181315 | ARE Activator, BTZO-1 - Calbiochem

181315
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₃H₈N₂OS

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      181315-10MG
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          Glass bottle 10 mg
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          Description
          OverviewA 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®
          SynonymsMacrophage Migration Inhibitory Factor Antagonist II, MIF Antagonist II, 2-Pyridin-2-yl-4H-1,3-benzothiazin-4-one, Antioxidant Response Element Activator
          References
          ReferencesKimura, H., et al. 2010. Chem. Biol. 17, 1282.
          Product Information
          FormOff-white solid
          Hill FormulaC₁₃H₈N₂OS
          Chemical formulaC₁₃H₈N₂OS
          Structure formula ImageStructure formula Image
          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

          Documentation

          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
          SynonymsMacrophage Migration Inhibitory Factor Antagonist II, MIF Antagonist II, 2-Pyridin-2-yl-4H-1,3-benzothiazin-4-one, Antioxidant Response Element Activator
          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 +2°C to +8°C
          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.
          Toxicity Regulatory Review
          ReferencesKimura, H., et al. 2010. Chem. Biol. 17, 1282.