PRT 4165

• Supplier: Tocris Bioscience
• Catalog: 2477
• Prices: $75.00, $315.00
• Sizes: 10 mg, 50 mg
• Function Type: Inhibitor
• Cas Number: 31083-55-3
• Chemical Name: 2-(3-Pyridinylmethylene)-1H-Indene-1,3(2H)-dione
• Formula: C15H9NO2
• Molecular Weight: 235.24
• Purity: >99 %
• Description: Inhibitor of Bmi1/Ring1A, subunits of the polycomb repressive complex 1 (PRC1); inhibits self-ubiquitination (IC 50 = 3.9 μ M) but does not increase cellular levels of either subunit. Prevents Bmi1/Ring1A-mediated ubiquitination and drug-induced degradation of topoisomerase 2 α (Top2 α ). 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 .

Product References

The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of - The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of

Alchanati I, Teicher C, Cohen G, Shemesh V, Barr HM, Nakache P, Ben-Avraham D, Idelevich A, Angel I, Livnah N, Tuvia S, Reiss Y, Taglicht D, Erez O. PLoS One. 2009 Dec 1;4(12):e8104.

A small molecule inhibitor of polycomb repressive complex 1 inhibits ubiquitin - A small molecule inhibitor of polycomb repressive complex 1 inhibits ubiquitin

Ismail IH, McDonald D, Strickfaden H, Xu Z, Hendzel MJ. J Biol Chem. 2013 Sep 13;288(37):26944-54.