5545978

Tocris Bioscience™ PRT 4165

Inhibitor of Bmi1/Ring1A; blocks histone H2A ubiquitination

Manufacturer: Fischer Scientific

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Purity

>99%

Product Type

PRT 4165

Molecular Weight (g/mol)

235.24

Inhibitors

PRT 4165

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Description

  • 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 .