Chemical probes for the BRPF bromodomain and BRPF3 are scaffold proteins. PFI 4 specifically binds to BRPF1B with IC50 = 172 nM and Kd = 13 nM, determined by ITC. PFI 4 shortens the recovery time of triple BRD cell constructs in FRAP and is potent in cells with IC50 250nM, with no effect on BRPF1A. PFI 4 is more than 100-fold selective for BRPF1 over a panel of other bromodomains including BRPF2 (BRD1), BRPF3 and BRD4.
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