Potent Bromodomain inhibitor with selectivity for BRPF1 and BRPF2 (Kd values 100 nM, 500 nM, and 2.4 μM for BRPF1B, BRPF2, and BRPF3, respectively). Selectivity against other bromodomains is very good, in general >100-fold. The closest off-target effects are against BRD4 (39-fold selectivity) and TIF1a (50% inhibition at 20 µM. OF-1 increases thermal stability in the cellular thermal shift assay (CETSA) of full length BRPF1B at 1 µM and also demonstrates accelerated FRAP recovery at 5 µM in the BRPF2 FRAP assay.

KEYWORDS: OF1 | supplier | BRPF inhibitor | OF-1 supplier | CAS [919973-83-4] | Histone | BRPF (BRD) | Inhibitor | SGC | Bromodomain | Chromatin | BRPF1 | BRPF1B | BRPF2 | BRD4 | TIF1a | FRAP | epigenetic | DNA