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509522 Transglutaminase 2 Inhibitor II, ERW1041E - Calbiochem

509522
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₀H₂₁BrN₄O₄

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      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
      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

      Documentation

      Transglutaminase 2 Inhibitor II, ERW1041E - 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
      Chemical formulaC₂₀H₂₁BrN₄O₄
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage -20°C
      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.
      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.