhibitor of menin-mixed-lineage leukemia 1 (menin-MLL) . It can be used for the research of cancer. Sep 03 2024
E4659 Pyr3 Pyr3 is a selective and potent inhibitor of transient receptor potential canonical channel 3 (TRPC3). It inhibits TRPC3-mediated Ca2+ influx in a dose-dependent manner with the IC50 value of 0.7 μM. It holds potential for treating TRPC3-related diseases like cardiac hypertrophy. Sep 03 2024
E1556 GSK-3484862 GSK-3484862 is a non-covalent, potent and selective inhibitor of DNMT1 with an IC50 of 0.23 μM. It demonstrates efficacy in acute myeloid leukemia. Sep 03 2024
E4660 TAC(TERT activator compound) TAC(TERT activator compound) is an activator of TERT, that upregulates TERT transcription via the MEK/ERK/AP-1 cascade. It enhances telomere synthesis, reduces aging markers, inflammation, and senescence, and preserves brain function, highlighting TERT's potential in combating aging and related diseases. Sep 03 2024
E4624 Tradipitant Tradipitant(VLY-686, LY686017) is the 2nd generation antagonist of neurokinin-1 (NK-1). It exhibits potential for treating chemotherapy-induced nausea, depression, alcoholism, social anxiety disorder, and for developing imaging ligands. Sep 03 2024
E4872 Mefloquine Mefloquine(Lariam, WR-142490) is a quinoline antimalarial drug and an antagonist of K+ channel (KvQT1/minK) with an IC50 of ~1 μM. It is widely used in both the treatment and prophylaxis of Plasmodium falciparum malaria, and can prolong cardiac repolarization. Sep 03 2024
E4888 Guanabenz hydrochloride Guanabenz hydrochloride(NE56490) is a small molecule, antihypertensive agonist of α2-adrenoceptor. It also inhibits eIF2α and GADD34, showing potential for treating cardiac hypertrophy, heart failure, atherosclerosis, and ischemic heart disease. Sep 03 2024
E4845 Ulipristal Ulipristal(Deacetyl CDB-2914, CDB-3236) is a selective modulator of progesterone receptors used in a single dose as an emergency postcoital contraceptive. Sep 03 2024
E4902 Dantrolene Dantrolene is an antagonist of ryanodine receptor (RYR) and a postsynaptic skeletal muscle relaxant that reduces calcium release from the sarcoplasmic reticulum (SR), leading to a dose-dependent decrease in myoplasmic free calcium levels. It is used to treat and control the accelerated hypermetabolism of skeletal muscle that leads to a malignant hyperthermia crisis. Sep 01 2024
E4673 AMTB hydrochloride AMTB hydrochloride is a blocker of the transient receptor potential melastatin 8 (TRPM8) ion channel. It reduces the activation of TRPM8 channels induced by icilin, as assessed through a Ca2+ influx assay, with a pIC50 of 6.23. It is used as a tool to evaluate the role of this channel in bladder rhythmic contraction. Sep 01 2024
E4904 Dacomitinib hydrate Dacomitinib hydrate(PF-00299804, PF-804) is an orally administered, highly selective irreversible inhibitor targeting pan-ERBB receptors, with an IC50 of 6.0 nM for EGFR, 45.7 nM for ERBB2, and 73.7 nM for ERBB4. It also demonstrates anti-tumor activity. Sep 01 2024
E4905 Cyclizine hydrochloride Cyclizine hydrochloride is an antagonist of the H1 histamine receptor used for the treatment and prevention of vertigo and motion sickness. It also exhibits antihistaminic properties. Sep 01 2024
E4885 Dopamine Dopamine is a catecholamine neurotransmitter in the mammalian brain. It plays role as a modulator of cardiovascular function, catecholamine release, hormone secretion, vascular tone, renal function, and gastrointestinal motility. Aug 28 2024
E4674 Cu(II)GTSM Cu(II)GTSM is a potent cell-permeable inhibitor of GSK3β that also inhibits Aβ oligomers and reduces tau phosphorylation. It shows potential as an anticancer and antimicrobial agent and may restore cognitive function by inhibiting neurotoxic Aβ trimers and phosphorylated tau. Aug 28 2024
E1952 BLU-222 BLU-222 is an oral, potent, and selective inhibitor of cyclin-dependent kinase (CDK) 2 and exhibits significant antitumor activity in the OVCAR-3 CDX model. Aug 28 2024
E4620 L-778123 hydrochloride L-778123 hydrochloride is a potent dual inhibitor of farnesyl protein transferase (FPTase) with an IC50 of 2 nM and geranylgeranyl protein transferase I (GGPTase-I) with an IC50 of 98 nM. It also displays promising anti-leukemia activity. Aug 28 2024
E1965 NST-628 NST-628 is a potent and well-tolerated single-agent inhibitor of both RAF and MEK. It acts as a pan-RAF–MEK molecular glue that blocks the phosphorylation and activation of MEK by RAF. Aug 28 2024
E1989 ART0380 ART0380 (IACS-030380) is a potent and selective, orally bioavailable inhibitor of ATR kinase, with an IC50 of 51.7 nM effectively inhibiting the enzyme activity of the ATR-ATRIP complex. It functions as an ATP-competitive inhibitor, binding to the ATP pocket of ATR, where ATP would typically bind. It interacts with the hinge through its morpholine oxygen and occupies the ribose pocket with a sulfoximine group. It also exhibits antitumor activity. Aug 28 2024
E4609 Amredobresib Amredobresib (BI894999) is an oral inhibitor of BET, which acts as an acetyl-lysine mimic. It prevents the bromodomains BRD4-BD1 and BRD4-BD2 from binding to acetylated histones, with an IC50 of 5 nM for BRD4-BD1 and 41 nM for BRD4-BD2. Aug 28 2024
E4847 Tosufloxacin Tosufloxacin (A-61827) is an orally active fluoroquinolone antibiotic. Tosufloxacin effectively targets a broad spectrum of antibacterial activity, including both gram-positive and gram-negative strains. Aug 28 2024
E4839 Ziprasidone Ziprasidone(CP-88059,Geodon,Zeldox) is an orally active agonist of 5-HT(1A) receptor. It has high affinity for dopamine D2, D3, 5-hydroxytryptamine 5HT2A, 5HT2C, 5HT1A, 5HT1D, α-adrenergic receptors Aug 28 2024
E4892 Formoterol Formoterol is a highly selective and potent long-acting beta2-adrenergic agonist that functions by binding to and activating beta2-adrenergic receptors on the smooth muscle cells of the airways. It is used in the treatment of patients with chronic obstructive pulmonary disease (COPD). Aug 28 2024
E4898 Escitalopram Escitalopram ((S)-Citalopram), (S)-+ Citalopram)) is a selective serotonin reuptake inhibitor (SSRI) with a Ki value of 0.89 nM. Escitalopram has approximately 30-fold higher binding affinity than its R(-)-enantiomer and exhibits selectivity over both norepinephrine transporter (NET) and dopamine transporter (DAT). Aug 28 2024
E4889 Glafenine Glafenine (Glafenin) is a non-steroidal anti-inflammatory drug (NSAID) and is a non-narcotic analgesic agent that not only acts as a proteostasis modulator but is also one of the most potent NSAID correctors of F508del-CFTR. It exhibits COX-2 inhibition in the arachidonic acid pathway and rescues class 2 CFTR mutants. Aug 28 2024
E4619 Basimglurant Basimglurant(RG7090, CTEP Derivative) is a potent and selective negative allosteric modulator of mGlu5, with a Kd of 1.1 nM, It inhibits the function of mGluR5, thereby regulating glutamatergic neurotransmission. Aug 26 2024
E4879 Laninamivir Laninamivir(R-125489) is a potent inhibitor of influenza neuraminidase(NA)with IC50s of 0.90 nM, 1.83 nM and 3.12 nM for avian H12N5 NA (N5), pH1N1 N1 NA (p09N1) and A/RI/5+/1957 H2N2 N2 (p57N2), respectively. It exhibits long-acting anti-influenza virus activity. Aug 26 2024
E2987 GCN2-IN-1 GCN2-IN-1 (A-92) is a specific and potent active site inhibitor of general control nonderepressible 2 kinase (GCN2) with an IC50 of <0.3 μM. It can be investigated in research related to diseases involving retroviral integration. Aug 26 2024
E4906 Cefadroxil Cefadroxil(BL-S 578) is a first-generation, cephalosporin antibiotic with broad spectrum of anti-bacterial activity. It can be used in the management of infections in the respiratory tract, urinary tract, skin and soft tissues, and bones and joints. Aug 26 2024
E4869 Niraparib hydrochloride Niraparib hydrochloride (MK-4827 hydrochloride) is a potent poly(ADP-ribose)polymerase (PARP) inhibitor with IC50s of 3.8 and 2.1 nM against both the PARP-1 and PARP-2 enzymes, respectively.It inhibits the repair of radiation-induced DNA double-strand breaks, activates apoptosis, and exhibits anti-tumor activity. Aug 26 2024
E4878 Lansoprazole sodium Lansoprazole Sodium, a sodium salt form of Lansoprazole, is an orally active inhibitor of proton pump, preventing the stomach from producing acid. Lansoprazole enhances the expression and transcriptional effectiveness of runt-related transcription factor 2 (Runx2), stimulating osteoprogenitor cell's commitment and differentiation toward their lineage. Aug 22 2024
E1859 FHD-609 FHD-609 acts as a selective inhibitor and degrader of BRD9 protein (bromodomain-containing protein 9). FHD-609 targets ncBAF and can be used in research of various cancers involving mutations in a BAF complex subunit. Aug 22 2024
P1230 Retatrutide Retatrutide (LY3437943) acts as a triple agonist peptide of the glucagon receptor (GCGR), glucagon-like peptide-1 receptor (GLP-1R) and glucosedependent insulinotropic polypeptide receptor (GIPR). Retatrutide binds to human GCGR, GLP-1R, and GIPR with EC50 values of 5.79, 0.775 nM, and 0.0643, respectively. Retatrutide has the potential for use in research on obesity. Aug 22 2024
E1771 Cycloleucine Cycloleucine is a specific antagonist of NMDA receptor(N-methyl-D-aspartate receptor coupled glycine receptor), with a Ki of 600 μM. Cycloleucine also acts as a specific inhibitor of S-adenosyl-methionine-mediated methylation. Cycloleucine exhibits cytostatic effects. Aug 22 2024
E4887 Dapoxetine Dapoxetine ((S)-(+)-Dapoxetine; LY-210448) is a selective serotonin reuptake inhibitor (SSRI) with oral activity. Dapoxetine is a short-acting SSRI developed specifically for the treatment of premature ejaculation (PE). Aug 22 2024
E4853 Rolapitant hydrochloride hydrate Rolapitant hydrochloride hydrate(SCH619734 hydrochloride hydrate) is a long-acting, extremely selective antagonist of the Nk-1 receptor antagonist (NK-1RA) with antiemetic activity. It significantly penetrates the central nervous system (CNS) and used clinically to prevent chemotherapy-induced nausea and vomiting (CINV) in cancer patients undergoing high and moderate emetogenic chemotherapy. Aug 21 2024
E4867 Omadacycline Omadacycline(Amadacycline) is an oral aminomethylcycline antibacterial antibiotic used to treat moderate-to-severe infections, such as community-acquired pneumonia and acute bacterial skin and skin structure infections caused by susceptible organisms. It inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit. Omadacycline has broad-spectrum antibacterial activity and is effective against Gram-positive and Gram-negative aerobic, anaerobic, and atypical bacteria. Aug 21 2024
E4685 Iclepertin Iclepertin(BI-425809) is a potent and selective inhibitor of glycine transporter 1 (GlyT1) that increases glycine levels in the cerebrospinal fluid (CSF). Aug 21 2024
S8687 MPP dihydrochloride Methyl-piperidino-pyrazole (MPP) dihydrochloride is a highly selective antagonist for estrogen receptor alpha (ERα), with an affinity 200 times greater than for estrogen receptor beta (ERβ). It inhibits 17β-estradiol binding to ERα by inducing conformational changes that alter the receptor’s binding site and also increases the energy required for genistein's interaction with ERα. Aug 21 2024
