OF-1 is a chemical probe for the bromodomains of the Bromodomain and PHD Finger-containing (BRPF) family of proteins. It binds BRPF1B, BRPF2, and BRPF3 with Kd values of 0.1, 0.5, and 2.4 μM, respectively, as determined by isothermal titration calorimetry. OF-1 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 shows modest general cytotoxicity. See the Structural Genomics Consortium (SGC) website for further information.
