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

505298
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Overview

Key Spec Table

CAS #Empirical Formula
321695-57-2C₁₅H₁₅NO₅S

Products

Catalogue NumberPackaging Qty/Pack
5052980001 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
Biological Information
Primary Targetp300 HAT
Purity≥99% by HPLC
Physicochemical Information
Cell permeableY
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
Global Trade Item Number
Catalogue Number GTIN
5052980001 04055977243666