E4610 SMIP34 SMIP34 is a small molecule inhibitor of proline, glutamic acid, and leucine-rich protein 1 (PELP1). It is effective in reducing cell viability, reducing invasion, and inducing apoptosis in Triple-negative breast cancer (TNBC) models. Aug 20 2024
E4655 VT104 VT104 is an inhibitor of TEAD auto-palmitoylation that effectively blocks the palmitoylation of TEAD1 and TEAD3 proteins. It selectively inhibits YAP/TAZ-TEAD-promoted gene transcription and exhibits strong antitumor and anti-proliferative effects. Aug 20 2024
E1964 BMS-986365 BMS-986365 (CC-94676) is a potent and selective, heterobifunctional ligand-directed degrader (LDD) and antagonist of androgen receptor (AR), that effectively targets both wildtype and mutant forms of the androgen receptor (AR) in the cytoplasm and nucleus. It rapidly degrades AR, suppresses AR signaling, and shows promising clinical activity in inhibiting tumor growth in patients with metastatic castration-resistant prostate cancer (mCRPC). Aug 18 2024
E1899 INCB059872 dihydrochloride INCB059872 dihydrochloride is a potent, selective, and irreversible inhibitor of Lysine-Specific Demethylase 1(LSD1). It exhibits potential antineoplastic activity and can be used in acute myeloid leukemia (AML) research. Aug 18 2024
E4877 Lefamulin Lefamulin (BC-3781), is a pleuromutilin antibiotic, inhibits protein synthesis by binding to the peptidyl transferase center of the 50S bacterial ribosome. It is effective against a range of gram-positive pathogens involved in community-acquired bacterial pneumonia (CABP), including Streptococcus pneumoniae, Haemophilus influenzae, Mycoplasma pneumoniae, Legionella pneumophila, Chlamydophila pneumoniae, Staphylococcus aureus (including methicillin-resistant and vancomycin-intermediate strains), and vancomycin-resistant Enterococcus faecium. Aug 18 2024
S8143 Mavoglurant Mavoglurant (AFQ056) is a structurally selective, non-competitive antagonist of mGlu5 receptor with an IC50 of 30 nM. It exhibits efficacy in treatment of L-dopa induced dyskinesia in Parkinson's disease and Fragile X syndrome. Aug 18 2024
E1847 GBD-9 GBD-9 is a double-mechanism efficient degrader of BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). GBD-9 acts both as a PROTAC molecule to induce the degradation of BTK and as a molecular glue to degrade GSPT1.It exhibits anti-proliferative effects, inhibiting cancer cell survival. Aug 15 2024
E1683 DN02 DN02 is a selective probe of BRD8 bromodomain family. It exhibits potency against BRD8(1) with a Kd of 32 nM, and interestingly, demonstrated this activity to be selective over BRD8's second bromodomain (BRD8(2) with a Kd of >1000 nM) Aug 15 2024
E4843 Vardenafil dihydrochloride Vardenafil dihydrochloride is a potent, and selective inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. It also exhibits inhibition of PDE1 and PDE6 with IC50 of 180 nM and 11 nM respectively. It can be used for the research of erectile dysfunction, hepatitis, diabetes. Aug 15 2024
E1612 Suzetrigine VX-548 (Suzetrigine), is an oral, highly selective inhibitor of voltage-gated sodium channel 1.8 (NaV1.8) with an IC50 of 0.7 nM. It can be used in research of transmitting nociceptive signals and treatment of acute pain after abdominoplasty or bunionectomy. Aug 15 2024
E1951 X5050 X5050 is a benzoimidazole-5-carboxamide derivative and a potent inhibitor of repressor element-1 silencing transcription factor (REST) with an EC50 of 2.1 μM. It can be used in research of Huntington's disease and other neurodegenerative disorders characterized by altered BDNF levels. Aug 15 2024
E4858 Rimonabant hydrochloride Rimonabant hydrochloride (SR 141716A hydrochloride) is a highly potent and selective antagonist of the central cannabinoid receptor (CB1) , with a Ki of 1.8 nM. It is an anorectic anti-obesity drug with potential to treat obesity and cardiovascular risk factors. Aug 15 2024
E4842 Vilanterol Vilanterol (GW642444) is a potent and selective agonist of β2-adrenoceptor (β2-AR) with pEC50 of β2-AR, β1-AR, and β3-AR is 10.37, 6.98 and 7.36 respectively in cAMP detection assays. Aug 15 2024
E4846 Treprostinil Treprostinil is a potent agonist of DP1 and EP2  with EC50 of 0.6 nM and 6.2 nM for DP1 and EP2 receptors, respectively. It is a vasodilator used to treat pulmonary arterial hypertension and improves mitochondrial impairment in vitro. Aug 15 2024
E1997 GLPG3970 GLPG3970 (compound 32) is a dual inhibitor of SIK2 and SIK3, with IC50 of 282.8 nM, 7.8 nM and 3.8 nM for SIK1, SIK2 and SIK3, respectively. It has the potential to treat autoimmune and inflammatory diseases. Aug 15 2024
E4870 Naratriptan Naratriptan is an agonist of 5-hydroxytryptamine1B/D (5-HT1B/D) receptors, which reduces the frequency of cluster headache. Aug 15 2024
E4866 Paroxetine Paroxetine is a potent and selective serotonin reuptake inhibitor (SSRI) used to treat depression and anxiety disorders. It inhibits pyroptosis and reduces osteoclast formation by blocking the NF-κB signalling pathway. Aug 15 2024
E1560 Raptinal Raptinal is a pro-apoptotic compound that induces apoptosis by promoting the release of cytochrome c from the mitochondria, thereby activating the intrinsic apoptotic pathway. It also inhibits the activity of caspase-activated Pannexin 1 (PANX1), a ubiquitously expressed transmembrane channel involved in regulating various cell death-associated processes. Aug 15 2024
E4868 Olsalazine Olsalazine is a salicylic acid-derived anti-inflammatory agent used to treat ulcerative colitis. Aug 15 2024
E4852 Tafamidis meglumine Tafamidis meglumine (Vyndaqel, Fx-1006A) stabilizes the tetrameric structure of transthyretin (TTR) by binding to thyroxine-binding sites. Tafamidis meglumine treats transthyretin familial amyloid polyneuropathies (TTR-FAP), a condition characterized by neurological damage from TTR amyloidosis, by preventing the misfolding and aggregation of transthyretin (TTR) into amyloid fibrils. Aug 12 2024
E1902 Nedometinib Nedometinib (NFX-179) is a highly specific and potent inhibitor of MEK1 with an IC50 of 135 nM. It also results in suppression of p-ERK levels and can be used in research and treatment of cutaneous neurofibromas (cNFs) associated with neurofibromatosis type 1 (NF1). Aug 12 2024
E1355 JNJ-64264681 JNJ-64264681 is an orally active, irreversible covalent inhibitor of Bruton's tyrosine kinase (BTK) with potent whole blood activity and exceptional kinome selectivity. It exhibits potential efficacy in treatment for B-cell malignancies and autoimmune disorders. Aug 12 2024
S5788 Tacrolimus monohydrate Tacrolimus monohydrate (Tacrolimus, FK506) is a macrolide antibiotic that primarily acts as an inhibitor of calcineurin phosphatase by binding to FK506 binding protein (FKBP). This inhibition blocks calcium-dependent processes, including interleukin-2 gene transcription, nitric oxide synthase activation, cell degranulation, and apoptosis, and also has immunosuppressive, neuroregenerative and neuroprotective properties. Aug 12 2024
E4854 Sodium picosulfate monohydrate Sodium picosulfate monohydrate, is a polyphenolic stimulant laxative and prodrug form of desacetyl bisacodyl (DAB). It is used for treating idiopathic constipation and preparing the bowel before colonoscopy. Aug 07 2024
E1978 Zelasudil Zelasudil (RXC007) is a selective inhibitor of Rho-associated coiled-coil-containing kinase 2 (ROCK2). It has been found to have the antifibrotic effect. Aug 07 2024
E4865 Noradrenaline bitartrate Noradrenaline bitartrate (Norepinephrine Bitartrate) is a central nervous system (CNS) neurotransmitter and stimulator of β1 adrenergic receptors and α-adrenergic receptors, causing increased contractility and heart rate, as well as vasoconstriction. Aug 07 2024
E4851 Tandospirone citrate Tandospirone citrate, is a potent, selective and a partial agonist of the 5-HT1A receptor. It exhibited good permeability in the intestine, with passive diffusion being the main mode of drug absorption, it also has anxiolytic effects and can be used in generalized anxiety disorder treatments. Aug 07 2024
E4840 Ziprasidone hydrochloride monohydrate Ziprasidone hydrochloride monohydrate is an antipsychotic drug, a combined antagonist of 5-HT (serotonin) and dopamine receptor. It exhibits binding affinities for D2, 5-HT2A, 5-HT1A with Ki values 4.8 nM, 0.42 nM, 3.4 nM respectively. Aug 07 2024
E1777 RIG012 RIG012 is a potent antagonist of Retinoic Acid Inducible Gene 1 (RIG-I), an innate immune receptor, with an IC50 of 0.71 μM in the NADH-coupled ATPase assay. It effectively blocks RIG-I-initiated signaling and inflammatory responses induced by SARS-CoV-2 RNA. Aug 07 2024
E4663 INF195 INF 195 is an NLRP3 inhibitor which inhibits NLRP3-driven macrophage pyrodeath and IL-1β release. At low dose, INF 195 can reduce the infarct size of isolated mouse hearts and effectively prevent myocardial ischemia/reperfusion injury. Aug 07 2024
E4855 Sertaconazole Sertaconazole(FI-7045) is an imidazole-type antifungal agent that inhibits ergosterol biosynthesis by inhibiting the cytochrome P450-dependent 14α-lanosterol demethylase or Erg11p. This inhibition disrupts fungal cell membrane integrity, ultimately leading to fungal cell death. Sertaconazole is used in the topical treatment of superficial mycoses. Aug 07 2024
E4616 Buloxibutid Buloxibutid (AT2 Agonist C21) is a selective agonist of angiotensin II type 2 receptor (AT2R) with a Ki value of 0.4 nM for the AT2 receptor and a Ki >10 µM for the AT1 receptor. Its treatment significantly reduces vascular remodelling, improves hemodynamics, and decreases pulmonary collagen deposition in the Sugen-Hypoxia model of pulmonary hypertension. Aug 07 2024
S8625 GNE-049 GNE-049 is a highly potent and selective inhibitor of CBP. It exhibits an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also effectively inhibits BRET and BRD4 with IC50 values of 12 nM and 4200 nM, respectively. Aug 06 2024
E4856 Rotigotine Hydrochloride Rotigotine Hydrochloride (N-0923 Hydrochloride) is a potent Agonist of dopamine receptor, with Ki values of 0.71 nM for dopamine D3 receptor, 4-15 nM for D2, D5, D4 receptors, and 83 nM for dopamine D1 receptor. It also acts as a partial agonist of the 5-HT1A receptor, and as an antagonist of the α2B-adrenergic receptor. Aug 06 2024
E1041 SY-5609 SY-5609 (CDK7-IN-3) is an orally active and highly selective inhibitor of CDK7 with a KD value of 0.065 nM. SY-5609 exhibits poor inhibition on CDK2, CDK9, CDK12. SY-5609 displays antitumor activity and can induce apoptosis in tumor cells. Aug 06 2024
E1823 Ninerafaxstat trihydrochloride Ninerafaxstat trihydrochloride (MB-1018972 trihydrochloride, IMB-101 trihydrochloride) acts as a competitive inhibitor of 3-ketoacyl-CoA thiolase (3-KAT) to partially suppress fatty acid oxidation. It is an orally active cardiac mitochondrial drug that restores myocardial energy homeostasis. Ninerafaxstat trihydrochloride regulates myocardial substrate utilization and improves cardiac efficiency. Ninerafaxstat trihydrochloride is also used in research of cardiovascular diseases. Aug 06 2024
E4850 Tazemetostat hydrobromide Tazemetostat hydrobromide (EPZ-6438 hydrobromide) is a potent, selective, and orally available inhibitor of EZH2. It inhibits EZH2 with IC50 values of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide also inhibits EZH1 with an IC50 of 392 nM. Aug 06 2024
