Sigma-Aldrich Transglutaminase 2 Inhibit

Product Name

Transglutaminase 2 Inhibitor II, ERW1041E, null

Assay

≥98% (HPLC)

Quality Level

100

Form

solid

Potency

11 μM K_i

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

off-white

Solubility

DMSO: 100 mg/mL

Storage Temp.

−20°C

General Description

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.

Biochem/Physiol Actions

Primary Target
TGM2

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

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