PRT 4165

Product Description

PRT 4165 is an inhibitor of Bmi1/Ring1A, subunits of the polycomb repressive complex 1 (PRC1); PRT 4165 inhibits self-ubiquitination (IC₅₀ = 3.9 μM) but does not increase cellular levels of either subunit. PRT 4165 prevents Bmi1/Ring1A-mediated ubiquitination and drug-induced degradation of topoisomerase 2α (Top2α). PRT 4165 inhibits the in vitro E3 ubiquitin ligase activity of RNF2 and a Bmi1/RNF2 complex, inhibiting H2A/H2AX ubiquitination. PRT 4165 blocks polycomb repressor complex (PRC) 1-mediated histone H2A ubiquitination in vitro.

Solubility

Preparing Stock Solutions for PRT 4165

The following data is based on the product molecular weight 235.24

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	4.25 mL	21.25 mL	42.51 mL
5 mM	0.85 mL	4.25 mL	8.50 mL
10 mM	0.43 mL	2.13 mL	4.25 mL
50 mM	0.09 mL	0.43 mL	0.85 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Ismail A small molecule inhibitor of polycomb repressive complex 1 inhibits ubiquitin signaling at DNA double-strand breaks. J.Biol.Chem. 2013 PMID: 23902761
• Alchanati The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of Top2α cleavage complex - a potentially new drug target. PLoS One 2009 PMID: 19956605