E1565 Iruplinalkib Iruplinalkib (WX-0593) is a highly selective oral inhibitor of ALK and ROS1 tyrosine kinase. It exhibits potent and promising antitumor activity in advanced non-small cell lung cancer (NSCLC) with ALK or ROS1 rearrangement. Aug 01 2024
E4632 Taminadenant Taminadenant (NIR178, PBF509) is a non-xanthine and non-furan antagonist of adenosine A2A receptor (A2AR). It can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with Kb values of 72.8 nM and 8.2 nM, respectively. It exhibits potential utility for Parkinson’s disease (PD) treatment. Aug 01 2024
E4636 W-7 hydrochloride W-7 hydrochloride is a potent antagonist of calmodulin (CaM) that inhibits Dengue virus (DENV) translation and replication. It also competitively inhibits Trypsin-treated Ca2+/calmodulin-dependent phosphodiesterase (Ca2+-PDE). It exhibits anti-proliferative and anti-tumor effect. Aug 01 2024
E1426 EAPB02303 EAPB02303 is a second-generation imiqualine that acts as a microtubule -disruptingagent and demonstrates anti-tumor effects and reduces tumor size in human melanoma xenografts. Aug 01 2024
E4841 Vorapaxar sulfate Vorapaxar sulfate (SCH 530348 sulfate) is a selective and orally active antagonist of protease-activated receptor (PAR-1), with a Ki value of 8.1 nM. Vorapaxar sulfate reduces thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner. Aug 01 2024
E4838 Cefuroxime Cefuroxime (Kefurox) is an orally active, second-generation, broad-spectrum cephalosporin antibiotic with increased stability to β-lactamase. Cefuroxime exhibits broad-spectrum activity against Gram-positive bacteria including penicillinase-producing staphylococci and non-β-lactamase-producing gram-negative bacteria. Aug 01 2024
E1403 Fumarate hydratase-IN-1 Fumarate hydratase-IN-1 is a small molecule cell-permeable inhibitor of fumarate hydratase. It induce alteration of TCA cycle metabolites, modulation of cytosolic processes, and substantial redox stress responses. Jul 29 2024
P1242 Proteinase K Proteinase K is a serine endoprotease, is used for isolating amyloid cores and is effective over a wide pH range (4–12), including in the presence of SDS or urea. It is commonly used as a preparative reagent for destruction of proteins, including DNAses and RNAses, in DNA and RNA preparations. Jul 29 2024
E1611 Atuzabrutinib Atuzabrutinib (SAR 444727, PRN473) is a reversible, selective inhibitor of Bruton's tyrosine kinase (Btk). It can effectively prevent neutrophil recruitment via inhibition of macrophage antigen‐1 signalling. Jul 25 2024
E1791 Zongertinib Zongertinib (BI 1810631, BI 764532) is a selective and potent inhibitor of human HER2 and EGFR tyrosine kinase that covalently binds to both wild-type and mutated HER2 receptors, including exon 20 insertion mutations, while sparing EGFR signaling. It exhibits effective and tolerable oral treatment for patients with HER2 aberration-positive solid tumors. Jul 25 2024
E1931 AD-5584 AD-5584 is a specific inhibitor of human acyl-CoA synthetase short chain family member 2 (ACSS2). It significantly reduces lipid storage, decreases colony formation, and increases cell death in vitro, while also confirming blood-brain barrier (BBB) permeability. Jul 25 2024
E1533 Lipofermata Lipofermata is an inhibitor of fatty acid transport protein 2 (FATP2) that demonstrates fatty acid transport inhibition with an IC50 of 4.84 μM in Caco-2 cells. It may offer therapeutic potential for diseases where lipotoxicity is a key factor. Jul 25 2024
E1877 BLU 451(LNG-451) BLU 451 (LNG-451) is a central nervous system (CNS)-penetrant, wild-type EGFR-sparing, covalent inhibitor of epidermal growth factor receptor (EGFR) exon 20 insertion (Ex20ins) with an IC50 of 7-78 nM. It also exhibits a potent anti-tumor efficacy. Jul 24 2024
E4827 Diphenhydramine Diphenhydramine is a first-generation antihistamine and sedative that acts as an antagonist of the H1 receptor and is used for treating acute allergic reactions. It is FDA-approved as an adjunct to epinephrine and corticosteroids and exhibits anticholinergic and antiemetic effects. Jul 23 2024
E1889 PCO371 PCO371 is a nonpeptidyl, orally active agonist of Parathyroid hormone type 1 receptor (PTHR1). It stimulates cAMP production in COS-7 cells with an EC50 of 2.4 μmol/L. It also acts as an osteoporosis drug and significantly enhances bone mineral density (BMD) and bone strength in the lumbar vertebrae of osteopenic ovariectomized (OVX) rats. It also restores normal serum calcium levels without increasing urinary calcium in hypocalcemic thyroparathyroidectomized (TPTX) rats. Jul 23 2024
E1985 YD23 YD23 is a PROTAC which induces the degradation of SMARCA2. It reduces chromatin accessibility in SMARCA4-deficient cells, affecting gene enhancers related to cell cycle and growth regulation, which leads to the downregulation of several cell cycle genes. It also selectively inhibits the growth of SMARCA4 mutant lung cancer cells in vitro. Jul 23 2024
E4835 Sumatriptan Sumatriptan (GR43175) is a selective agonist of 5-HT1D receptor, which is effectively used in the acute treatment of migraine. It causes a vasopressor response in the systemic and pulmonary arterial circulations and coronary artery vasoconstriction. Jul 23 2024
E4836 Bupivacaine Bupivacaine is a potent local anesthetic and sodium channel blocker used for local infiltration, nerve block, epidural, and intrathecal anesthesia. It significantly reduces cell viability and induces apoptosis. It also stimulates the production of ROS and activates MAPK pathways, which increases the expression of WDR35 in mouse neuroblastoma Neuro2a cells. It also activates NF-κB and c-Jun/AP-1 signalling pathways in Neuro2a cells. Jul 23 2024
E1961 NVL-655 NVL-655 is a selective inhibitor of anaplastic lymphoma kinase (ALK), with potential antineoplastic activity in the Ba/F3 xenograft model. It also exhibits significant inhibitory activity against ROS1, LTK, PYK2, TRKB, and FAK, with an IC50 ≤10-fold ALK and demonstrates high potency against specific ALK mutations, with an IC50 of <0.73 nM, 7 nM, 3 nM, 3 nM for G1202R, G1202R/L1196M, G1202R/G1269A and G1202R/L1198F respectively. Jul 23 2024
E1015 Angiotensin II human Angiotensin II human is a potent vasoconstrictor that induces angiogenesis by activating angiotensin II type 1 (AT1) receptor, which increases the production of vascular endothelial growth factor (VEGF) in a redox-sensitive manner and promotes the formation of capillaries from endothelial cells through the LOX-1-dependent redox-sensitive pathway. Jul 23 2024
E4837 Trimethoprim (lactate) Trimethoprim (lactate) is an antifolate antibacterial agent that inhibits bacterial dihydrofolate reductase (DHFR), an essential enzyme responsible for the production of tetrahydrofolic acid (THF). By blocking this enzyme, trimethoprim prevents the synthesis of bacterial DNA, hindering bacterial survival. It is a standard antibiotic for treating urinary tract infections (UTIs). Jul 23 2024
E4647 Aticaprant Aticaprant (CERC-501, LY-2456302) is a potent, orally bioavailable, centrally-penetrant antagonist of the kappa opioid receptor with a Ki of 0.807 nM. It exhibits an antidepressant effect with the potential to treat major depressive disorder (MDD). Jul 23 2024
E1957 NX-1607 NX-1607 (Cbl-b-IN-3) is an oral inhibitor of Casitas B-lineage lymphoma proto-oncogene B (CBL-B), which is an E3 ubiquitin ligase and a key regulator of T, NK, and dendritic cell activation and suppresses their anti-tumor functions. NX-1607 enhances antigen recall, reduces T cell exhaustion, and increases cytokine production in response to T cell receptor stimulation, thereby counteracting suppressive signals from the tumor microenvironment. Jul 23 2024
E4826 L-Ornithine L-aspartate L-ornithine-L-aspartate (LOLA) is a stable salt composed of two natural nonessential L-amino acids: ornithine and aspartic acid. It effectively lowers blood ammonia concentration by enhancing ammonia detoxification in the muscles, and alleviating hepatic encephalopathy symptoms in liver cirrhosis. Jul 19 2024
E4822 Tacrine Tacrine is a potent acetylcholinesterase (AChE) inhibitor. It inhibits acetylcholinesterase(AChE) and butyrylcholinesterase(BChE) with an IC50 of 77 nM and 69 nM, respectively. It is used in the treatment of Alzheimer's disease (AD), also poisoning topoisomerases and inhibiting in vivo (mitochondrial)mtDNA synthesis. Jul 19 2024
E4832 DL-Alanine DL-alanine (DL-2-Aminopropionic acid) is a racemic mixture of L- and D-alanine that forms complexes with transition metals like Cu(II), Zn(II), and Cd(II). It also plays a key role in the glucose-alanine cycle between tissues and the liver. Jul 19 2024
E4831 L-Arginine (L-glutamate) L-Arginine (L-glutamate) (Arginine glutamate) is a mixture of amino acids that induces apoptosis via hypertonic stress. It also promotes gastric relaxation by providing L-arginine for nitric oxide production, thereby benefiting gastrointestinal motility and conditions associated with vagus nerve dysfunction. Jul 19 2024
E4830 Guanidine thiocyanate Guanidine thiocyanate is a potent inhibitor of nucleases and a powerful denaturant of proteins. It is used for RNA isolation due to its strong chaotropic properties, which effectively denature RNase enzymes in samples, ensuring RNA stability and purity during extraction processes. Nucleic acid extraction buffers containing guanidine thiocyanate effectively deactivate high-titer polioviruses found in potentially infectious materials. Jul 19 2024
E4825 Naphazoline (nitrate) Naphazoline (nitrate) is a agonist of peripheral α2-adrenergic receptor and used as a topical decongestant. It also acts as a vasoconstrictor that effectively reduces intraoperative bleeding and enhances postoperative analgesia. When used in conjunction with intranasal lidocaine, it significantly reduces both intra- and postoperative pain, thereby decreasing the need for rescue analgesics in the postoperative period following septorhinoplasty. Jul 19 2024
E4828 Cloperastine fendizoate Cloperastine fendizoate (Hustazol) is a sedative used to relieve cough and also has a peripheral action that desensitizes the afferent nerves in the tracheobronchial region. It inhibits the hERG K+ currents in a concentration-dependent manner, with an IC50 value of 0.027 μM. Jul 19 2024
E4824 Hydroxychloroquine Hydroxychloroquine (HCQ) is an antimalarial drug that inhibits autophagy and is used to treat systemic lupus erythematosus (SLE) and rheumatoid arthritis (RA). It exhibits immunomodulatory, antithrombotic, and antiplatelet properties. It inhibits the release endothelin-1, a potent vasoconstrictor, and restores impaired angiogenesis in TNF-α-treated endothelial cells in vitro. It also reduces the production of inflammatory cytokines such as TNF-α, IFN-γ, and IL-6 from peripheral blood mononuclear cells, upregulates IL-10 and decreases platelet aggregation. Jul 19 2024
E4806 Quinine dihydrochloride Quinine dihydrochloride is an antiparasitic used to treat malaria and is particularly important for managing malaria during the first trimester of pregnancy. It inhibits Slo3 (KCa 5.1) channel, which are a significant part of the mammalian KSper (sperm potassium conductance), by binding to hydrophobic side chains located at the intracellular region of the channel pore. Jul 19 2024
