C646 ((E)-4-(4-((5-(4,5-Dimethyl-2-nitrophenyl)furan-2-yl)-methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid)

Reversible cell permeable p300/CBP histone acetyltransferase (HAT) inhibitor. Specific inhibition to p300 (86%) compared to N-acetyltransferase, PCAF, GCN5, Rtt109, Sas or MOZ histone acetyltransferases (<10%). Cell growth inhibitor in melanoma and non-small-cell-lung (NSCL) human cancer cell lines.\n\nStorage and Stability:\nShort-term Storage: +4 degrees C\nLong-term Storage: -20 degrees C\nStable for at least 2 years after receipt when stored at -20 degrees C. Store solutions at -20 degrees C in the dark.

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SPECIFICATIONS

Catalog Number

044620

Size

1mg

Purity

>98% (NMR)

References

Product Reference: \n?Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor: E.M. Bowers, et al.; Chem. Biol. 17, 471 (2010)\n?HAT Trick: p300, Small Molecule, Inhibitor: M. Ott & E. Verdin; Chem. Biol. 17, 417 (2010)\n?Butyrate greatly enhances derivation of human induced pluripotent stem cells by promoting epigenetics remodeling and the expression of pluripotency-associated genes: P. Mali, et al.; Stem Cells 28, 713 (2010)\n?Dynamic acetylation of all lysine-4 trimethylated histone H3 is evolutionarily conserved and mediated by p300/CBP: N.T. Crump, et al.; PNAS 108, 7814 (2011)\n?Paradoxical Enhancement of Fear Extinction Memory and Synaptic Plasticity by Inhibition of the Histone Acetyltransferase p300: R. Marek, et al.; J. Neurosci. 31, 7486 (2011)\n?Inhibition of the acetyltransferases p300 and CBP reveals a targetable function for p300 in the survival and invasion pathways of prostate cancer cell lines: F.R. Santer, et al.; Mol. Cancer Ther. (Epub ahead of print) (2011)\n?

Alternative Names

(E)-4-(4-((5-(4,5-Dimethyl-2-nitrophenyl)furan-2-yl)-methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid