Biological Activity:
OF-1 is the potent and selective BRPF (BRomodomain and PHD Finger containing) inhibitor. It binds to BRPF1B with a KD of 100 nM (ITC), to BRPF2 with a KD of 500 nM (ITC) and to BRPF3 with a KD of 2.4 mM (ITC). It has general >100-fold selectivity against other bromodomains (39-fold selectivity over BRD4). 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. It shows modest general cytotoxicity.
How to Use:
Reference
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