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PTP Inhibitor I
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 I图片
CAS NO:2491-38-5
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5g电议
10g电议
25g电议
50g电议

产品介绍
PTP Inhibitor I 一种 PTP1B 抑制剂，Ki 为 42 μM.
Cas No.2491-38-5
别名2-溴-4'-羟基苯乙酮,α-Bromo-4-hydroxyacetophenone|2-Bromo-4'-hydroxyacetophenone|4-Hydroxyphenacyl bromide|Protein Tyrosine Phosphatase Inhibitor I|SHP-1 Inhibitor II
化学名2-bromo-1-(4-hydroxyphenyl)-ethanone
Canonical SMILESOC1=CC=C(C(CBr)=O)C=C1
分子式C8H7BrO2
分子量215.0
溶解度≥ 11.5mg/mL in DMSO
储存条件Room temperature,unstable in solution, ready to use.
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

KI: 43 and 42 μM for SHP-1 and PTP1B, respectively.

PTP Inhibitor I is a tyrosine phosphatase (PTP) inhibitor.

Protein tyrosine phosphatases (PTPs) are considered to be involved in the etiology of diabetes mellitus, neural diseases such as Alzheimer’s and Parkinson’s disease, regulation of allergy and inflammation. PTPs are also considered to be responsible for the pathogens’ virulence.

In vitro: In previous study, the corresponding values of PTP Inhibitor I against PTP1B were determined to be KI of 42 μM, kinact of 0.57 min-1, and kinact/KI of 1.4*104 M-1 min-1, respectively. This study also showed that α-bromoacetophenone such as PTP Inhibitor I could provide an effective, neutral pY mimetic inhibitor of PTPs. While perturbation of the electronic properties of the phenyl ring did not significantly improve its potency against PTPs, attachment of a proper peptidyl moiety to the para position could improve both the potency and the selectivity substantially. In addition, since the covalent PTP inhibitor complex could be cleaved to regenerate the PTP activity photolytically, PTP Inhibitor I might provide a novel class of photolytic switch for controlling cellular signaling processes [1].

In vivo: Currently, there is no animal in vivo data reported.

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

Reference:
[1] Arabaci G, Yi T, Fu H, Porter ME, Beebe KD, Pei D.  alpha-bromoacetophenone derivatives as neutral protein tyrosine phosphatase inhibitors: structure-Activity relationship. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3047-50.