Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: 2-(3-pyridinylmethylene)-1H-indene-1,3(2H)-dione
Purity: ≥98%
Formula Markup: C15H9NO2
Formula Weight: 235.2
CAS Number: 31083-55-3
Notes: BMI1/RING1A and BMI1/RNF2 are E3 ubiquitin ligase complexes that mediate the monoubiquitination of histone 2A (H2A). This is an essential function of polycomb repressive complex 1 (PRC1).{30718} PRT4165 is an inhibitor of the ubiquitin ligase activity of PRC1.{30882,30883} It blocks BMI1/RING1A self-ubiquitination (IC50 = 3.9 µM), as well as polyubiquitination of topoisomerase 2α in cells.{30882} PRT4165 inhibits ubiquitination of H2A by either RNF2 or RING1. Through these actions, PRT4165 prevents the accumulation of detectable ubiquitin at DNA double-strand breaks, the retention of response proteins around breaks, and the repair of breaks.{30883}
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