5.09522

Transglutaminase 2 Inhibitor II, ERW1041E

• 别名: Transglutaminase 2 Inhibitor II, ERW1041E, TG2 Inhibitor, TGM2 Inhibitor
• 经验公式（希尔记法）: C₂₀H₂₁BrN₄O₄
• CAS号: 918440-87-6
• 分子量: 461.31
• 分類程式碼代碼: 12352200
• PubChem物質ID: 16094751

属性

• 化驗: ≥98% (HPLC)
• 品質等級: 100
• 形狀: solid
• 效力: 11 μM K_i
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: off-white
• 溶解度: DMSO: 100 mg/mL
• 儲存溫度: −20°C
• SMILES 字串: C1CC(N(C1)C(=O)OCC2=CC3=CC=CC=C3N=C2)C(=O)NCC4CC(=NO4)Br

说明

一般說明

A cell-permeable, dihydroisoxazole compound that acts as an active-site directed, acyl-donor substrate competitive inhibitor of transglutaminase 2 (TG2, K_i = 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, K_i = 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

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

其他說明

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.

法律資訊

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

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable