Transglutaminase 2 Inhibitor II, ERW1041E-Calbiochem

半岛bd体育手机客户端 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, K_i= 11 ?M). 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, K_i= 11 ?M). 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

半岛bd体育手机客户端 性质

质量水平	100
测定	≥98% (HPLC)
形式	solid
效能	11 μM Ki
manufacturer/tradename	Calbiochem?
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
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable