PTP1B-IN-2 - Phosphatase 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPTP1B-IN-2Cat. No.: HY-100462CAS No.: 1919853-46-5分式: CHNOS分量: 680.79作靶点: Phosphatase作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (146.89 mM)* mea

2、ns soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.4689 mL 7.3444 mL 14.6888 mL5 mM 0.2938 mL 1.4689 mL 2.9378 mL10 mM 0.1469 mL 0.7344 mL 1.4689 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 PTP1B-IN-2有效地蛋酪氨酸磷酸酶 (PTP1B) 抑制剂，IC50值为50 nM。IC5

3、0 & Target IC50: 50 nM (PTP1B) 1体外研究PTP1B-IN-2 displays more than 40-fold selectivity for PTP1B over SHP-2 and LAR and 15-fold higherselectivity for PTP1B over the highly homologous TCPTP. PTP1B-IN-2 extends deep into the active site1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEpocket, forming se

4、veral hydrogen bonds and hydrophobic interactions with key residues of the catalytic site.The binding characteristics between PTP1B domain and ligand shows that PTP1B-IN-2 is an ABC typeinhibitor which not only interacted with catalytic site but also B site and C site. PTP1B-IN-2 greatly enhancesins

5、ulin-mediated IR phosphorylation at concentrations of 15 M and 30 M. Insulin-stimulated glucoseuptake is also significantly increased in L6 myotubes treated with PTP1B-IN-2, and this increase is 16.0%,19.0% and 38.1% at 5, 10 and 20 M, respectively 1.PROTOCOLKinase Assay 1 PTP1B-IN-2 is predispensed

6、 in 96-well microplates as 1.0 L aliquots per well in 100% DMSO. The PTP1Benzymatic assay is carried out in a total volume of 100 L per well in assay plates with 15 nM recombinantPTP1B protein, 2 mM p-nitrophenylphosphonic acid (pNPP), 1 mM dithiothreitol and 1 mM EDTA (pH 6.5).After 30 min incubati

7、on at 37oC, the reaction is terminated by addition of 2.5 M NaOH. The amount ofhydrolysis product, pNP, is monitored by detection of the absorbance at 405 nm 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Liu P, et al. Discovery of novel, high potent, ABC type PTP1B inhibitors with TCPTP selectivity and cellular activity. Eur J Med Chem.2016 Aug 8;118:27-33.McePdfHeightCaution: Product has not been fully validated for medical applications.For rese