OF-1

OF-1 is a selective BRPF1B and BRPF2 bromodomain inhibitor (Kd values are 100 and 500 nM respectively). OF-1 displays 39-fold selectivity for BRPF1B and BRPF2 over BRD4. It increases thermal stability of full length BRPF1B at 1 µM, in the cellular thermal shift assay. It also demonstrates accelerated fluorescence recovery after photobleaching (FRAP) at 5 µM in the BRPF2 FRAP assay. OF-1 displays modest general cytotoxicity.