BAY-496

BAY-496 is a potent and selective small molecule inhibitor of the BRPF1 (Bromodomain and PHD Finger-containing protein 1) bromodomain. Developed by Bayer in collaboration with the University of Oxford and the University of Frankfurt, it was identified through virtual screening and chemical optimization. BAY-496 exhibits high affinity for the BRPF1 bromodomain with an IC50 of 20 nM and demonstrates selectivity over the closely related BRPF2 (IC50 160 nM) and the unrelated BRD4 bromodomain. In preclinical research, the compound has shown anti-proliferative activity in specific cancer cell lines, including ES-2 (ovarian cancer), DMS-53 (small cell lung cancer), and THP-1 (acute myeloid leukemia). It is primarily utilized as a chemical probe to investigate the epigenetic role of BRPF1 in gene regulation and its potential as a therapeutic target in oncology.