PTP1B-IN-2
A PTP1B inhibitor
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包装价格促销价数量
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1mg￥550.00440.00- +
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5mg￥1625.001300.00- +
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10mg￥2287.001830.00- +
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50mg￥6800.005440.00- +
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100mg￥10575.008460.00- +
- 货号: ajce46890
- CAS: 1919853-46-5
- 别名: Protein Tyrosine Phosphatase 1B Inhibitor 2
- 分子式: C34H36N2O9S2
- 分子量: 680.79
- 纯度: ＞98%
- 溶解度: DMSO : ≥ 100 mg/mL (146.89 mM)
- 储存: Store at -20°C
- 库存: 现货
Background
PTP1B-IN-2 is an inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC50 = 50 nM).1 It is selective for PTP1B over T cell protein tyrosine phosphatase (TCPTP), Src homology region 2 domain-containing phosphatase 1 (SHP-1), SHP-2, and leukocyte common antigen-related (LAR) phosphatase (IC50s = 760, 2,450, 2,160, and 12,610 nM, respectively). PTP1B-IN-2 (5-20 ?M) enhances insulin-induced glucose uptake in L6 myotubes.
1.Liu, P., Du, Y., Song, L., et al.Discovery of novel, high potent, ABC type PTP1B inhibitors with TCPTP selectivity and cellular activityEur. J. Med. Chem.11827-33(2016)
Protocol
Kinase experiment: | PTP1B-IN-2 is predispensed in 96-well microplates as 1.0 μL aliquots per well in 100% DMSO. The PTP1B enzymatic assay is carried out in a total volume of 100 μL per well in assay plates with 15 nM recombinant PTP1B protein, 2 mM p-nitrophenylphosphonic acid (pNPP), 1 mM dithiothreitol and 1 mM EDTA (pH 6.5). After 30 min incubation at 37oC, the reaction is terminated by addition of 2.5 M NaOH. The amount of hydrolysis product, pNP, is monitored by detection of the absorbance at 405 nm[1]. |
参考文献: [1]. 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. | |
