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All New Products Listed Chronologically
| Catalog No. | Product Name | Information | Isotype |
|---|---|---|---|
| E4800 | BML-284 | Nov 25 2024 | |
| E4719 | XYL-1 | Nov 25 2024 | |
| E4637 | PK 11195 | Nov 25 2024 | |
| E4793 | Bucladesine calcium | Nov 25 2024 | |
| E4681 | PF-07799933 | Nov 24 2024 | |
| E6015 | Heparin Lithium salt | Nov 24 2024 | |
| E6009 | Esomeprazole | Nov 24 2024 | |
| E6014 | Primaquine | Nov 21 2024 | |
| E4995 | Cl-amidine hydrochloride | Nov 21 2024 | |
| E6013 | Sivelestat (sodium) | Nov 21 2024 | |
| E1628 | BMS-911172 | Nov 21 2024 | |
| E4657 | PFI-6 | Nov 20 2024 | |
| E4977 | Zileuton (sodium) | Nov 20 2024 | |
| S7615 | MS417 | 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 |
| 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. | Nov 14 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 |
| 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. | 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 |
| E6007 | Pexidartinib hydrochloride | Pexidartinib Hydrochloride (PLX-3397 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. | 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 |
| A2166 | Anti-mouse CD28(37.51)-InVivo | Anti-mouse CD28(37.51)-InVivo reacts with mouse CD28, a 45 kDa costimulatory receptor and a member of the Ig superfamily. CD28 is expressed by thymocytes, most peripheral T cells, and NK cells. | Nov 07 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 |
| 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. | 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 |
| 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. | 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 |
| 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. | 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 |
| 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). | 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 |
| S9463 | Demecarium Bromide | Demecarium Bromide, an anticholinesterase, is an inhibitor of monoamine oxidase (MAO). It induces long-term miosis and decreases intraocular pressure (IOP) in normotensive eyes of Beagles and of eyes of Beagles with inherited glaucoma. | Dec 26 2023 |
| E1538 | PRGL493 | PRGL493 is a potent and selective inhibitor of long-chain acyl-CoA synthetase 4 (ACSL4). PRGL493 blocks cell proliferation and tumor growth in both breast and prostate cellular and animal models. PRGL493 is used for cancer research. | Dec 26 2023 |
| E1775 | 2,4-Thiazolidinedione | 2,4-Thiazolidinedione (Thiazolidinedione), an insulin sensitizer, is a specific agonist of peroxisome proliferator-activated receptor (PPAR)γ. Thiazolidinedione treatment corrects impaired muscle insulin action in vivo. | Dec 26 2023 |
| E1773 | Fasoracetam (NS 105) | Fasoracetam (NS 105) is a metabotropic glutamate receptor activator with a potential to treat vascular dementia. | Dec 26 2023 |
| E1714 | B022 | B022 is a potent and selective NF-κB-inducing kinase (NIK) inhibitor with a Ki of 4.2 nM. B022 protects liver from toxin-induced inflammation, oxidative stress, and injury. | Dec 26 2023 |
| E1734 | OD36 | OD36 is an inhibitor of RIPK2 with an IC50 value of 5.3 nM. OD36 is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. | Dec 24 2023 |
| E2983 | PF-04957325 | PF-04957325 is a highly potent and selective inhibitor of PDE8, with IC50 values of 0.7 nM and 0.3 nM for PDE8A and PDE8B, respectively. PF-04957325 greatly potentiates steroidogenesis in wild type adrenal cells. | Dec 20 2023 |
| E1618 | TC-S 7009 | TC-S 7009 is a potent and selective inhibitor of HIF-2α with a Kd value of 81 nM. TC-S 7009 is more selective for HIF-2α than HIF-1α. It disrupts HIF-2α heterodimerization, decreases DNA-binding activity, and reduces HIF-2α target gene expression. | Dec 20 2023 |
