A-485

A-485 is a potent and selective p300/CREB-binding protein (CBP) HAT domain inhibitor (IC₅₀ values are 2.6 and 9.8 nM for the CBP-bromodomain HAT-C/H3 (BHC) and p300-BHC domains, respectively). A-485 displays > 1000-fold selectivity over closely related HATs. It decreases acetylated histone H3 lysine 27 (H3K27Ac), but not H3K9Ac, levels in PC3 cells in a concentration-dependent manner. A-485 reduces proliferation of non-small cell lung cancer (NSCLC), small cell lung cancer, triple-negative breast cancer, mantel cell lymphoma, multiple myeloma, non-Hodgkin's, and acute myeloid leukemia cell lines.