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PTP Inhibitor IV

 
Catalog No.
C4401
PTP抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,679.00
Ship with 10-15 days
10mg
¥ 2,654.00
Ship with 10-15 days
25mg
¥ 4,550.00
Ship with 10-15 days

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A

背景

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).

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt608.6
Cas No.329317-98-8
FormulaC26H26F6N2O4S2
SynonymsProtein Tyrosine Phosphatase Inhibitor IV
Solubility≤25mg/ml in ethanol;25mg/ml in DMSO;30mg/ml in dimethyl formamide
Chemical NameN,N'-[1,4-phenylenebis[(1-methylethylidene)-4,1-phenylene]]bis[1,1,1-trifluoro-methanesulfonamide
SDFDownload SDF
Canonical SMILESO=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
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Chemical structure

PTP Inhibitor IV