E1885 LY3522348 LY3522348 is a highly selective oral dual inhibitor of the human ketohexokinase isoforms C and A, with IC50 values of 20nM for hKHK-C and 24nM for hKHK-A. It shows a significant pharmacodynamic effect in a mouse model of fructose metabolism. Jul 19 2024
E1686 SW-100 SW-100 is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 2.3 nM. It displays 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. Jul 18 2024
E4630 Ilginatinib hydrochloride Ilginatinib hydrochloride (NS-018 hydrochloride) is a potent small-molecule inhibitor of JAK2 that is competitive with adenosine triphosphate (ATP) which exhibits 30–50-fold greater selectivity for JAK2 over other Jak-family kinases such as JAK1, JAK3, and TYK2.It inhibits JAK2, JAK1, JAK3, and TYK2 with IC50 of 0.72 nM, 33 nM, 39 nM, and 22 nM, respectively. It also showed potent inhibition of Src-family kinases, SRC and FYN. It can be used in research of myeloproliferative neoplasms. Jul 18 2024
E4823 Pargyline Pargyline is an irreversible selective inhibitor of monoamine oxidase (MAO) with Kis of 13 μM and 0.5 μM for MAO-A and MAO-B respectively. It has pharmaceutical potential as an anticancer drug for human prostate cancer. Jul 18 2024
E4829 Bismuth subnitrate Bismuth subnitrate is an antigastric ulcer and antidiarrheic agent that induces metallothionein (MT). It can be used as an adjunct in cancer chemotherapy to induce MT in target organs. Jul 18 2024
P1241 Bromelain Bromelain is an aqueous extract of pineapple that is composed of 95%-mixture of proteases, acting as an inhibitor of Prostaglandin E2 (PGE2) and Cox-2. It exhibits potent anti-inflammatory, anti-thrombotic, fibrinolytic and anti-cancer functions. Jul 18 2024
E4592 UGT8-IN-1 UGT8-IN-1 is a brain-penetrable and orally active inhibitor of ceramide galactosyltransferase enzyme (UGT8). UGT8-IN-1 targets sulfatide metabolism resulting in ceramide-induced lethal mitophagy and subsequent cancer cell death in vitro, and reduces tumour growth in mutant Kras; Gnas allografts. Jul 16 2024
E1966 VVD-214 VVD-214 (RO7589831, VVD-133214) is a synthetic allosteric inhibitor of WRN helicase. VVD-214 binds irreversibly to cysteine 727 on WRN, suppressing ATP hydrolysis and helicase activity. VVD-214 exhibits potent efficacy in inducing double-stranded DNA breaks, nuclear enlargement, and cellular apoptosis in cancers with high microsatellite instability (MSI). Jul 15 2024
E1970 BAL-0028 BAL-0028 (Compound 3), which belongs to the indazole class is an inhibitor of NLRP3 activation with an IC50 value of 25 nM. BAL-0028 binds tightly to the NACHT domain of NLRP3, with KD values ranging from 104 to 123 nM. BAL-0028 also exhibits anti-inflammatory activity. Jul 15 2024
E1186 Tenapanor Tenapanor (AZD1722, RDX5791) is a potent and orally active inhibitor of sodium/hydrogen exchanger isoform 3 (NHE3). It exhibits an IC50 of 2 and 6 nM in human and mouse ileum monolayers, respectively. Tenapanor reduces intestinal phosphate absorption predominantly by reducing passive paracellular phosphate flux. Jul 15 2024
E4821 Simvastatin acid (ammonium) Simvastatin acid (Tenivastatin) ammonium is a potent inhibitor of HMG-CoA reductase (HMGCR). Simvastatin acid ammonium also decreases Indoxyl sulfate-induced reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium regulates the expression of OATP3A1 in cardiomyocytes. Jul 15 2024
E4820 Sulbactam pivoxil Sulbactam pivoxil (CP 47904), a proagent of sulbactam, is an inhibitor of β-lactamase. Sulbactam pivoxil provides higher absorption than its parent compound and achieves high serum levels following oral administration. Jul 15 2024
E4818 Pemetrexed (disodium heptahydrate) Pemetrexed (disodium heptahydrate) is a folate antimetabolite that inhibits thymidylate synthase, dihydrofolate reductase and glycinamide ribonucleotide formyltransferase. It also induces apoptosis and cell-cycle arrest in non-small-cell lung cancer carrying an EGFR exon 19 deletion. Jul 14 2024
E1290 Ziftomenib Ziftomenib (KO-539) is an oral inhibitor of menin targeting the menin–KMT2A protein-protein interaction. It exhibits antileukemic activity and induces apoptosis of acute myeloid leukemia(AML) cells. Jul 11 2024
E4819 Afatinib free base Afatinib free base (Gilotrif, BIBW2992, Boehringer Ingelheim) is a second-generation tyrosine kinase inhibitor (TKI) that irreversibly inhibits EGFR and HER2, with IC50 of 0.5 nM, 0.4 nM, 14 nM and 1 nM for wild-type EGFR, EGFR-L858R, HER2, ErbB4, respectively. Jul 11 2024
E1867 NPD4928 NPD4928 is an inhibitor of Ferroptosis Suppressor Protein 1 (FSP1) that enhances ferroptosis. It enhances the cytotoxic effects on various cell types when combined with GPX4 antagonists. Jul 11 2024
E4816 Choline hydroxide, 42.5 wt.% in water Choline hydroxide, 42.5 wt.% in water, is a strong organic base used as a metal-free, nontoxic, and water-soluble catalyst. It facilitates the synthesis of 1,8-naphthyridine derivatives while avoiding the use of hazardous or carcinogenic organic solvents. Jul 10 2024
E1975 HC-7366 HC-7366, is a First-in-Human modulator of General controlled nonderepressible 2 (GCN2) that activates GCN2. It demonstrates anti-metastatic efficacy, reducing lung metastases and exhibits anti-tumor activity. Jul 09 2024
A2163 Anti-mouse IL-12 p40-InVivo Anti-mouse IL-12 p40-InVivo reacts with mouse p40 also known as IL-12β. p40 is a 40 kDa subunit of IL-12 and IL-23. IL-12 is a heterodimeric cytokine composed of subunits IL-12α p35 and IL-12β p40. Jul 09 2024
A2164 Anti-mouse B220-InVivo Anti-mouse B220-InVivo reacts with mouse B220 also known as CD45R. B220 is a 220 kDa transmembrane protein tyrosine phosphatase expressed on B cells and some subsets of T and NK cells. Jul 09 2024
E4805 Methylene Blue trihydrate Methylene blue trihydrate (C.I. Basic Blue 9 trihydrate) acts as an inhibitor of soluble guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS). Methylene blue trihydrate exhibits antimalarial, antidepressant, and anxiolytic activity effects. Methylene Blue trihydrate has potential applications in treating methemoglobinemia, neurodegenerative disorders, and ifosfamide-induced encephalopathy. Jul 08 2024
E4807 Dexketoprofen trometamol Dexketoprofen trometamol (Dexketoprofen tromethamine salt) is an orally active non-selective inhibitor of COX. Dexketoprofen trometamol exhibits analgesic efficacy and can be used in treating acute pain. Jul 08 2024
E4811 Levofloxacin hydrochloride Levofloxacin hydrochloride ((-)-Ofloxacin hydrochloride), a synthetic fluoroquinolone antibiotic, is an inhibitor of DNA gyrase and Topoisomerase IV. It exhibits bactericidal effects by preventing bacterial DNA replication. Jul 08 2024
E4812 Fluoxetine Fluoxetine (LY-110140 free base) is a selective 5-hydroxytryptamine (5-HT) reuptake inhibitor. Fluoxetine is used widely in the treatment of depression, anxiety-related symptoms and also displays anticonvulsant activity. Jul 08 2024
E1987 APX2009 APX2009 is a second-generation redox-specific inhibitor of APE1/Ref-1, an essential enzyme in the base excision repair (BER) pathway. APX2009 effectively reduces breast cancer cell proliferation and colony formation. Jul 08 2024
E1944 INS018-055(ISM001-055) INS018-055 (ISM001-055, TNIK&MAP4K4-IN-2, compound 112) is an inhibitor of TNIK and MAP4K4. It exhibits an IC50 values of 12-120 nM on TNIK. Jul 08 2024
E1854 INX-315 INX-315 is an orally active and selective inhibitor of CDK2 that induces cell cycle arrest in the G1 phase. It exhibits an IC50 value of 2.3 nM in intracellular NanoBRET assay, respectively. It displays a 50-fold increased CDK2 selectivity compared to CDK1. INX-315 decreases the phosphorylation of CDK2 substrates and suppresses tumor growth in xenograft mouse models in a dose-dependent manner. Jul 05 2024
E1900 Simnotrelvir Simnotrelvir(SIM0417, SARS-CoV-2-IN-41) is an inhibitor of coronavirus main proteinase (3CLpro) (SARS-CoV-2 3CLpro) with an IC50 of 24 nM. It has a potential anti-SARS-CoV-2 activity. Jul 04 2024
E4809 Piperaquine tetraphosphate tetrahydrate Piperaquine tetraphosphate tetrahydrate is an inhibitor of autophagy . It is a bisquinoline antimalarial agent effective against Plasmodium falciparum. Piperaquine tetraphosphate tetrahydrate is useful in antimalarial research. Jul 04 2024
E4808 Propionyl-L-carnitine hydrochloride Propionyl-L-carnitine hydrochloride(Levocarnitine propionate hydrochloride) supports mitochondrial metabolism, offers cardiovascular benefits, acts as a free radical scavenger, and is used in treating colonic inflammatory bowel disease. Jul 04 2024
E4810 Piperacillin Piperacillin is a broad-spectrum β-lactam antibiotic with potent bactericidal activity against Gram-negative bacteria and selects Gram-positive strains via penicillin-binding proteins. Jul 04 2024
E4634 MIRA-1 MIRA-1(NSC 19630), a maleimide compound, is a selective inhibitor of Werner syndrome WRN helicase activity with an IC50 of 20 µM while sparing ATPase and exonuclease activities. It reactivates mutant p53, inducing apoptosis in various human solid tumor cell lines with tetracycline-regulated mutant p53. Jul 03 2024
E4803 Vardenafil Vardenafil is an orally active and selective inhibitor of phosphodiesterase-5 (PDE5), with an IC50 value of 0.7 nM, respectively. Vardenafil acts as a competitive inhibitor of cyclic guanosine monophosphate (cGMP) hydrolysis, thereby increasing cGMP levels. Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes. Jul 02 2024
E1848 BGB-8035 BGB-8035 is an orally active, highly selective inhibitor of Bruton's tyrosine kinase (BTK) with IC50 values of 1.1 nM for BTK, respectively. BGB-8035 exhibits antitumor and anti-arthritis activity and displays potential for its use in research of B-cell malignancies and autoimmune diseases. Jul 02 2024
E1558 GSK-3008348 HCl GSK-3008348 HCl is a small molecule antagonist of integrin αvβ6 with an affinity (pIC50) value of 8.1 for αvβ6 in cell Adhesion assays. Jul 02 2024
E1582 Edralbrutinib Edralbrutinib (TG-1701) is an irreversible, highly specific, and potent inhibitor of Bruton's tyrosine kinase (BTK). TG-1701 shows similar efficacy but greater selectivity compared to the first-in-class BTK inhibitor ibrutinib, with a Kd value of 3 nmol/L, in both in vitro and in vivo models of B-cell non-Hodgkin lymphoma (B-NHL). Jul 02 2024
E4804 Sitagliptin phosphate Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of dipeptidyl peptidase IV (DPP-4) with an IC50 value of 19 nM in Caco-2 cell extracts. Jul 02 2024
E4801 Cu(II)-Elesclomol Cu(II)-Elesclomol, a Cu2+ complex of Elesclomol, is a weak inhibitor of DNA topoisomerase I. It is also highly capable of inducing cuproptosis and apoptosis. It induces DNA double-strand breaks in K562 cells and causes a G1 cell cycle block. Cu(II)-Elesclomol displays anticancer activity. Jun 27 2024
E4802 Ticarcillin disodium Ticarcillin disodium is a semisynthetic β-lactam antibiotic, which is active against Pseudomonas aeruginosa, Escherichia coli, Pseudomonas mirabilis, Pseudomonas rettgeri, and Klebsiella aerogenes. Jun 27 2024
