Prt 4165, Inhibitor Of Bmi1/Ring1a; Blocks Histone H2a Ubiquitination, Each

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Prt 4165 is an inhibitor of bmi1/ring1a, subunits of the polycomb repressive complex 1 (prc1); inhibits self-ubiquitination (ic50 = 3.9 μM) but does not increase cellular levels of either subunit. Prevents bmi1/ring1a-mediated ubiquitination and drug-induced degradation of topoisomerase 2α (top2α). Also shown to inhibit the in vitro e3 ubiquitin ligase activity of rnf2 and a bmi1/rnf2 complex, inhibiting h2a/h2ax ubiquitination. Blocks polycomb repressor complex (prc) 1-mediated histone h2a ubiquitination in vitro.