PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 = 80 nM. PFI-4 specifically binds to BRPF1B with a Kd =13 nM as determined by ITC. It reduces recovery time in triple BRD cell construct in FRAP and is potent in cells with IC50 250nM, while showing no effect on BRPF1A. BRPF1 exists in 2 different isoforms: BRPF1A and BRPF1B. A residue insertion in the ZA loop of BRPF1A prevents binding to acetylated histone peptides. BRPF1A may act as dominant negative isoform of BRPF1 generated by alternative splicing.
Epigenetic Reader Domain Inhibitors Related Products:
ICG-001; (+)-JQ1; I-BET151; PFI-1; Molibresib; Apabetalone; C646; Curcumin; Bromosporine; Birabresib; UNC1215; GSK6853; CPI-637; BI-9564; XMD8-92; MS436; CPI-203; KG-501; Mivebresib; GSK2801