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181315 ARE Activator, BTZO-1 - Calbiochem

181315
  
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      Overview

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₁₃H₈N₂OS
      Description
      Overview

      This product has been discontinued.



      A cell-permeable benzothiazinone that is shown to interact with MIF homotrimer (Kd = 68.6 nM and 157 nM toward human and rat MIF, respectively, at pH 7.3) via the N-terminal proline in a pH-dependent manner, limiting its inhibitory capability against MIF tautomerase activity (13% inhibition at pH 6.0; [BTZO-1] = 30 µM) due to reduced MIF binding at acidic pH. Shown to protect primary rat cardiomyocytes (330 nM) from apoptotic death upon serum deprivation or DOX (200 nM; Cat. No. 324380) treatment via activation of ARE- (antioxidant response element) mediated cytoprotective genes transcription in a MIF-dependent manner.

      Catalogue Number181315
      Brand Family Calbiochem®
      Synonyms2-Pyridin-2-yl-4H-1,3-benzothiazin-4-one, Antioxidant Response Element Activator, Macrophage Migration Inhibitory Factor Antagonist II, MIF Antagonist II
      References
      ReferencesKimura, H., et al. 2010. Chem. Biol. 17, 1282.
      Product Information
      FormOff-white solid
      Hill FormulaC₁₃H₈N₂OS
      Chemical formulaC₁₃H₈N₂OS
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      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 Regulatory Review
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freez e(-20°C). Stock solutions are stable for up to 6 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
      181315 0

      Documentation

      ARE Activator, BTZO-1 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Kimura, H., et al. 2010. Chem. Biol. 17, 1282.
      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.

      Revision18-July-2012 JSW
      Synonyms2-Pyridin-2-yl-4H-1,3-benzothiazin-4-one, Antioxidant Response Element Activator, Macrophage Migration Inhibitory Factor Antagonist II, MIF Antagonist II
      DescriptionA cell-permeable benzothiazinone that is shown to interact with MIF homotrimer (Kd = 68.6 nM and 157 nM toward human and rat MIF, respectively, at pH 7.3) via the N-terminal proline of each subunit in a pH-dependent manner, limiting its inhibitory capability against MIF tautomerase activity at acidic pH (13% inhibition at pH 6.0; [BTZO-1] = 30 µM) due to reduced MIF binding at acidic pH. Shown to prevent primary rat cardiomyocyte apoptotic death upon serum deprivation (2.38-fold of no-drug control survival rate after 4 days; [BTZO-1] = 330 nM) or DOX (200 nM; Cat. No. 324380) treatment (95% vs. 40% viability after 18 h, respectively, with or without 330 nM BTZO-1) via activation of ARE- (antioxidant response element) mediated cytoprotective genes transcription (5.3- and 3.6-fold, respectively, of control STS Ya and HO-1 mRNA after 24 h; [BTZO-1] = 1 µM) in a MIF-dependent manner.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₃H₈N₂OS
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freez e(-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Regulatory Review
      ReferencesKimura, H., et al. 2010. Chem. Biol. 17, 1282.