OF-1

OF-1 is a new SGC chemical probe for the bromodomains of the BRPF (BRomodomain and PHD Finger containing) family of scaffolding proteins (BRPF1/2/3).

OF-1 is a chemical probe for the bromodomains of the BRPF (BRomodomain and PHD Finger containing) family of scaffolding proteins (BRPF1, BRPF2, BRPF3) that assemble histone acetyltransferase (HAT) complexes of the MYST family members MOZ and MORF. The BRPF1 protein is the scaffold subunit of the MYST acetyltransferase complex, which plays a crucial roles in DNA repair, recombination and replication as well as transcription activation. OF-1 binds to BRPF1B with a K_d of 100 nM , to BRPF2 with a K_d of 500 nM and to BRPF3 with a K_d of 2.4 mM, and shows >100-fold selectivity against most other bromodomains. The closest off-target effects are against BRD4 (39-fold selectivity) and 50% inhibition of TIF1a at 20 μM. For full characterization details, please see OF-1 on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

OF-1 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.

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