E1858 RMC-7977 RMC-7977 is a potent, reversible, tri-complex oral inhibitor that selectively targets active (GTP-bound) forms of KRAS, HRAS, and NRAS, which exhibits broad-spectrum activity against both mutant and wild-type variants (a RASMULTI (ON) inhibitor). It also exhibits significant anti-tumor efficacy in pancreatic ductal adenocarcinoma (PDAC). Jun 27 2024
E1857 TH-Z816 TH-Z816 is an inhibitor of ,KRAS(G12D) with an IC50 of 14 μM in an SOS-catalyzed nucleotide exchange assay with GDP as the incoming nucleotide. Jun 27 2024
E1865 Envonalkib Envonalkib(TQ-B3139, CT-71, Formula 1) is a potent and orally active inhibitor of ALK, that exhibits IC50 values of 1.96 nM, 35.1 nM, and 61.3 nM for wild-type and mutated L1196M and G1269S-ALK. Envonalkib is also used in the research of non-small cell lung cancer. Jun 27 2024
E1995 AZD-5462 AZD-5462(Example 1) is a modulator of RXFP1, the cognate receptor for human relaxin, that belongs to the GPCR family 1c number. AZD-5462 exhibits anti-fibrotic and anti-inflammatory properties. Jun 27 2024
E1824 Vazegepant hydrochloride Vazegepant hydrochloride (BHV-3500, Zavegepant), is a highly potent, selective, and structurally unique small molecule antagonist of CGRP receptor. It can also be used for the acute treatment of migraine. Jun 27 2024
E1703 SF2312 SF2312 is a highly potent inhibitor of Enolase with IC50s of 37.9 nM and 42.5 nM for human recombinant ENO1 and ENO2, respectively, and also is a natural phosphonate antibiotic. SF2312 displays activity against bacteria under anaerobic conditions. Jun 27 2024
E1932 DW71177 DW71177 is a potent BD1-Selective inhibitor of BET. DW71177 selectively interacts with BD1 and exhibits strong antileukemic activity. DW71177 can also be used in the study of acute myeloid leukemia. Jun 27 2024
E1846 TL13-112 TL13-112 is a degrader of anaplastic lymphoma kinase (ALK) with an IC50 of 0.60 nM. It demonstrates anti-proliferative activity in non-small-cell lung cancer (NSCLC) and anaplastic large cell lymphoma (ALCL) cell lines. Jun 25 2024
E1580 TNG260 TNG260 is an inhibitor of CoREST-selective deacetylase (CoreDAC) that inhibits HDAC1 with 10-fold selectivity over HDAC3. It decreases intratumoral neutrophil infiltration and exhibits immune-mediated cell killing. Jun 24 2024
E1188 Brensocatib Brensocatib (AZD7986, INS1007) is an oral, selective, reversible inhibitor of dipeptidyl peptidase-1 (DPP-1). It reduces the activity of all major neutrophil serine proteases (NSPs) including, neutrophil elastase (NE), proteinase 3 (PR3), and cathepsin G (CatG) in patients with bronchiectasis. Jun 24 2024
P1238 SN 52 SN52, a cell-permeable peptide containing the p50 NLS, is a selective inhibitor of NF-κB pathway. It selectively and completely blocks the ionizing radiation (IR)-induced nuclear import of p52 and RelB. It also enhances the radiosensitivity of prostate cancer cells. Jun 24 2024
E1660 NX-5948 NX-5948(BTK-IN-24) is a novel oral small molecule that induces BTK degradation via cereblon E3 ubiquitin ligase recruitment. It mediates potent anti-inflammatory activity and can cross the blood-brain barrier in animal models. Jun 23 2024
E1986 TR-107 TR-107 is a chemical activator of the human mitochondrial protease ClpP with an EC50 of 140 nM. It exhibits excellent potency and specificity in the research of triple-negative breast cancer (TNBC) cell models. Jun 23 2024
E1947 DiR (Cy7 DiC18) DiR (Cy7 DiC18) is a near-infrared fluorescent long-chain carbocyanine dye used for labeling cell membranes, organelles, liposomes, viruses, and lipoproteins in vivo and in vitro. Jun 23 2024
E1437 PHI-101 PHI-101 is an orally active, potent third-generation inhibitor of FLT3 that overcomes resistance to multiple drug-resistant mutations. It has potential for research in relapsed or refractory acute myeloid leukemia (AML). Jun 23 2024
E1751 MSC-4381 MSC-4381 (MCT4-IN-1) is an orally active, selective inhibitor of monocarboxylate transporter 4 (MCT4) with an IC50 of 77 nM and a Ki of 11 nM. It has the potential to inhibit lactate efflux and promote intracellular lactate accumulation in MCT4-expressing cell lines. Jun 23 2024
E4607 Oseltamivir acid Oseltamivir acid(GS 4071,Ro 64-0802,Oseltamivir carboxylate), a metabolite of the antiviral compound oseltamivir, acts as a competitive inhibitor of influenza neuraminidases A and influenza neuraminidases B with IC50 of 0.1 to 4.9 nM respectively, thereby preventing virus budding and release. Jun 23 2024
E4594 Lithium iodide hydrate Lithium iodide hydrate is a reagent and the water-crystallized form of lithium iodide. It is commonly used as an electrolyte additive in dye-sensitized solar cells and Li-S batteries, enhancing their cycle life. Jun 23 2024
E4606 Dihexa Dihexa(PNB-0408), an oligopeptide drug, is an orally active and blood-brain barrier-permeable analog of angiotensin IV. It binds to hepatocyte growth factor (HGF) with high affinity and potentiates its activity at its receptor, c-Met. Dihexa can also be used as a therapeutic potential in the treatment of Alzheimer’s disease. Jun 19 2024
E1917 SLF1081851 hydrochloride SLF1081851 hydrochloride is a potential inhibitor of Spns2 that blocks S1P release with an IC50 of 1.93 μM. It can be developed as a probe for studying Spns2 biology and immune modulation. Jun 18 2024
E1528 RP-6685 RP-6685 is a potent, selective, and orally active inhibitor of DNA polymerase theta (Polθ). RP-6685 exhibits antitumor efficacy in animal models. Jun 18 2024
E1912 B102(PARP/HDAC-IN-1) B102(PARP/HDAC-IN-1) is a dual inhibitor of PARP and HDAC, with IC50 of 19.01 nM, 2.13 nM, 1.69 μM, > 10 μM for PARP1, PARP2, HDAC1, HDAC6, respectively, in an enzymatic assay. It exhibits anti-proliferative and anti-tumor effects. It also induces DNA damage and apoptosis in vitro. Jun 17 2024
E1980 Atogepant Atogepant(MK-8031, AGN-241689) is a potent, selective, orally available antagonist of the calcitonin gene-related peptide (CGRP) receptor, with ki of 0.026 nM for human CGRP receptor. It is used for the preventive treatment episodic migraine. Jun 17 2024
E1788 CQ211 CQ211 is a cell penetrant, potent and selective inhibitor of RIOK2(Right open reading frame kinase 2) with a Kd of 6.1 nM. It effectively inhibits cancer cell proliferation and shows promising in vivo efficacy in mouse xenograft models. Jun 13 2024
E1894 PROTAC tubulin-Degrader-1(compound W13) PROTAC tubulin-Degrader-1(compound W13) is an inhibitor of PROTAC tubulin exhibiting antitumor activity against human lung cancer. Jun 11 2024
P1239 ADH-1 ADH-1, an antagonist of N-cadherin, blocks N-cadherin-mediated cell adhesion. It exhibits significant antitumor activity against N-cadherin-expressing cells in vitro assays. Jun 10 2024
E1949 DuP-697 DuP-697 is a potent, irreversible, selective, and orally active inhibitor of COX-2 with an IC50 value of 10 nM for human COX-2, respectively. DuP-697 exerts antiproliferative, antiangiogenic, and apoptotic effects in colorectal cancer cells. Jun 10 2024
E1662 Elenestinib phosphate Elenestinib phosphate(BLU-263 phosphate) is a potent and orally active inhibitor of tyrosine kinase that exhibits potent inhibition of c-KIT (D816V) mutation. BLU-263 phosphate has the potential for its use in the research of systemic mastocytosis (SM). Jun 10 2024
E1908 HRO761 HRO761 is a potent, selective, allosteric inhibitor of Werner syndrome RecQ helicase (WRN). It binds at the interface of the D1 and D2 helicase domains, locking WRN in an inactive conformation, and demonstrates anti-proliferative effects specifically in microsatellite instability (MSI) cancer cells. Jun 10 2024
E4596 GSK-2879552 GSK-2879552 is a selective and potent inhibitor of Lysine-specific demethylase 1 (LSD1, KDM1A), with the potential to treat Small cell lung cancer (SCLC). It induces the expression of putative KDM1A target genes and demonstrates potent, predominantly cytostatic, antiproliferative activity in SCLC cell lines and tumor xenograft models. Jun 07 2024
E4595 SB-743921 SB-743921 (SB-921) is an inhibitor of Kinesin Spindle Protein (KSP), a mitotic protein essential for cell cycle control and motility. It functions by selectively targeting rapidly dividing cells and disrupting spindle formation during cell division, leading to G2/M phase arrest and ultimately causing cell death. It also inhibits proliferation and induces apoptosis in diffuse large B-cell lymphoma (DLBCL) cell lines. Jun 07 2024
S7512 GSK269962A GSK269962A is a potent and selective inhibitor of ROCK with IC50 values of 1.6 nM for ROCK1 and 4 nM for ROCK2. It shows potential as an alternative treatment for overactive bladder (OAB), and also exhibits anti-inflammatory and vasodilatory activities. Jun 06 2024
S9894 Vafidemstat Vafidemstat(ORY-2001) is a potent, selective, brain-penetrant dual inhibitor of lysine-specific histone demethylase (LSD1, KDM1A) and MAO-B, with IC50 values of 105 nM and 58 nM, respectively. It shows potential for treating memory deficits and behavioral alterations in neurodegenerative and psychiatric diseases. Jun 06 2024
E4593 Benzo-15-crown-5 ether Benzo-15-crown-5-ether (B15C5) is employed as a ligand in metal-catalyzed reactions to improve reactivity and selectivity by coordinating with metal cations. Additionally, it serves as a chelating agent for sodium and potassium ions. Jun 06 2024
E1872 Selnoflast Selnoflast(RO-7486967) is a selective and reversible small molecule inhibitor of NLRP3 inflammasome, with the potential to treat moderate to severe active ulcerative colitis. Jun 03 2024
E1625 Elsubrutinib Elsubrutinib(ABBV-105) is a covalent, irreversible, potent, and highly selective inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 0.18 μM for BTK catalytic domain. It specifically inhibits BTK dependent cellular functions, including both BCR and FcγR mediated signaling. It also exhibits significant efficacy in pre-clinical mechanistic models of antibody production, as well as in models of rheumatoid arthritis and lupus. Jun 03 2024
E1878 Bromoenol lactone Bromoenol lactone((6E)-Bromoenol lactone) is a selective, irreversible, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 value of ≈7 μM. It prevents antigen-stimulated exocytosis in mast cells without hindering Ca2+ influx. Jun 02 2024
E1761 AMG PERK 44 AMG PERK 44 is a highly selective and orally active inhibitor of PERK with an IC50 of 6 nM. AMG PERK 44 exhibits 1000-fold and 160-fold selectivity over GCN2 and B-Raf, respectively. Jun 02 2024
E1922 OX04528 OX04528 (compound 68) is a potent and G-protein-biased agonist of G protein-coupled receptor 84 (GPR84). OX04528 inhibits cAMP production with an EC50 value of 0.00598 nM (5.98 pM), respectively. Jun 02 2024
E1907 HADA hydrochloride HADA hydrochloride (HCC-Amino-D-alanine hydrochloride) is a blue fluorescent D-amino acid (FDAA) that labels peptidoglycans in live bacteria without affecting growth and also displays mitochondrial outer membrane permeability. May 28 2024
E1884 HC-258 HC-258 is a covalent acrylamide inhibitor of TEAD that reduces the CTGF, CYR61, AXL, and NF2 transcript levels and inhibits the migration of MDA-MB-231 breast cancer cells. May 27 2024
E1536 (R)-HTS-3 (GLXC-25878) (R)-HTS-3 (GLXC-25878) is a potent, selective, and cell-active inhibitor of lysophosphatidylcholine acyltransferase 3 (LPCAT3) with an IC50 of 0.09 µM, an enzyme critical for synthesizing C20:4-containing phospholipids. It reduces arachidonic acid-d8 incorporation into phospholipids and mitigates RSL3-induced ferroptosis in HT-1080 and 786-O cancer cells. May 27 2024
E1264 VIT-2763 VIT-2763 is an oral small-molecule inhibitor of ferroportin. It displaces TMR-hepcidin from ferroportin with an IC50 of 24 nM. It also ameliorates anemia, enhances erythropoiesis, and reduces organ iron loading in the Hbbth3/+ β-thalassemia intermedia disease model. May 23 2024
E1800 Oxythiamine chloride hydrochloride Oxythiamine chloride hydrochloride(Hydroxythiamine chloride hydrochloride) is a salt form of Oxythiamine. It is an inhibitor of transketolase, the enzyme that controls the nonoxidative branch of the pentose phosphate pathway. It also suppresses tumor cell proliferation and promotes apoptosis. May 23 2024
E1385 Bexotegrast Bexotegrast(PLN-74809) is potent dual selective inhibitor of αvβ6 and αvβ1 integrins with Kd of 5.7 nM and 3.4 nM, respectively. It has antifibrogenic effects, blocks multiple TGF-β activation pathways in the fibrotic lung, and is useful for researching fibrosis, including idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP). May 21 2024
E1607 RK-701 RK-701 is a highly selective, potent, and low-toxicity inhibitor of histone methyltransferases G9a and GLP1 with IC50 values of 23-27 nM and 53 nM. RK-701 treatment induces fetal globin expression in human erythroid cells and in mice and plays an essential role in γ-globin induction. RK-701 is used in the research of sickle cell disease. May 19 2024
E1632 VU0463271 VU0463271 is a selective and potent antagonist of neuronal-specific potassium-chloride cotransporter 2 KCC2, with an IC50 of 61 nM. VU0463271 demonstrates over 100-fold selectivity compared to the closely related Na-K-2Cl cotransporter 1 (NKCC1). May 16 2024
E1340 Glesatinib Glesatinib(MGCD265) is an orally bioavailable potent dual inhibitor of c-MET and SMO. Glesatinib counteracts P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC). May 16 2024
E1962 RMC-9805 RMC-9805(KRAS G12D ON inhibitor) is an orally active inhibitor of KRAS G12D. RMC-9805 inhibits RAS signaling, leading to apoptosis in cancer cells with the KRAS G12D mutation. May 15 2024
E1613 UNC8153 UNC8153 is a selective degrader of nuclear receptor-binding SET domain-containing 2 (NSD2) with a binding Kd of 24 nM, effectively reducing NSD2 protein levels and the dimethylate lysine 36 of histone 3 (H3K36me2) chromatin mark. Its simple warhead promotes proteasome-dependent degradation of NSD2 via a novel mechanism. May 14 2024
E1818 PF-07265807 PF-07265807(TAM&Met-IN-1) is a dual inhibitor of AXL and MER, which exhibits anti-tumor effects. It also enhances the function of dendritic cells to cross-prime CD8+ T cells. May 14 2024
E1830 Baxdrostat Baxdrostat(CIN-107) is a selective and potent inhibitor of aldosterone synthase(CYP11B2), a rate-limiting enzyme in the pathway of aldosterone synthesis, with the potential to treat resistant hypertension. It also inhibits the function of multidrug and toxin extrusion 1 (MATE1) and MATE2-K with IC50 values of 1.34 µM and 2.67 µM, respectively. May 14 2024
E1745 Ulonivirine Ulonivirine(MK-8507) is a selective and potent inhibitor of HIV-1 nonnucleoside reverse transcriptase (NNRTI) that binds to the classic NNRTI hydrophobic binding pocket near the polymerase active site. It demonstrates a potential to treat HIV-1 infections and induce the expression of CYP3A4, an enzyme often involved in drug metabolism. May 14 2024
E1724 CRT-0105446 CRT 0105446 (compound 22d) is a potent inhibitor of LIMK1 with an IC50 of 8 nM. It can inhibit the growth of MCF-7 breast cancer cells and the invasion of MDA-MB-231 cells by reducing the expression of phosphorylated cofilin. May 09 2024
E1875 BI-3231 BI-3231 is the potent and selective chemical probe, which inhibits hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13) with an IC50 of 1 nM and Ki of 0.7 nM in the enzymatic assay. It has the potential to treat NASH and other liver diseases.  May 09 2024
E1937 PT-179 PT-179, an orthogonal Thalidomide derivative targets cereblon without causing off-target degradation effects. PT-179 specifically binds CRBN, forms a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediates the degradation of the tagged protein. May 09 2024
E1795 Triparanol(MER-29) Triparanol (MER-29) is an inhibitor of 24-dehydrocholesterol reductase (DHCR24), an enzyme involved in cholesterol biosynthesis. It exhibits antitumor properties, such as decreasing proliferation and inducing apoptosis in various cancer cell lines, while also reducing Hedgehog pathway signaling in these cells. May 09 2024
E0448 RO8191 RO8191 (CDM-3008, RO4948191), an imidazonaphthyridine compound, is an orally active and potent agonist of interferon (IFN) receptor. RO8191 binds directly to the IFNα/β receptor 2 (IFNAR2), activating IFN-stimulated genes (ISGs) expression and the phosphorylation of JAK/STAT signaling. May 09 2024
S7994 GSK864 GSK864 is a cell-penetrant, potent, and selective inhibitor of isocitrate dehydrogenase 1 (IDH1) mutants, specifically targeting the R132C, R132H, and R132G variants with IC50 values of 8.8 nM, 15.2 nM, and 16.6 nM, respectively. May 06 2024
E1929 LTGO-33 LTGO-33 is a potent and selective inhibitor of voltage-gated sodium channel NaV1.8. LTGO-33, with its potency in the nanomolar range, selectively inhibits NaV1.8 over 600 times more than human NaV1.1-NaV1.7 and NaV1.9. Its inhibition is not dependent on the state of the channels and displays consistent potency against both closed and inactivated conformations. LTGO-33 holds promise for research in pain disorders. Apr 28 2024
E1925 Butylhydroxyanisole Butylhydroxyanisole (Butylated hydroxyanisole, BHA, E320) is an inhibitor of ferroptosis, a food preservative and antioxidant that prevents the formation of harmful compounds, extending shelf life. However, it's associated with liver toxicity, reproductive organ development issues, learning delays, and sleep problems. Apr 25 2024
E1740 Mepazine hydrochloride Mepazine hydrochloride (Pecazine hydrochloride) is a potent and selective inhibitor of MALT1 protease, with IC50 values of 0.83 μM for GSTMALT1 full length and 0.42 μM for GSTMALT1 aa 325-760. It effectively suppresses the activation of the NF-kB pathway specifically in activated B cell subtype of diffuse large B cell lymphoma (ABC-DLBCL) cells and makes it a promising candidate for the treatment of ABC-DLBCL. Apr 25 2024
E1806 AGI-24512 AGI-24512 is an inhibitor of MAT2A with an IC50 of 8 nM. It increases R-Loop formation and DNA damage in MTAP-deleted and WT cell models. It also exhibits anti-proliferative activity in vitro. Apr 25 2024
E1798 HOIPIN-8 HOIPIN-8, is a potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) and NF-κB signaling with an IC50 value of 11 nM. It serves as a powerful tool for investigating the physiological and cellular functions of LUBAC. Apr 23 2024
E1699 SR10221 SR10221 is a inverse-agonist of PPARγ with IC50 of 1.6 nM in RT112/84 FABP4-NLucP reporter assay. It exhibits an antiproliferative activity in vitro. Apr 22 2024
S8546 Alrizomadlin Alrizomadlin(APG-115, AA-115) is a highly potent and efficacious inhibitor of MDM2 and binds to MDM2 with IC50 of 3.8 nM. It exhibits potent antiproliferative and apoptogenic activities and also significantly reduces tumor burden and prolonged survival in AML xenograft models. Apr 21 2024
A2162 Anti-mouse/human VLA-4 (CD49d)-InVivo Anti-mouse/human VLA-4 (CD49d)-InVivo reacts with human and mouse VLA-4 α chain also known as CD49d and integrin alpha 4. VLA-4 is a 150 kDa glycoprotein belonging to the integrin family that is expressed by many cell types including T and B lymphocytes, monocytes, eosinophils, basophils, mast cells, thymocytes, NK cells, and dendritic cells. Apr 19 2024
E4585 N-Arachidonyldopamine N-Arachidonyldopamine is a potent agonist of cannabinoid receptor 1 (CB1), with a Ki of 250 nM in rat brain membranes, showing 40-fold selectivity for CB1 over CB2 receptors. It also triggers intracellular calcium mobilization in N18TG2 neuroblastoma cells. Apr 17 2024
E1728 STC-15 STC-15 is an oral, small-molecule inhibitor of RNA methyltransferase METTL3. It inhibits tumor growth through the activation of anti-cancer immune responses associated with increased interferon signaling and synergizes with T-cell checkpoint blockade. Apr 16 2024
E1904 SKF-34288 hydrochloride SKF-34288 hydrochloride(3-Mercaptopicolinic acid hydrochloride, 3-MPA hydrochloride) is an orally active, specific inhibitor of phosphoenolpyruvate carboxykinase (PEPCK) with Ki values of 2-9 μM. SKF-34288 hydrochloride is a potent hypoglycemic agent by inhibiting glucose synthesis. SKF-34288 hydrochloride also inhibits cell proliferation, induces myogenic differentiation in vitro. Apr 14 2024
E1036 BMS-986278 BMS-986278 is a potent and orally active antagonist of lysophosphatidic acid receptor 1 (LPA1). BMS-986278 exhibits Kbs of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively, and is widely used in the research of pulmonary fibrotic diseases. Apr 14 2024
S9716 H3B-8800 H3B-8800 is a potent and orally active modulator of SF3B splicing. H3B-8800 interacts directly with the SF3b complex, demonstrating anti-cancer properties. H3B-8800 holds promise for studying acute myeloid leukemia (AML) with SF3B1 mutations. Apr 10 2024
E1597 RMC-6236 RMC-6236 (RAS-IN-2) is a RAS(ON) multi-selective noncovalent inhibitor of the active, GTP-bound state of both mutant and wild-type variants of canonical RAS isoforms with broad therapeutic potential. RMC-6236 exhibits strong anticancer efficacy in RAS-addicted cell lines, especially those with mutations at codon 12 of KRAS. Apr 10 2024
E1880 OTUB2-IN-1 OTUB2-IN-1 is a specific inhibitor of OTUB2, decreases PD-L1 protein expression in tumor cells, leading to suppressed tumor growth through enhanced infiltration of cytotoxic T lymphocytes (CTLs) within the tumor microenvironment. Apr 10 2024
E1903 SLU-PP-332 SLU-PP-332 is an agonist of pan-Estrogen Receptor/ERR with EC50 values of 98nM, 230nM, and 430 nM for ERRα, ERRβ, and ERRγ, respectively with the highest potency for ERRα. SLUPP-332 amplifies mitochondrial function and cellular respiration in skeletal muscle cell lines and also offers opportunities for researching metabolic ailments and enhancing muscle functionality. Apr 10 2024
E1876 GTS-21 dihydrochloride GTS-21 dihydrochloride(DMXB-A, DMBX-anabaseine) is a selective agonist of alpha7 nicotinic acetylcholine receptor (α7-nAChR) and exhibits anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also an antagonist of α4β2 with a Ki value of 20 nM for humanα4β2 and 5-HT3A receptor with an IC50 value of 3.1 μM. Apr 10 2024
E1924 TI17 TI17 is an inhibitor of thyroid hormone receptor-interacting protein Trip13. TI17 efficiently suppresses the proliferation of multiple myeloma (MM) cells and triggers cell cycle arrest and apoptosis. Trip13, an AAA-ATPase involved in double-strand break (DSB) repair, is targeted by TI17, leading to impaired function and heightened DNA damage. Apr 10 2024
E1710 LY2780301 LY2780301 is a highly selective adenosine triphosphate (ATP)-competitive dual inhibitor of p70S6K and Akt. LY2780301 binds to Akt, inhibiting its activity, which consequently blocks the PI3K/Akt signaling pathway which leads to reduced cell proliferation and the initiation of apoptosis in tumor cells. Apr 08 2024
