Chemical Name: 2-(3-Pyridinylmethylene)-1H-Indene-1,3(2H)-dione
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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A small molecule inhibitor of polycomb repressive complex 1 inhibits ubiquitin signaling at DNA double-strand breaks.
Ismail et al.
The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of Top2α cleavage complex - a potentially new drug target.
Alchanati et al.
PLoS One, 2009;4:e8104
Citations for PRT 4165
The citations listed below are publications that use Tocris products. Selected citations for PRT 4165 include:
2 Citations: Showing 1 - 2
SCL/TAL1 cooperates with Polycomb RYBP-PRC1 to suppress alternative lineages in blood-fated cells.
Authors: Chagraoui Et al.
Nat Commun 2018;9:5375
BMI1 regulates androgen receptor in prostate cancer independently of the polycomb repressive complex 1.
Authors: Zhu Et al.
Nat Commun 2018;9:500
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