Cat. No. 5047
Chemical Name: 2-(3-Pyridinylmethylene)-1H-Indene-
Biological ActivityInhibitor 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 and in vivo.
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Certificate of Analysis / Product Datasheet / Safety Data Sheet
Ismail et al (2013) A small molecule inhibitor of polycomb repressive complex 1 inhibits ubiquitin signaling at DNA double-strand breaks. J.Biol.Chem. 288 26944. PMID: 23902761.
Alchanati et al (2009) The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of Top2α cleavage complex - a potentially new drug target. PLoS One 4 e8104. PMID: 19956605.
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Keywords: PRT 4165, supplier, PRT4165, E3, ubiquitin, ligase, inhibitors, inhibits, Bmi1, Ring1A, ubiquitination, ubiquitylation, topoisomerase, 2a, Top2a, Top2alpha, Top2α, polycomb, repressive, complex, 1, PRC1, RNF2, Bmi1/RNF2, Tocris Bioscience, Ubiquitin E3 Ligase Inhibitor products
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