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Sigma-Aldrich

Transglutaminase 2 Inhibitor II, ERW1041E

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Synonym(s):
Transglutaminase 2 Inhibitor II, ERW1041E, TG2 Inhibitor, TGM2 Inhibitor
Empirical Formula (Hill Notation):
C20H21BrN4O4
CAS Number:
Molecular Weight:
461.31
PubChem Substance ID:

assay

≥98% (HPLC)

Quality Level

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

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This Item
444286-M5.083185.04651
MMP-2 Inhibitor II The MMP-2 Inhibitor II, also referenced under CAS 869577-51-5, controls the biological activity of MMP-2. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

444286-M

MMP-2 Inhibitor II

Sigma-Aldrich

5.08318

SHIP2 Inhibitor II, CPDA

PERK Inhibitor II, GSK2656157

5.04651

PERK Inhibitor II, GSK2656157

form

solid

form

solid

form

solid

form

powder

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage temp.

−20°C

storage temp.

−20°C

storage temp.

2-8°C

storage temp.

−20°C

solubility

DMSO: 100 mg/mL

solubility

DMSO: 200 mg/mL

solubility

DMSO: 100 mg/mL

solubility

DMSO: 100 mg/mL

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.
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.

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.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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