382113 Histone Acetyltransferase p300 Inhibitor, C646 - Calbiochem

382113
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Overview

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Key Specifications Table

Empirical FormulaCAS #
C₂₄H₁₉N₃O₆ 328968-36-1

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382113-10MG
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      Plastic ampoule 10 mg
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      Description
      OverviewA reversible, cell-permeable pyrazolone p300/CBP HAT inhibitor (Ki = 400 nM), which competes with acetyl-CoA for the p300 Lys-CoA binding pocket. This compound demonstrates 86% inhibition against p300 at 10 nM, but elicits less than 10% inhibition against serotonin N-acetyltransferase, PCAF histone acetyltransferase, GCN5 histone acetyletransferase, Rtt109 histone acetyletransferase, Sas histone acetyl transferase, and MOZ histone acetyltransferase in a chemical screening assay. Treatment of C3H 10T1/2 mouse fibroblasts with 25 µM of compound results in an inhibitory effect against basal and TSA-inducible acetylation of histones H3 and H4. It is also shown to inhibit human cell growth in both melanoma and non-small-cell-lung (NSCL) cancer cell lines at 10 µM with similar or higher potency compared with that of the peptide-based bisubstrate p300/CBP HAT inhibitor Lys-CoA-Tat at 25 µM.
      Catalogue Number382113
      Brand Family Calbiochem®
      Synonyms4-(4-{[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene}-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid, p300/CBP Inhibitor IV, Histone Acetyltransferase Inhibitor V, HAT Inhibitor V
      References
      ReferencesBowers, EM., et al. 2010. Chem Biol 17, 471.
      Product Information
      CAS number328968-36-1
      FormBrick red solid
      Hill FormulaC₂₄H₁₉N₃O₆
      Chemical formulaC₂₄H₁₉N₃O₆
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationHistone Acetyltransferase p300 Inhibitor, C646, CAS 328968-36-1, is a cell-permeable, reversible inhibitor of p300/CBP HAT (Ki = 400 nM). Competes with acetyl-CoA for the p300 Lys-CoA binding pocket.
      Biological Information
      Purity≥99% by HPLC (sum of isomers)
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped 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

      Histone Acetyltransferase p300 Inhibitor, C646 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Histone Acetyltransferase p300 Inhibitor, C646 - Calbiochem Certificates of Analysis

      TitleLot Number
      382113

      References

      Reference overview
      Bowers, EM., et al. 2010. Chem Biol 17, 471.

      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.

      Revision19-February-2013 JSW
      Synonyms4-(4-{[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene}-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid, p300/CBP Inhibitor IV, Histone Acetyltransferase Inhibitor V, HAT Inhibitor V
      DescriptionA reversible, cell-permeable pyrazolone p300/CBP HAT inhibitor (Ki = 400 nM), which competes with acetyl-CoA for the p300 Lys-CoA binding pocket. This compound demonstrates 86% inhibition against p300 at 10 nM, but elicits less than 10% inhibition against serotonin N-acetyltransferase, PCAF histone acetyltransferase, GCN5 histone acetyletransferase, Rtt109 histone acetyletransferase, Sas histone acetyl transferase, and MOZ histone acetyltransferase in a chemical screening assay. Treatment of C3H 10T1/2 mouse fibroblasts with 25 µM of compound results in an inhibitory effect against basal and TSA-inducible acetylation of histones H3 and H4. It is also shown to inhibit human cell growth in both melanoma and non-small-cell-lung (NSCL) cancer cell lines at 10 µM with similar or higher potency compared with that of the peptide-based bisubstrate p300/CBP HAT inhibitor Lys-CoA-Tat at 25 µM.
      FormBrick red solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number328968-36-1
      Chemical formulaC₂₄H₁₉N₃O₆
      Structure formulaStructure formula
      Purity≥99% by HPLC (sum of isomers)
      SolubilityDMSO (50 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
      ReferencesBowers, EM., et al. 2010. Chem Biol 17, 471.