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

Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
321695-57-2C₁₅H₁₅NO₅S

Products

Catalogue NumberPackaging Qty/Pack
5.05298.0001 Glass bottle 10 mg
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®
SynonymsGCN5 Inhibitor III, Histone Acetyltransferase Inhibitor IX, PCAF Inhibitor IV, 4-(4-Methoxyphenylsulfonyloxyimino)-2,6-dimethyl-2,5-cyclohexadien-1-one
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
Quality LevelMQ100
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
Global Trade Item Number
Catalogue Number GTIN
5.05298.0001 04055977243666

Documentation

p300/CBP Inhibitor VI, L002 - CAS 321695-57-2 - Calbiochem 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
SynonymsGCN5 Inhibitor III, Histone Acetyltransferase Inhibitor IX, PCAF Inhibitor IV, 4-(4-Methoxyphenylsulfonyloxyimino)-2,6-dimethyl-2,5-cyclohexadien-1-one
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 Protect from light
+2°C to +8°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
ReferencesYang, H., et al. 2013. Mol. Cancer Ther. 12, 610.