Family VIII bromodomain inhibitor / PFI-3 (1819363-80-8) is a selective inhibitor of family VIII bromodomains PB1(5), SMARCA2, and SMARCA4.1 It showed complete selectivity over all non-family VIII bromodomains. PFI-3 blocked adipogenesis in C3H10T1/2 mesenchymal cells at 20µM.Treatment of embryonic stem cells with PFI-3 led to deprivation of stemness and deregulated lineage specificity. Differentiation of trophoblast stem cells in the presence of PFI-3 was enhanced.2 Cell permeable.
Biochemicals & reagents
1819363-80-8
1) Gerstenberger et al. (2016), Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit; J.Med.Chem. 59 4800 2) Fedorov et al. (2015), Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance; Sci.Adv. 1 e1500723
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TARGET: Bromodomain -- PATHWAY: Chromatin; Posttranslational modification; Beta-catenin; Wnt -- RESEARCH AREA: Epigenetics; Stem Cells -- DISEASE AREA: Cancer