5.09522

ERW1041E

≥98% (HPLC), solid, TG2 inhibitor, Calbiochem^®

• Synonym(e): Transglutaminase 2 Inhibitor II, ERW1041E, TG2 Inhibitor, TGM2 Inhibitor
• Empirische Formel (Hill-System): C₂₀H₂₁BrN₄O₄
• CAS-Nummer: 918440-87-6
• Molekulargewicht: 461.31
• UNSPSC-Code: 12352200
• PubChem Substanz-ID: 16094751
• NACRES: NA.77

Eigenschaften

• product name: Transglutaminase 2 Inhibitor II, ERW1041E,
• Assay: ≥98% (HPLC)
• Qualitätsniveau: 100
• Form: solid
• Wirksamkeit: 11 μM K_i
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: off-white
• Löslichkeit: DMSO: 100 mg/mL
• Lagertemp.: −20°C
• SMILES String: C1CC(N(C1)C(=O)OCC2=CC3=CC=CC=C3N=C2)C(=O)NCC4CC(=NO4)Br

Beschreibung

Allgemeine Beschreibung

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. Wirkung

Primary Target
TGM2

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Sonstige Hinweise

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.

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable