PRT4165
E3 ubiquitin ligase inhibitor / 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. Blocks Bmi1/Ring1A-mediated ubiquitination and drug-induced degradation of topoisomerase 2α.1 Inhibits H2A/H2AX ubiquitination via blocking the E3 ubiquitin ligase activity of RNF2 and a Bmi1/RNF2 complex. Blocks polycomb repressor complex (PRC) 1-mediated histone H2A ubiquitination in vitro and in vivo and as such represents a new tool for studying chromatin remodeling.2
Biochemicals & reagents
31083-55-3
1) Alchanati et al. (2009), The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of Top2alpha cleavage complex – a potentially new drug target; PLoS One, 4 e8104 2) Ismail et al. (2013), A small molecule inhibitor of polycomb repressive complex 1 inhibits ubiquitin signaling at DNA double-strand breaks; J. Biol. Chem., 288 26944
RT
TARGET: Ubiquitin ligase -- PATHWAY: Degradation; Posttranslational modification -- RESEARCH AREA: Ubiquitin/Proteasome