Histone Acetyltransferase p300 Inhibitor, C646-Calbiochem

C₂₄H₁₉N₃O₆

445.42

MFCD01784780

NA.77

A reversible, cell-permeable pyrazolone p300/CBP HAT inhibitor (K_i = 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.

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C. Stock solutions are stable for up to 3 months at -20°C.

Bowers, EM., et al. 2010. Chem Biol17, 471.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥99% (sum of isomers, HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

brick red

DMSO: 50 mg/mL

ambient

−20℃

10 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 3