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PTP Inhibitor IV
本半岛bd体育手机客户端 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
包装与价格：
包装 价格(元)
1mg 电议
5mg 电议
10mg 电议
25mg 电议

半岛bd体育手机客户端 介绍
Cas No. 329317-98-8
别名 Protein Tyrosine Phosphatase Inhibitor IV
化学名 N,N'-[1,4-phenylenebis[(1-methylethylidene)-4,1-phenylene]]bis[1,1,1-trifluoro-methanesulfonamide
Canonical SMILES O=S(NC1=CC=C(C(C)(C)C2=CC=C(C(C)(C)C3=CC=C(NS(=O)(C(F)(F)F)=O)C=C3)C=C2)C=C1)(C(F)(F)F)=O
分子式 C26H26F6N2O4S2
分子量 608.6
溶解度 ≤25mg/ml in ethanol;25mg/ml in DMSO;30mg/ml in dimethyl formamide
储存条件 Store at -20℃
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 描述

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).
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