505299 Histone Lysine Demethylase Inhibitor IX, PBIT - Calbiochem

505299
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₄H₁₁NOS

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      Glass bottle 25 mg
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      Description
      OverviewA cell-permeable iron chelating benzisothiazolone compound with microbicide and fungicide properties that acts as a potent, selective, and reversible inhibitor of Jumonji AT-Rich Interactive Domain 1 (JARID1) histone demethylases (IC50 = 3 µM for JARID1B). Also blocks the activity of other related demethylases at higher concentration (IC50 = 6, 4.9, and 28 µM for JARID1A, JARID1C, and JMJD2E, respectively). However, it does affect the activity of unrelated UTX and JMJD3 H3K27me3 demethylases. HeLa cells overexpressing full length JARID1B show a significant reduction in H3K4Me3 activity following PBIT treatment (~10 µM). Blocks the proliferation of UACC-812 tumor cells expressing higher levels of JARDID1B, but does not significantly affect MCF7 or MCF10A cells expressing lower levels of JARDID1B.
      Catalogue Number505299
      Brand Family Calbiochem®
      Synonyms2-(4-Methylphenyl)-1,2-benzisothiazol-3(2H)-one, JHDM Inhibitor V
      References
      ReferencesSayegh, J., et al. 2013. J. Biol. Chem. 288, 9408.
      Product Information
      FormWhite solid
      Hill FormulaC₁₄H₁₁NOS
      Chemical formulaC₁₄H₁₁NOS
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetJARID1 Histone Demethylases
      Purity≥99% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°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 1 month at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Histone Lysine Demethylase Inhibitor IX, PBIT - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Sayegh, J., et al. 2013. J. Biol. Chem. 288, 9408.

      Technical Info

      Title
      White Paper - The Message in the Marks: Deciphering Cancer Epigenetics (EMD)
      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-August-2013 JSW
      Synonyms2-(4-Methylphenyl)-1,2-benzisothiazol-3(2H)-one, JHDM Inhibitor V
      DescriptionA cell-permeable iron chelating benzisothiazolone compound with microbicide and fungicide properties that acts as a potent, selective, and reversible inhibitor of Jumonji AT-Rich Interactive Domain 1 (JARID1) histone demethylases (IC50 = 3 µM for JARID1B). Also blocks the activity of other related demethylases at higher concentration (IC50 = 6, 4.9, and 28 µM for JARID1A, JARID1C, and JMJD2E, respectively). However, it does affect the activity of unrelated UTX and JMJD3 H3K27me3 demethylases. HeLa cells overexpressing full length JARID1B show a significant reduction in H3K4Me3 activity following PBIT treatment (~10 µM). Blocks the proliferation of UACC-812 tumor cells expressing higher levels of JARDID1B, but does not significantly affect MCF7 or MCF10A cells expressing lower levels of JARDID1B.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₄H₁₁NOS
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
      Storage +2°C to +8°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 1 month at -20°C.
      Toxicity Standard Handling
      ReferencesSayegh, J., et al. 2013. J. Biol. Chem. 288, 9408.