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Description: PFI-4 is a novel, potent, cell permeable and selective inhibitor of bromodomain and PHD finger-containing protein 1 (BRPF1) with antineoplastic activity. It inhibits BRPF1 with an IC50 of 80 nM. PFI-4 aacts by specifically binding 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 of 250nM, while showing no effect on BRPF1A. BRPF1A may act as dominant negative isoform of BRPF1 generated by alternative splicing. 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.
References: ACS Med Chem Lett. 2014 Sep 10; 5(11):1190-5.
Chemical Name: N-[2, 3-Dihydro-1, 3-dimethyl-2-oxo-6-(1-pyrrolidinyl)-1H-benzimidazol-5-yl]-2-methoxybenzamide
InChi Key: QCIJLRJBZDBVDB-UHFFFAOYSA-N
InChi Code: InChI=1S/C21H24N4O3/c1-23-17-12-15(22-20(26)14-8-4-5-9-19(14)28-3)16(25-10-6-7-11-25)13-18(17)24(2)21(23)27/h4-5, 8-9, 12-13H, 6-7, 10-11H2, 1-3H3, (H, 22, 26)
SMILES Code: O=C(NC1=C(N2CCCC2)C=C(N3C)C(N(C)C3=O)=C1)C4=CC=CC=C4OC
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