| S2520 | CD437(AHPN) | CD437(AHPN), a synthetic retinoid, is a selective Retinoic acid Receptor γ ( RARγ) agonist. It exhibits an antiproliferative effect and induces apoptosis via activation of AP-1 in vitro. | Dec 18 2023 |
| E1780 | Alexidine dihydrochloride | Alexidine dihydrochloride, a dibiguanide compound, is an effective and selective inhibitor of protein tyrosine phosphatases localized to mitochondrion 1 (PTPMT1) with an IC50 of 1.08 μM in vitro. It has the potential to treat type II diabetes. | Dec 18 2023 |
| E1605 | Avotaciclib trihydrochloride | Avotaciclib trihydrochloride(BEY1107 trihydrochloride) is a potent and orally active inhibitor of cyclin dependent kinase 1 (CDK1). It can be used for the research of locally advanced or metastatic pancreatic cancer. | Dec 17 2023 |
| E1678 | SPOP-i-6lc | SPOP-i-6lc is a selective speckle-type POZ protein (SPOP) E3 ubiquitin ligase inhibitor with IC50 of 2.1 μM and 3.5 μM, in A498 and OS-RC-2 cell lines, respectively. In vitro, It suppresses viability and proliferation of A498 and OS-RC-2 kidney cancer cell lines. | Dec 17 2023 |
| E1743 | VX-561(CTP-656) | VX-561 (CTP-656) is a potent CFTR modulator and exhibits an EC50 value of 255 nM for CFTR potentiation in G551D/F508del HBE cells. | Dec 17 2023 |
| A3174 | Mosunetuzumab (Anti-CD20 & CD3e) | Mosunetuzumab (Anti-CD20 & CD3e) is expressed from CHO. The heavy chain type is IgG1, and the light chain type is hukappa. MW: 146.72 kDa. | Dec 14 2023 |
| E1028 | POMHEX | POMHEX, is a potent ENO2 -specific inhibitor of enolase and a racemic mixture, a cell-permeable pivaloyloxymethyl (POM) prodrug of HEX. It is also glycolysis inhibitor and can be used for the research of cancer. | Dec 13 2023 |
| E1203 | Sirpiglenastat | Sirpiglenastat (DRP-104) is a broad acting glutamine antagonist. It has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response with immunomodulatory and antineoplastic activities. | Dec 13 2023 |
| S8091 | 25-Hydroxycholesterol | 25-Hydroxycholesterol is a side-chain oxysterol and a selective suppressor of IgA production by B cells with an EC50≈65 nM. It affects the immune system and has a key role in the pathogenesis of atherosclerosis. | Dec 12 2023 |
| E1409 | Zidesamtinib | Zidesamtinib (NVL-520) is a potent brain-penetrating inhibitor of ROS1 tyrosine kinase with IC50 of 0.7 nM for wild-type ROS1 . It acts as a potential antineoplastic agent and can be used for the research of cancer. | Dec 11 2023 |
| S8395 | INDY | INDY, a benzothiazole derivative is a potent and ATP-competitive inhibitor of Dyrk1A and Dyrk1B with an IC50 value of 0.24 μM and Ki value of 0.18 μM, respectively. INDY diminishes the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells. | Dec 11 2023 |
| E1636 | MV1035 | MV1035, an inhibitor of ALKBH5 significantly reduces GBM U87-MG cell migration and invasiveness through inhibition of the RNA demethylase ALKBH5. | Dec 11 2023 |
| E1598 | VT103 | VT103 is an orally active and selective inhibitor of TEAD1 protein palmitoylation with anti-proliferative and anti-tumor activity. It also inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation and disrupts interaction between YAP/TAZ and TEAD. | Dec 07 2023 |
| E1735 | PK11007 | PK11007 is a thiol-reactive anticancer agent that stabilizes p53 via selective alkylation of two surface cysteines without compromising its DNA binding. It induces mutant p53 cancer cell death by increasing reactive oxygen species (ROS) levels. | Dec 07 2023 |
| E1684 | C1632 | C1632 (Lin28-let-7 antagonist 1) is a RNA-binding protein and a potent antagonist of Lin28/pre-let-7 interaction. It inhibits Lin28A binding to pre-let-7a-2, with an IC50 of 8 μM as well as inhibits proliferation in human cancer cells. | Dec 07 2023 |
