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PTP Inhibitor II
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 II图片
CAS NO:2632-13-5
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
25g电议
50g电议
100g电议

产品介绍
PTP Inhibitor II 是一种蛋白质酪氨酸磷酸酶 (PTP) 抑制剂,具有抗血管生成作用。
Cas No.2632-13-5
别名alpha-溴-4-甲氧基苯乙酮,α-Bromo-4’-methoxyacetophenone|ω-Bromo-4’-methoxyacetophenone|4-(Bromoacetyl)anisole|4-Methoxyphenacyl bromide|NSC 129010|Protein Tyrosine Phosphatase Inhibitor II
化学名2-bromo-1-(4-methoxyphenyl)-ethanone
Canonical SMILESCOC1=CC=C(C(CBr)=O)C=C1
分子式C9H9BrO2
分子量229.1
溶解度≥ 10.85mg/mL in DMSO
储存条件Room temperature
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: 128 μM

PTP Inhibitor II is a protein tyrosine phosphatase (PTP) inhibitor.

Protein tyrosine phosphatases (PTPs) are reported to be involved in the etiology of diabetes mellitus, neural diseases such as Alzheimer and Parkinson diseases, regulation of allergy and inflammation, or PTPs are even regarded to be responsible for the pathogens.

In vitro: In a previous study, it was found that all of the previously reported PTP inhibitors contained a negatively charged, nonhydrolyzable pY mimetic as the core structure, such as malonates, aryl carboxylates, phosphonates, or cinnamates. The poor membrane permeability of these inhibitors might compromise their potential development. It was reported that several α-bromoacetophenone derivatives, such as PTP Inhibitor II, could act as fairly potent PTP inhibitors, by covalently alkylating the conserved catalytic cysteine in the PTP active Site. Since PTP Inhibitor II is neutral, it could readily diffuse into human B cells and inhibit the intracellular PTPs. The SAR study was performed with the catalytic domain of phosphatase SHP-1, and ti was found that PTP Inhibitor II showed time-dependent inactivation of SHP-1, consistent with the mechanism. Furthermore, the potency of PTP Inhibitor II was described by an equilibrium constant KI, representing the dissociation constant of the noncovalent enzyme–inhibitor complex. PTP inhibitor II bound with lower affinity than PTP Inhibitor I with Ki values of 128 μM [1].

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

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

Reference:
[1] P. Heneberg. Use of protein tyrosine phosphatase inhibitors as promising targeted therapeutic drugs. Current Medicinal Chemistry 16(6), 706-733 (2009).