E1849 TL12-186 TL12-186 is a cereblon-dependent multi-kinase PROTAC degrader. TL12-186 also inhibits CDK2/cyclin A and CDK9/cyclin T1 with IC50 values of 73 nM and 55 nM, respectively. Apr 08 2024
S8267 RapaLink-1 RapaLink-1, a third-generation bivalent inhibitor of mTOR, combines Rapamycin with MLN0128 using an inert chemical linker. It demonstrates efficacy against resistant mutants of malignant brain tumors and inhibits cancer cell progression by binding to mesenchymal markers. Apr 06 2024
E1653 CCT241533 hydrochloride CCT241533 hydrochloride is an ATP competitive, potent, and selective inhibitor of CHK2 with an IC50 of 3 nM and a Ki of 1.16 nM and shows minimal cross-reactivity against a panel of kinases. CCT241533 inhibits CHK2 activity in human tumor cell lines when subjected to DNA damage. Apr 06 2024
E1905 Nalidixic acid sodium salt Nalidixic acid sodium salt is an inhibitor of bacterial DNA gyrase and topoisomerase IV, essential enzymes for DNA supercoiling during replication, making it an effective quinolone antibiotic against both gram-positive and gram-negative bacteria. Apr 06 2024
A2160 Anti-rat Kappa Immunoglobulin Light Chain-InVivo Anti-rat Kappa Immunoglobulin Light Chain-InVivo reacts with the kappa chain of the rat immunoglobulin light chain. The κ chain is one of two types of polypeptide subunits which make up the immunoglobulin light chain. Apr 03 2024
A2161 Anti-mouse ICOSL (CD275)-InVivo Anti-mouse ICOSL (CD275)-InVivo reacts with mouse ICOSL (inducible T cell co-stimulator ligand) also known as CD275, B7RP-1, and B7-H2. ICOSL is a 40 kDa immune checkpoint protein belonging to the Ig receptor superfamily. Apr 03 2024
E1781 Biricodar Biricodar(VX-710) is a modulator of P-glycoprotein and MRP-1 with minimal in vivo toxicity. It enhances the effectiveness of various antibiotics against numerous gram-positive pathogens and exhibits potent chemosensitizing properties in cells resistant to multiple drugs. Mar 31 2024
E1554 Tefinostat(CHR-2845) Tefinostat(CHR-2845) is a monocyte/macrophage-targeted inhibitor of pan-histone deacetylase (HDAC). Tefinostat undergoes cleavage mediated by the intracellular esterase human carboxylesterase-1 (hCE-1) to yield the active acid CHR-2847. In vitro studies reveal a specific heightened sensitivity of monocytoid leukemias to tefinostat. Mar 27 2024
E1783 Conteltinib(CT-707) Conteltinib(CT-707) is a potent multikinase inhibitor of ALK, FAK,Pyk2, showing promising anti-tumor activities. Conteltinib exhibits significant inhibitory effects on FAK with an IC50 value of 1.6 nM in vitro kinase assay. Mar 26 2024
E1114 Ifebemtinib Ifebemtinib(IN10018, BI853520) is a highly selective, potent inhibitor of focal adhesion kinase (FAK), with an IC50 of 1 nM for inhibiting FAK autophosphorylation. It also inhibits FER Kinase and FES Kinase with IC50s of 900 nM and 1040 nM, respectively, inhibiting spheroid formation and orthotopic tumor growth in malignant pleural mesothelioma. IN10018 exhibits anti-tumor activity in vitro and in vivo. Mar 25 2024
S9861 PY-60 PY-60 is a small-molecule activator of the transcriptional coactivator Yes-associated protein (YAP) with EC50 of 1.6 µM, which acts by inhibiting a central scaffolding protein in the Hippo pathway, Annexin A2. It promotes the regenerative repair of cutaneous wounds in pig and human models. Mar 24 2024
E1356 BI-0474 BI-0474 is a potent inhibitor of KRASG12C with an IC50 value of 7.0 nM. It inhibits GDP-KRAS::SOS1 protein-protein interactions. It exhibits anti-proliferative and anti-tumour activity and can be used in cancer research. Mar 24 2024
E1165 JAB-3068 JAB-3068 (SHP2-IN-6) is a potent allosteric inhibitor of SHP2. JAB-3068 enhances the anti-tumor activity of CD8+ T cells and can be used in combination to address non-responsive tumors alongside PD-1/PD-L1 antibodies. Mar 20 2024
E1768 MEDICA16 MEDICA16 is an inhibitor of ATP-citrate lyase and also acts as an agonist of G protein-coupled receptor 40 (GPR40). It functions to blunt the development of insulin resistance in the JCR:LA-cp rat as well as it is a potent triacylglycerol-lowering agent. Mar 14 2024
S9734 Bomedemstat Bomedemstat(IMG-7289) is an orally active and irreversible inhibitor of LSD1(lysine-specific demethylase 1). Bomedemstat exhibits the ability to enhance methylation levels of H3K4 and H3K9, subsequently leading to modifications in gene expression. Bomedemstat demonstrates anti-cancer properties by restraining cancer cell proliferation and prompting apoptosis. Mar 12 2024
E1341 Cerivastatin sodium Cerivastatin sodium, a sodium salt of cerivastatin, is an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase with Ki of 1.3 nM. It is also a synthetic, enantiomerically pure, pyridine derivative that effectively reduces serum cholesterol levels at microgram doses. Mar 12 2024
E1694 Sardomozide dihydrochloride Sardomozide dihydrochloride (CGP 48664A) is a potent inhibitor of S-adenosylmethionine decarboxylase (SAMDC) with an IC50 of 5 nM. It is also a potent inhibitor of polyamine oxidase and exhibits with broad spectrum antiproliferative and antitumor activity. Mar 07 2024
S7972 Litronesib Litronesib (LY2523355) is a selective allosteric inhibitor of the human mitosis-specific kinesin Eg5. LY2523355 also exhibits highly schedule-dependent, broad-spectrum anticancer activity against tumor models and causes mitotic arrest and apoptosis in cancer cells. Mar 07 2024
E1754 BRD7389 BRD7389 is an inhibitor of RSK family kinases with IC50 of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 also increases β-cell–specific gene expression in primary human islet cells.  Mar 06 2024
A2159 Anti-mouse CSF1R (CD115)-InVivo Anti-mouse CSF1R (CD115)-InVivo reacts with mouse colony stimulating factor 1 receptor (CSF1R), also known as macrophage colony-stimulating factor receptor (M-CSFR), and CD115. CSF1R is a single-pass type I membrane protein and member of the platelet-derived growth factor receptor family. Mar 03 2024
E1722 Acetalax(Oxyphenisatin acetate) Oxyphenisatin acetate is the pro-drug of oxyphenisatin. It has antiproliferative activity and also used to be a laxative. Mar 03 2024
E1352 Butyzamide Butyzamide is a non-peptidyl thrombopoietin receptor, activator of Mpl . It also augments the phosphorylation level of JAK2, STAT3, STAT5 and MAPK. It has potential for treatment of thrombocytopenia. Mar 03 2024
A2158 Anti-mouse Ly6G-InVivo Anti-mouse Ly6G-InVivo reacts with mouse Ly6G. Ly6G is a 21-25 kDa member of the Ly-6 superfamily of GPI-anchored cell surface proteins with roles in cell signaling and cell adhesion. Mar 01 2024
E2504 Toyocamycin Toyocamycin(Vengicide), an adenosine analog, acts as an inhibitor of XBP1. Toyocamycin is also a specific inhibitor of CDK9 with an IC50 value of 79 nM. Feb 26 2024
E1787 SN-001 SN-001 is a potent inhibitor of STING that specifically inhibits STING activation and STING-dependent signaling. SN-011 significantly decreases inflammatory cytokine production and osteoclast formation in vivo. Feb 26 2024
E1796 Dimethindene maleate Dimethindene maleate is a selective antagonist of histamine H1 and exhibits antihistamine effects. It suppresses the cromakalim-induced/glibenclamide-sensitive K+ currents in a concentration-dependent and reversible manner. Feb 26 2024
E1698 EN460 EN460 is a small-molecule inhibitor of endoplasmic reticulum oxidation 1(ERO1), which is specific for the reduced active form of ERO1α and prevents re-oxidation. It also protects cells from erastin-induced ferroptosis. Feb 26 2024
E1670 MKI-1 MKI-1(MASTL Kinase Inhibitor-1) is an small-molecule inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 9.9 μM in kinase assay. It also exerts antitumor and radiosensitizer activities through PP2A-mediated c-Myc inhibition in breast cancer models. Feb 26 2024
E1614 OUL232 OUL232 (Compound 27) is an potent inhibitor of mono-ADP-ribosylation (mono-ARTs) PARP10 with IC50 of 7.8 nM. It also inhibits PARP7, PARP11, PARP12, PARP14, and PARP15 at nM potencies. Feb 26 2024
A2150 Armenian hamster IgG isotype control-InVivo Armenian hamster IgG isotype control-InVivo is ideal for use as an isotype control for Armenian hamster IgG antibodies in most in vivo and in vitro applications. Feb 21 2024
A2151 Anti-mouse IL-10R (CD210)-InVivo Anti-mouse IL-10R (CD210)-InVivo reacts with mouse IL-10R (IL-10 receptor) also known as CD210. The IL-10R is a class II cytokine receptor and is expressed by a variety of cell types including thymocytes, T lymphocytes, B lymphocytes, NK cells, monocytes, and macrophages. Feb 21 2024
A2152 Anti-mouse IFNγ (XMG1.2)-InVivo Anti-mouse IFNγ (XMG1.2)-InVivo reacts with mouse IFNγ (interferon gamma) a 20 kDa soluble pleiotropic cytokine and the sole member of the type II class of interferons. Feb 21 2024
A2153 Anti-mouse IL-2 (S4B6-1)-InVivo Anti-mouse IL-2 (S4B6-1)-InVivo reacts with mouse IL-2, a 17 kDa cytokine that is mainly produced by T cells in response to antigenic or mitogenic stimulation. Feb 21 2024
A2154 Anti-mouse CD86 (B7-2)-InVivo Anti-mouse CD86 (B7-2)-InVivo reacts with mouse CD86 also known as B7-2. CD86 is an 80 kDa Ig superfamily member. Feb 21 2024
A2156 Anti-human PD-L1 (B7-H1)-InVivo Anti-human PD-L1 (B7-H1)-InVivo reacts with human PD-L1 (programmed death ligand 1) also known as B7-H1 or CD274. PD-L1 is a 40 kDa type I transmembrane protein that belongs to the B7 family of the Ig superfamily. Feb 21 2024
A2157 Anti-mouse IL-6R-InVivo Anti-mouse IL-6R-InVivo reacts with the mouse IL-6 receptor α chain also known as CD126. CD126 is an 80 kDa type I cytokine receptor and a member of the immunoglobulin superfamily. Feb 21 2024
E1163 MS177 MS177 is an EZH2-targeting PRTOAC degrader and a potent inhibitor of enzymatic EZH2, that effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukemia cell growth inhibition, apoptosis, and cell cycle progression arrest. Feb 21 2024
E4578 Trilaciclib dihydrochloride Trilaciclib dihydrochloride(G1T28 dihydrochloride) is a potent inhibitor of CDK4/cyclin D1 and CDK6/cyclin D3 with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively. Trilaciclib hydrochloride regulates cell proliferation and protects against chemotherapy toxicity in murine and canine bone marrow cells. Feb 06 2024
A2141 Anti-mouse Ter-119-InVivo Anti-mouse Ter-119-InVivo reacts with mouse Ter-119, a 52 kDa glycophorin A-associated protein that is expressed by erythroid cells from the early proerythroblast stage to mature erythrocytes. Anti-mouse Ter-119-InVivo is commonly used for identifying erythrocytes and cells in the erythroid lineage. Feb 05 2024
A2142 Anti-mouse/rat IL-1β-InVivo Anti-mouse/rat IL-1β-InVivo reacts with precursor and mature secreted forms of mouse and rat IL-1β a 17 kDa pro-inflammatory cytokine produced primarily by monocytes. Feb 05 2024
A2143 Anti-mouse 4-1BB (CD137)-InVivo Anti-mouse 4-1BB (CD137)-InVivo reacts with mouse 4-1BB, a TNF receptor superfamily member also known as CD137. Feb 05 2024
A2144 Anti-mouse TIGIT-InVivo Anti-mouse TIGIT-InVivo reacts with mouse TIGIT (T cell immunoreceptor with Ig and ITIM domains). TIGIT is a 26 kDa, type I transmembrane protein and a member of the poliovirus receptor (PVR) family. Feb 05 2024
