505298 | p300/CBP Inhibitor VI, L002 - CAS 321695-57-2 - Calbiochem

505298
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₅H₁₅NO₅S 321695-57-2

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      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.05298.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable phenylsulfonyloxyiminocyclohexadienone compound that acts as a potent, selective, and reversible inhibitor of p300 histone acetyl transferase (IC50 = 1.98 µM). Shown to occupy Ac-CoA binding pocket of p300, and less potent to CBP, PCAF, GCN5 and GNAT. Suppresses Histone H3 and H4 acetylation in triple negative breast cancer cell line MDAMB-468 as well as in HCT116 cell line and blocks p300-mediated STAT3 phosphorylation in pancreatic cancer cell line MIA Paca-2. Does neither inhibit the activities of histone deacetylases 1, 6, and 11 nor 8-diverse histone methyltransferases tested (DOT1, EZH1, G9a, PRMT1, SETD2, SET7-9, SMYD2, and SUV39H2). Reported to suppress tumor growth in mice bearing tumor xenografts of MDAMB-468 cell line (at 500 µg/100 µl, i.p. twice a week).
          Catalogue Number505298
          Brand Family Calbiochem®
          Synonyms4-(4-Methoxyphenylsulfonyloxyimino)-2,6-dimethyl-2,5-cyclohexadien-1-one, GCN5 Inhibitor III, Histone Acetyltransferase Inhibitor IX, PCAF Inhibitor IV
          References
          ReferencesYang, H., et al. 2013. Mol. Cancer Ther. 12, 610.
          Product Information
          CAS number321695-57-2
          FormBrown solid
          Hill FormulaC₁₅H₁₅NO₅S
          Chemical formulaC₁₅H₁₅NO₅S
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary Targetp300 HAT
          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 3 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
          Yang, H., et al. 2013. Mol. Cancer Ther. 12, 610.
          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.

          Revision10-January-2014 JSW
          Synonyms4-(4-Methoxyphenylsulfonyloxyimino)-2,6-dimethyl-2,5-cyclohexadien-1-one, GCN5 Inhibitor III, Histone Acetyltransferase Inhibitor IX, PCAF Inhibitor IV
          DescriptionA cell-permeable phenylsulfonyloxyiminocyclohexadienone compound that acts as a potent, selective, and reversible inhibitor of p300 histone acetyl transferase (IC50 = 1.98 µM). Shown to occupy Ac-CoA binding pocket of p300, and less potent to CBP, PCAF, GCN5 and GNAT. Suppresses Histone H3 and H4 acetylation in triple negative breast cancer cell line MDAMB-468 as well as in HCT116 cell line and blocks p300-mediated STAT3 phosphorylation in pancreatic cancer cell line MIA Paca-2. Does neither inhibit the activities of histone deacetylases 1, 6, and 11 nor 8-diverse histone methyltransferases tested (DOT1, EZH1, G9a, PRMT1, SETD2, SET7-9, SMYD2, and SUV39H2). Reported to suppress tumor growth in mice bearing tumor xenografts of MDAMB-468 cell line (at 500 µg/100 µl, i.p. twice a week).
          FormBrown solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number321695-57-2
          Chemical formulaC₁₅H₁₅NO₅S
          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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesYang, H., et al. 2013. Mol. Cancer Ther. 12, 610.