An inhibitor of the ubiquitin ligase activity of PRC1; blocks BMI1/RING1A self-ubiquitination (IC50 = 3.9 µM)

PRT4165 – 25 mg

Brand:
Cayman
CAS:
31083-55-3
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

An inhibitor of the ubiquitin ligase activity of PRC1; blocks BMI1/RING1A self-ubiquitination (IC50 = 3.9 µM), as well as polyubiquitination of topoisomerase 2α in cells; inhibits ubiquitination of H2A by either RNF2 or RING1

Formal name: 2-(3-pyridinylmethylene)-1H-indene-1,3(2H)-dione

Synonyms:  NSC 600157

Molecular weight: 235.2

CAS: 31083-55-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Ubiquitin Ligase System||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System||Research Area|Epigenetics, Transcription, & Translation|Writers|Ubiquitination

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