Biological Activity:

NI-57 is a potent and selective inhibitor of the bromodomain of the BRPFs. It binds to BRPF1B with a KD of 31 nM (ITC), to BRPF2 with a KD of 108 nM (ITC) and to BRPF3 KD of 408 nM (ITC). NI-57 is very selective against other non-Class IV bromodomains, including the BETs, has minimum 32-fold selectivity against BRD9. It shows accelerated FRAP recovery at 1 µM in the BRPF2 FRAP assay preventing binding of full-length BRPF2 to chromatin.

How to Use:

In vitro: NI-57 was used at 10 µM final concentration in vitro and in cellular assays.
In vivo: n/a

Reference:

• 1. http://www.thesgc.org/chemical-probes/NI-57/teaser.