5.09522
ERW1041E
≥98% (HPLC), solid, TG2 inhibitor, Calbiochem®
別名:
Transglutaminase 2 Inhibitor II, ERW1041E, TG2 Inhibitor, TGM2 Inhibitor
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この商品について
実験式（ヒル表記法）:
C20H21BrN4O4
CAS番号:
分子量:
461.31
UNSPSC Code:
12352200
NACRES:
NA.77
PubChem Substance ID:
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
製品名
Transglutaminase 2 Inhibitor II, ERW1041E,
assay
≥98% (HPLC)
Quality Segment
form
solid
potency
11 μM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
DMSO: 100 mg/mL
storage temp.
−20°C
SMILES string
C1CC(N(C1)C(=O)OCC2=CC3=CC=CC=C3N=C2)C(=O)NCC4CC(=NO4)Br
General description
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.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Primary Target
TGM2
TGM2
Packaging
Packaged under inert gas
Other Notes
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.
Dafik, L., et al. 2012. PLoS One.7, e30642.
Watts, R.W., et al. 2006. J. Med. Chem.49, 7493.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
保管分類
11 - Combustible Solids
一体何が起きているの？
WGK 3
引火点 (F)
Not applicable
引火点（°C）
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
509522-50MG: + 5095220001: + 5095220002:
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