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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
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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