Inhibitor of Bmi1/Ring1A, subunits of the polycomb repressive complex 1 (PRC1); inhibits self-ubiquitination (IC50 = 3.9µM) 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 and in vivo.
Chemical Name: 2-(3-Pyridinylmethylene)-1H-Indene-1,3(2H)-dione
CAS Number: 31083-55-3
Solubility: Soluble to 100mM in DMSO and to 5mM in 1eq. HCl with gentle warming
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