HomeAll New Products Listed Chronologically

All New Products Listed Chronologically

Catalog No. Product Name Information Isotype
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