5.09522
ERW1041E
≥98% (HPLC), solid, TG2 inhibitor, Calbiochem®
别名:
Transglutaminase 2 Inhibitor II, ERW1041E, TG2 Inhibitor, TGM2 Inhibitor
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关于此项目
经验公式（希尔记法）:
C20H21BrN4O4
化学文摘社编号:
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
产品名称
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)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable