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Background
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Synonyms:
4-[4-[[5-(4,5-Dimethyl-2-nitrophenyl)-2-furanyl]methylene]-4,5-dihydro-3-methyl- 5-oxo-1H-pyrazol-1-yl]benzoic acid
A reversible, cell-permeable pyrazolone p300/CBP HAT inhibitor (Ki = 400 nM), which competes with acetyl-CoA for the p300 Lys-CoA binding pocket. Demonstrates 86 % inhibition against p300 at 10 nM. Less than 10 % inhibition against serotonin N-acetyltransferase, PCAF, GCN5, Rtt109, Sas, and MOZ HATs in a chemical screening assay. Treatment of C3H 10T1/2 mouse fibroblasts at 25 µM results in an inhibitory effect against basal and TSA- inducible acetylation of histones H3 and H4. Shown to inhibit human cell growth in melanoma and non-small- cell-lung cancer cell lines at 10 µM with similar or higher potency than peptide-based bisubstrate p300/CBP HAT inhibitor Lys-CoA-Tat at 25 µM.
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