A2145 Mouse IgG2b isotype control-InVivo Mouse IgG2b isotype control-InVivo is ideal for use as a non-reactive isotype-matched control for mouse IgG2b antibodies in most in vivo and in vitro applications. Feb 05 2024
A2146 Anti-LCMV nucleoprotein-InVivo Anti-LCMV nucleoprotein-InVivo reacts with lymphocytic choriomeningitis virus (LCMV) nucleoprotein (NP), a 63 kDa structural protein. Feb 05 2024
A2147 Anti-mouse CXCR3 (CD183)-InVivo Anti-mouse CXCR3 (CD183)-InVivo reacts with mouse CXCR3 also known as CD183, a 38 kDa chemokine receptor for CXCL9 (MIG), CXCL10 (IP-10), and CXCL11 (ITAC). Feb 05 2024
A2148 Anti-mouse GM-CSF-InVivo Anti-mouse GM-CSF-InVivo reacts with mouse granulocyte-macrophage colony-stimulating factor (GM-CSF), also known as colony stimulating factor 2 (CSF2). Feb 05 2024
A2149 Anti-mouse CD19-InVivo Anti-mouse CD19-InVivo reacts with mouse CD19, a B cell-specific 95 kDa transmembrane glycoprotein of the immunoglobulin superfamily. Feb 05 2024
E1287 SB 204990 SB-204990, a γ-lactone prodrug of SB-201076, is a potent and specific inhibitor of ATP citrate lyase (ACLY). SB 204990 potently limits SARS-CoV-2 replication in vivo. Feb 04 2024
E1721 TJ-M2010-5 TJ-M2010-5 is a small molecule inhibitor of MyD88 that selectively binds to the Toll/Interleukin-1 receptor (TIR) domain of MyD88, disrupting its homodimerization and subsequently inhibiting the Toll-like receptor (TLR)/MyD88 signaling pathway. TJ-M2010-5 exhibits an anti-hepatic fibrosis effect with the potential to treat liver fibrosis. Feb 04 2024
E1713 FL118 FL118(10,11-(Methylenedioxy)-20(S)-camptothecin), a Camptothecin analog, is a potent and orally active inhibitor of Survivin. FL118 also selectively and independently inhibits three additional cancer-associated survival genes Mcl-1, XIAP, and cIAP2 in a p53 status-independent manner. FL118 displays potent antitumor activity and can be used in cancer research. Feb 04 2024
E1655 KT 474 KT-474 (SAR444656) is a selective small-molecule degrader of IRAK4 in development for the treatment of TLR/IL-1R–driven autoimmune diseases. KT-474 potently downregulates R848 (TLR7/8) and lipopolysaccharide (LPS)-induced IL-6 and IL-8 production in peripheral blood mononuclear cells (PBMCs). Feb 01 2024
E1627 BMS493 BMS493 is an inverse agonist of pan retinoic acid receptor (RAR). It increases nuclear corepressor interaction with RARs and can be used as an inhibitor for the dietary and pharmacologic manipulation of retinoic acid (RA) activity in vivo and in vitro. Feb 01 2024
E1685 D609 D609 is a selective, competitive inhibitor of phosphatidylcholine-specific phospholipase C (PC-PLC) with a Ki of 6.4 μM. It is an antioxidative protector and has antiviral and anti-inflammatory activity and also inhibits angiogenesis by preventing the synthesis of basement membrane (BM). Feb 01 2024
E1748 HG6-64-1 HG6-64-1 (HMSL 10017-101-1) is a highly potent and selective inhibitor of B-Raf with an IC50 of 0.09 μM on B-raf V600E transformed Ba/F3 cells. Feb 01 2024
E1874 Erastin2 Erastin2 is an inducer of ferroptosis. It also selectively inhibits xc(-) cystine/glutamate transporter. It induces ferroptosis in HT-1080, T98G, and A549 cells with the potential to treat neurodegenerative diseases. Feb 01 2024
E1520 NSC 663284 NSC 663284(DA-3003-10) is a potent, cell-permeable, and irreversible dual specificity phosphatase inhibitor of Cdc25, and exhibits an IC50 of 0.21 μM for Cdc25B2 and is 20 and 450-fold highly selective against Cdc25B2. NSC 663284 also inhibits NSD2 with an IC50 of 170 nM via a direct interaction with the catalytic SET domain. Jan 30 2024
E1750 XST-14 XST-14 is a potent, competitive, and highly selective inhibitor of ULK1 and exhibits an IC50 of 26.6 nM in an in vitro ULK1 kinase activity assay, respectively. XST-14 reduces the phosphorylation of the ULK1 downstream substrate and induces autophagy inhibition. It exhibits antitumor effects. Jan 30 2024
E1832 ZK53 ZK53 is a selective activator of mitochondrial caseinolytic protease P (HsClpP). It exhibits an EC50 of 1.37 μM for α-casein hydrolysis by HsClpP. ZK53 treatment allosterically activates HsClpP to uncontrollably degrade the essential mitochondrial proteins and is inactive toward bacterial ClpP proteins. Jan 30 2024
S9852 Orforglipron Orforglipron(LY3502970) is a non-peptidal agonist of glucagon-like peptide 1(GLP-1) receptor. It can be used efficiently in glycemic control and weight reduction in type 2 diabetes mellitus (T2DM), obesity or both. Jan 24 2024
E1749 limertinib limertinib (ASK120067) is an irreversible third-generation inhibitor of EGFRT790M with IC50 of 0.3 nM, with selectivity over EGFRWT having IC50 of 6.0 nM. It exhibits potent anti-proliferation activity in non-small cell lung cancer (NSCLC) tumor cells. Jan 23 2024
E4449 AG 825 AG-825 (Tyrphostin AG-825) is a potent and selective inhibitor of ErbB2 with IC50 values of 0.15 µM. It also inhibits PDGFR autophosphorylation with IC50 value of 40 µM. It exhibits anti-cancer activity and significantly induces apoptosis in cancer cells. Jan 22 2024
E1810 dCeMM1 dCeMM1 is a degrader of RBM39. dCeMM1 functions by altering the activity of the CRL4DCAF15 ligase, and also decreases RBM39 expression levels in wild-type KBM7 cells. Jan 22 2024
E1752 JNJ-42226314 JNJ-42226314 is a potent, selective, and reversible noncovalent inhibitor of monoacylglycerol lipase (MAGL). It enhances the expression of endocannabinoid 2-arachidonoylglycerol (2-AG) and exhibits antinociceptive efficacy in models of neuropathic and inflammatory pain. Jan 22 2024
E4453 Cathepsin G Inhibitor I Cathepsin G Inhibitor I exhibits reversible, competitive cathepsin G inhibition with IC50 and Ki values of 53 nM and 63 nM respectively. It can be used in antigen-processing studies and for modulation of T cell response in situ and in vivo. Jan 22 2024
E1711 FHT-1015 FHT-1015 is a potent, small-molecule, allosteric inhibitor of SMARCA4/SMARCA2 ATPase with IC50 values ≤10 nM. FHT-1205 decreases PD1+TIM3+ cells and cytokine expression in vivo. Jan 21 2024
E1634 CH6953755 CH6953755 is a potent, orally active, and selective inhibitor of YES1 kinase with an IC50 of 1.8 nM. CH6953755 demonstrates antitumor activity against YES1 gene-amplified cancers. Jan 21 2024
S6392 SHIN1(RZ-2994) SHIN1 (RZ-2994) is an inhibitor of SHMT1/2 (human serine hydroxymethyltransferase 1 and 2) with IC50 values of 5 and 13 nM, respectively, in in vitro assay. SHIN1 hinders cell growth by gradually reducing purine levels. Jan 21 2024
E4580 Sovleplenib Sovleplenib(HMPL-523) is a highly potent and selective SYK inhibitor with IC50 of 0.025 μM, that exhibits anti-tumor activities in vitro and in vivo. Sovleplenib exhibits synergistic activities in combination with BTK, PI3Kδ, and Bcl2 family inhibitors in killing human-diffused large B cell lymphoma (DLBCL). Jan 17 2024
E1769 Merbarone Merbarone(NSC 336628) is a catalytic inhibitor of topoisomerase II with IC50 of 120 μM, with anti-proliferative activity against human cancer cells. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage. Jan 17 2024
E1604 Vevorisertib trihydrochloride Vevorisertib trihydrochloride(ARQ 751 trihydrochloride) is a selective, allosteric inhibitor of pan-AKT and AKT1-E17K mutant with Kd values of 1.2 nM and 8.6 nM, respectively. It also has IC50 values of 0.55, 0.81, and 1.3 nM for AKT1, AKT2, and AKT3, respectively and can be used for the research of cancer. Jan 16 2024
A3176 Human IgG2sa isotype control Human IgG2sa isotype control is suitable for use as a non-targeting isotype control in various in vitro and in vivo studies, is the isotype control of human IgG2sa antibody. Jan 15 2024
E1667 LY2880070 LY2880070 is an orally active inhibitor of CHK1. LY2880070 can be used as an anticancer agent and shows promise in preclinical models of pancreatic ductal adenocarcinoma (PDAC) when used in combination with DNA-damaging agents. Jan 10 2024
E1812 N6F11 N6F11 is an inducer of ferroptosis. N6F11 is bound to the RING domain of the E3 ubiquitin ligase tripartite motif containing 25 (TRIM25) in cancer cells to trigger TRIM25-mediated K48-linked ubiquitination of glutathione peroxidase 4 (GPX4), resulting in proteasomal degradation. Jan 10 2024
E1739 MST-312 MST-312(Telomerase Inhibitor IX) is an inhibitor of telomerase. MST-312 is a chemically modified derivative of green tea epigallocatechin gallate (EGCG). MST-312 exhibits high chemical stability, lowers the effective dose in the induction of telomere shortening, and lowers drug resistance. MST-312 can be used for the research of cancer. MST-312 can also be used as a promising strategy in the treatment of multiple myeloma (MM). Jan 10 2024
E1658 PRT543 PRT543 is a potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) with broad antitumor activity in vitro and in vivo. It also inhibits the methyltransferase activity of the PRMT5/MEP50 complex with an IC50 of 10.8 nM. Jan 09 2024
E1744 UNC5293 UNC5293 is a potent, highly selective, orally available inhibitor of MER receptor tyrosine kinase (MERTK) with IC50 of 0.9 nM and Ki 0.19 nM. Jan 09 2024
E1742 Reversan Reversan (CBLC4H10) is a selective and nontoxic inhibitor of multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (P-gp), with the potential to treat neuroblastoma and other MRP1-overexpressing drug-refractory tumors. Jan 09 2024
E1723 NSC16168 NSC16168 is a specific inhibitor of ERCC1-XPF, and exhibits an IC50 value of 0.42 μM in a high throughput screen (HTS) assay, respectively. NSC16168 inhibits DNA repair and potentiates cisplatin efficacy in cancer. Jan 09 2024
E1746 Protokylol hydrochloride Protokylol hydrochloride(Caytine hydrochloride, JB-251 hydrochloride) is a salt form of protokylol and is an agonist of β-adrenergic receptor. Protokylol hydrochloride is also used as a bronchodilator. Jan 07 2024
E1727 Pimicotinib Pimicotinib (ABSK021) is an orally bioavailable inhibitor of colony stimulating factor 1 receptor (CSF1R). It enhances antitumor T-cell immune responses and inhibits the proliferation of tumor cells having potential immunomodulatory and antineoplastic activities. Jan 07 2024
E1564 BI-2493 BI-2493, a structural analogue of BI-2865, is a highly selective inhibitor of pan-KRAS. BI-2493 attenuates tumor growth and can be used for cancer research. Jan 07 2024
E1620 Fluorofurimazine Fluorofurimazine is a novel furimazine analogue, with increased aqueous solubility enabling higher signal emission than furimazine for bioluminescence imaging. Fluorofurimazine enables higher substrate loading and improved optical imaging sensitivity in in-vivo. Jan 04 2024
E1435 Tinengotinib Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC). Jan 01 2024
E1649 Exarafenib Exarafenib(KIN-002787, KIN-2787, RAF/KIN_2787) is an orally-available, selective inhibitor of pan-RAF. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines. KIN-2787 exhibits low nanomolar to picomolar potency against RAF1, BRAF, and ARAF with an IC50 of 0.06-3.46 nM with minimal activity towards non-RAF kinases. Dec 28 2023
E1708 Solutol HS-15 Solutol HS-15(Polyethylene glycol 12-hydroxystearate) is a Macrogol 15 hydroxy stearate, which improves permeability by disrupting the membrane structure/fluidity change. Note: Due to its chemical properties, this product will be semi-solid and solid at room temperature and low temperature. Dec 27 2023