| E1512 | M3541 | M3541 is a potent and selective inhibitor of ATM kinase activity with an IC50 value of 0.25 nM in cell-free assays. M3541 suppresses double-strand breaks (DSB) repair, clonogenic cancer cell growth and potentiates antitumor activity of ionizing radiation in cancer cell lines. | Dec 06 2023 |
| E1638 | ALKBH5 inhibitor 2 (Cpd 20m) | ALKBH5 inhibitor (Cpd 20m) is a potent and selective inhibitor of RNA m6A demethylase AlkB homolog 5 ALKBH5 with IC50 of 21 nM. | Dec 05 2023 |
| A3173 | Minretumomab (CC-49) | Minretumomab (CC-49) is a monoclonal antibody against TAG-72 (tumor-associated glycoprotein 72). Minretumomab can be used in cancer and immunity research. | Dec 04 2023 |
| A2136 | Anti-mouse CD40-InVivo | Anti-mouse CD40-InVivo reacts with mouse CD40 also known as Bp50. CD40 is a type I transmembrane glycoprotein that belongs to the tumor necrosis factor receptor (TNFR) superfamily. | Dec 04 2023 |
| A2137 | Anti-mouse CD8β (Lyt 3.2)-InVivo | Anti-mouse CD8β (Lyt 3.2)-InVivo reacts with mouse CD8β also known as Lyt 3.2. The CD8 antigen is a transmembrane glycoprotein that acts as a co-receptor for the T cell receptor (TCR). | Dec 04 2023 |
| A2138 | Anti-mouse IL-2-InVivo | Anti-mouse IL-2-InVivo reacts with mouse IL-2, a cytokine that is mainly produced by T cells in response to antigenic or mitogenic stimulation | Dec 04 2023 |
| A2140 | Anti-mouse/human/rat CD47 (IAP)-InVivo | Anti-mouse/human/rat CD47 (IAP)-InVivo reacts with mouse CD47 otherwise known as integrin-associated protein (IAP). CD47 is an approximately 50 kDa glycosylated five transmembrane protein that is ubiquitously expressed by both hematopoietic cells such as T and B lymphocytes, monocytes, platelets and erythrocytes and non-hematopoietic cells. | Dec 04 2023 |
| E1603 | ACT001(DMAMCL) | ACT001(DMAMCL, dimethylaminomicheliolide) is a PAI-1 inhibitor and exerts antitumor effects on neuroblastoma (NB) both in vitro and in vivo. It also exerts synergistic effects in combination with cisplatin through the inhibition of the PAI-1/PI3K/AKT pathway. | Nov 29 2023 |
| E1497 | Tulmimetostat | Tulmimetostat (CPI-0209) is an orally bioavailable and selective inhibitor of EZH2 that has therapeutic potential for androgen receptor-dependent prostate cancer. | Nov 26 2023 |
| E4037 | L-Canavanine sulfate | L-Canavanine sulfate is a selective inhibitor of inducible NO synthase. L-Canavanine sulfate exhibits IC50 values ranging from 5 to 10 mM in arginine-rich media and causes a limited degree of cytotoxicity in HeLa, Hep G2, and SK-HEP-1 cells. | Nov 26 2023 |
| E1731 | JW74 | JW74 is a specific inhibitor of the canonical Wnt signaling with IC50 790 nM in the ST-Luc assay. It inhibit the growth of tumor cells in both mouse xenograft model of colorectal cancer and in ApcMin mice. | Nov 26 2023 |
| E4031 | 8-Cyclopentyl-1,3-dimethylxanthine | 8-Cyclopentyl-1,3-dimethylxanthine is a selective adenosine A1 receptor antagonist with Ki's of 10.9 nM and 1440 nM for A1 receptor and A2 receptor, respectively. | Nov 26 2023 |
| E1733 | PBIT | PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. It inhibits JARID1B (KDM5B/PLU1), JARID1Aand JARID1C with an IC50 of 3 μM, 6 μM and 4.9 μM respectively. It is capable of inhibiting the multiplication of breast cancer cell lines expressing high levels of JARIDB1. | Nov 26 2023 |
| E1574 | FSEN1 | FSEN1 is a potent and non-competitive FSP1 inhibitor with an IC50 value of 313 nM. It triggers iron death in cancer cells by inhibiting FSP1 and can be used in research of cancer. | Nov 26 2023 |
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