C646 is a selective, competitive histone acetyltransferase (HAT) p300 inhibitor with Ki of 400 nM, less potent for other acetyltransferases.
C646 blocks dynamic acetylation of H3K4me3 globally in mouse and fly cells, and locally across the promoter and start-site of inducible genes in the mouse, thereby disrupting RNA polymerase II association and the activation of genes.
C646 increses caspase-dependent apoptosis involving both extrinsic and intrinsic cell death pathways in androgen-dependent and castration-resistant prostate cancer cells.
C646 inhibits the growth of human melanoma and other tumor cells and promotes cellular senescence.
