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382113 Histone Acetyltransferase p300 Inhibitor, C646 - Calbiochem

Histone 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.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 4-(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

382113
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
328968-36-1C₂₄H₁₉N₃O₆

Products

Catalogue NumberPackaging Qty/Pack
382113-10MG Plastic ampoule 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
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
Global Trade Item Number
Catalogue Number GTIN
382113-10MG 04055977213119

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
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 Protect from light
-20°C
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.