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Transglutaminase 2 Inhibitor II, ERW1041E-Calbiochem

品牌
Sigma-Aldrich
货号
5.09522
规格纯度
A cell-permeable, active-site directed, acyl-donor substrate competitive inhibitor of transglutaminase 2 (TG2, Ki = 11 μM).
参考价格
3024.64 *本价格含增值税费
促销
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  • 包邮
  • 增值税票
数量
-+
产品名称:
Transglutaminase 2 Inhibitor II, ERW1041E-Calbiochem
TG2 Inhibitor, TGM2 Inhibitor
产品介绍:

产品说明

一般描述

A cell-permeable, dihydroisoxazole compound that acts as an active-site directed, acyl-donor substrate competitive inhibitor of transglutaminase 2 (TG2, Ki = 11 µM). Shown to bind to the active site cysteine. Blocks 5-biotinylamido pentylamine (5BP)-induced TG2 activation in C57BL/6 mice lung in a dose-dependent manner and reduces hypoxia-induced pulmonary hypertension. Blocks poly(I:C)-induced TG2 activity in small intestine without affecting villous atrophy. Exhibits good selectivity over TG3 and Factor XIIIa, but has equipotent effect on TG1. It is well-tolerated by mice (~50 mg/kg) and displays moderate pharmacokinetic properties with t1/2= 12 h.
A cell-permeable, dihydroisoxazole compound that acts as an active-site directed, acyl-donor substrate competitive inhibitor of transglutaminase 2 (TG2, Ki = 11 µM). Shown to bind to the active site cysteine. Blocks 5-biotinylamido pentylamine (5BP)-induced TG2 activation in C57BL/6 mice lung in a dose-dependent manner and reduces hypoxia-induced pulmonary hypertension. Blocks poly(I:C)-induced TG2 activity in small intestine without affecting villous atrophy. Exhibits good selectivity over TG3 and Factor XIIIa, but has equipotent effect on TG1. It is well-tolerated by mice (~50 mg/kg) and displays moderate pharmacokinetic properties with t1/2= 12 h.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

生化/生理作用

Primary Target
TGM2

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

其他说明

DiRaimond, T.R., et al. 2014. ACS Chem. Biol.9, 266.
Dafik, L., et al. 2012. PLoS One.7, e30642.
Watts, R.W., et al. 2006. J. Med. Chem.49, 7493.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式C20H21BrN4O4
分子量461.31

产品性质

质量水平100
测定≥98% (HPLC)
形式solid
效能11 μM Ki
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 off-white
溶解性DMSO: 100 mg/mL
储存温度−20℃

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

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