5.09522

ERW1041E

≥98% (HPLC), solid, TG2 inhibitor, Calbiochem^®

• 別名: Transglutaminase 2 Inhibitor II, ERW1041E, TG2 Inhibitor, TGM2 Inhibitor
• 実験式（ヒル表記法）: C₂₀H₂₁BrN₄O₄
• CAS番号: 918440-87-6
• 分子量: 461.31
• UNSPSCコード: 12352200
• PubChem Substance ID: 16094751
• NACRES: NA.77

特性

• 製品名: Transglutaminase 2 Inhibitor II, ERW1041E,
• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• フォーム: solid
• 有効性: 11 μM K_i
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: off-white
• 溶解性: DMSO: 100 mg/mL
• 保管温度: −20°C
• SMILES記法: C1CC(N(C1)C(=O)OCC2=CC3=CC=CC=C3N=C2)C(=O)NCC4CC(=NO4)Br

詳細

詳細

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.

生物化学的／生理学的作用

Primary Target
TGM2

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable