Chemical Name: 4-[4-[[5-(4,5-Dimethyl-2-nitrophenyl)-2-furanyl]methylene]-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl]benzoic acid
Biological ActivitySelective p300/CREB-binding protein (CBP) inhibitor (Ki = 400 nM). Selective for p300 over six other histone acetyltransferases (HATs). Suppresses histone H3 and H4 acetylation in mouse fibroblast cell lines. Also represses pluripotency markers in mouse embryonic stem cells.
This compound is a mixture of Z:E isomers (~ 80:20).
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
- This compound is a mixture of Z:E isomers (~ 80:20)
Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor.
Bowers et al.
Butyrate greatly enhances derivation of human induced pluripotent stem cells by promoting epigenetic remodeling and the expression of pluripotency-associated genes.
Mali et al.
Stem Cells, 2010;28:713
HAT trick: p300, small molecule, inhibitor.
Ott and Verdi
Dynamic acetylation of all lysine-4 trimethylated histone H3 is evolutionarily conserved and mediated by p300/CBP.
Crump et al.
Proc.Natl.Acad.Sci. USA, 2011;108:7814
Roles for histone acetylation in regulation of telomere elongation and two-cell state in mouse ES cells.
Dan et al.
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It is dissolved well in DMSO. I diluted it with serum free medium (final concentration of 10 micromolar) and treated the cells for different time points to detect its inhibitory effect of p300 at protein level.