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382113 Histone Acetyltransferase p300 Inhibitor, C646 - Calbiochem

382113
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Descripción

Replacement Information

Tabla espec. clave

Empirical FormulaCAS #
C₂₄H₁₉N₃O₆ 328968-36-1

Products

Número de referenciaEmbalaje Cant./Env.
382113-10MG Ampolla de plást. 10 mg
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
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 Ficha datos de seguridad (MSDS)

Título

Ficha técnica de seguridad del material (MSDS) 

Histone Acetyltransferase p300 Inhibitor, C646 - Calbiochem Certificados de análisis

CargoNúmero de lote
382113

Referencias bibliográficas

Visión general referencias
Bowers, EM., et al. 2010. Chem Biol 17, 471.

Licencias necesarias e Información técnica

Cargo
White Paper - The Message in the Marks: Deciphering Cancer Epigenetics
Ficha técnica

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.