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509522 Transglutaminase 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).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: TG2 Inhibitor, TGM2 Inhibitor

Primary Target: TGM2
509522
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
918440-87-6C₂₀H₂₁BrN₄O₄

Products

Catalogue NumberPackaging Qty/Pack
5.09522.0001 Glass bottle 5 mg
Description
OverviewA 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 Number509522
Brand Family Calbiochem®
SynonymsTG2 Inhibitor, TGM2 Inhibitor
References
ReferencesDiRaimond, 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.
Product Information
CAS number918440-87-6
FormOff-white solid
Hill FormulaC₂₀H₂₁BrN₄O₄
Chemical formulaC₂₀H₂₁BrN₄O₄
Quality LevelMQ100
Applications
Biological Information
Primary TargetTGM2
Primary Target K<sub>i</sub>11 µ
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
5.09522.0001 04055977240955

Documentation

Transglutaminase 2 Inhibitor II, ERW1041E - CAS 918440-87-6 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
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.

Revision30-May-2014 JSW
SynonymsTG2 Inhibitor, TGM2 Inhibitor
DescriptionA 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.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number918440-87-6
Chemical formulaC₂₀H₂₁BrN₄O₄
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesDiRaimond, 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.