PFI 4

Short Summary : Potent and selective BRPF1 Bromodomain inhibitor

Category : Chromatin/Epigenetics|Bromodomain

Purity : 0.9944

CAS Number : 900305-37-5

Formula : C21H24N4O3

Molecular Weight :

Molecular Weight : 380.44

SMILE : [H]N(C(C1=CC=CC=C1OC)=O)C2=C(N3CCCC3)C=C(N(C)C(N4C)=O)C4=C2

Solubility : >13.3mg/mL in DMSO

Storage : Store at -20°C

Description : PFI 4 is a cell permeable, potent and selective inhibitor of BRPF1 Bromodomain with pIC50 and pKd values of 7.1 and 8.0 [1]. The BRPF (bromodomain and PHD finger-containing) family BRPF1, BRPF2/BRD1, and BRPF3 operate as scaffolds to assemble MYST-family histone acetyltransferases (HATs) complexes. BRPF1 is a component of complexes containing the MOZ/MORF transcriptional coactivators and links the catalytic HATs to the other subunits ING5 and hEAF6.8. BRPF1 is important for maintaining skeletal development and Hox gene expression in fish [1]. In the BROMOscan panel of 35 bromodomain binding assays, PFI 4 exhibited excellent BRPF1 potency with pKd value of 8.0 and excellent selectivity over other bromodomains. In a cellular protein interaction assay, PFI 4 displaced NanoLuc-tagged BRPF1 bromodomain from Halotaggedhistone H3.3 and disrupted chromatin binding [1]. Reference:[1]. Demont EH, Bamborough P, Chung CW, et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. ACS Med Chem Lett, 2014, 5(11): 1190-1195.

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