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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![l-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-lHpyrazolo [3,4-d]pyrimidin-l-yl]-l-piperidinyl]-2-propyn-l-one](https://e1752fbe.rocketcdn.me/wp-content/uploads/AP14272-CAS-936563-91-6-1-e1686054563587.png)
