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509522
Sigma-AldrichTransglutaminase 2 Inhibitor II, ERW1041E - CAS 918440-87-6 - Calbiochem
A cell-permeable, active-site directed, acyl-donor substrate competitive inhibitor of transglutaminase 2 (TG2, Ki = 11 µM).
More>>A cell-permeable, active-site directed, acyl-donor substrate competitive inhibitor of transglutaminase 2 (TG2, Ki = 11 µM). Less<<
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Description
Overview
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.
Catalogue Number
509522
Brand Family
Calbiochem®
Synonyms
TG2 Inhibitor, TGM2 Inhibitor
References
References
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.
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.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
30-May-2014 JSW
Synonyms
TG2 Inhibitor, TGM2 Inhibitor
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.
Form
Off-white solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
918440-87-6
Chemical formula
C₂₀H₂₁BrN₄O₄
Purity
≥98% by HPLC
Solubility
DMSO (100 mg/ml)
Storage
Protect from light -20°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
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.
