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PTP Inhibitor IV
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。
PTP Inhibitor IV图片
CAS NO:329317-98-8
规格:98%
分子量:608.6
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
PTP inhibitor
CAS:329317-98-8
分子式:C26H26F6N2O4S2
分子量:608.6
纯度:98%
存储:Store at -20°C

Background:

IC50: 1.8, 2.5, 8.4, 13, 20, 6.4, and 6.7 μM for SHP-2, PTP1B, PTP-ε, PTP-Meg-2, PTP-σ, PTP-β, and PTP-μ, respectively


PTP Inhibitor IV is a protein tyrosine phosphatases (PTPs) inhibitor.


PTPs are reported to be important in the regulation of various signal transduction processes. Enzymes of this class are considered as potential therapeutic targets in the treatment of various diseases including inflammation, diabetes, as well as cancer. However, previously identified PTP inhibitors are peptide-based containing a highly charged component, which usually lack membrane permeability resulting in their limited utility in the inhibition of intracellular phosphatases.


In vitro: PTP inhibitor IV was identified as an uncharged, 1,4-di-substituted, phenyl-linked bis-trifluoromethylsulfonamido phosphate mimetic acting as a competitive, reversible, and active-site directed inhibitor. It was noticed that PTP inhibitor IV showed greatly increased potency not only on PTP1B but also on the phosphatases SHP-2 and Mu. Moreover, the interaction of the second SO2CF3 moiety in PTP inhibitor IV with conserved Arg residue of PTP might explain the increased inhibitory potency towards other PTPs in addition to PTP1B [1].


In vivo: Up to now, there is no animal in vivo data reported.


Clinical trial: So far, no clinical study has been conducted.


Reference:
[1] Huang, P. ,Ramphal, J.,Wei, J., et al. Structure-based design and discovery of novel inhibitors of protein tyrosine phosphatases. Bioor.Med.Chem. 11, 1835-1849 (2003).