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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:

• In vitro:? OF-1 was used at 5-10 μM final concentration in various in vitro assays.
• In vivo: n/a?

Reference

1. ?http://www.thesgc.org/chemical-probes/OF-1?