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PTP1B-IN-2
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PTP1B-IN-2图片
CAS NO:1919853-46-5
规格:98%
分子量:680.79
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
PTP1B-IN-2是有效地蛋白酪氨酸磷酸酶(PTP1B)抑制剂,IC50值为50nM。
CAS:1919853-46-5
分子式:C34H36N2O9S2
分子量:680.79
纯度:98%
存储:Store at -20°C

Background:

PTP1B-IN-2 is a potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 50 nM.


PTP1B-IN-2 displays more than 40-fold selectivity for PTP1B over SHP-2 and LAR and 15-fold higher selectivity for PTP1B over the highly homologous TCPTP. PTP1B-IN-2 extends deep into the active site pocket, forming several 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 type inhibitor which not only interacted with catalytic site but also B site and C site. PTP1B-IN-2 greatly enhances insulin-mediated IRβ phosphorylation at concentrations of 15 µM and 30 µM. Insulin-stimulated glucose uptake 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 µM, respectively [1].



[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.