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5-c]quinolin-2(3H)-one
111(3):508-17
InChiKey: ARHBIBDGWDRBJH-UHFFFAOYSA-N
Discovery of a First-in-Class
Chemical Name: N-((4
CPI-169 racemate - EZH2 Methyltransferase Inhibitor. CAS# 1450655-76-1 60159 5-c]quinolin-2(3H)-oneCPI 169, CAS No. 1450655 76 1, is a highly potent and selective small molecule inhibitor of histone methyltransferase EZH2. CPI 169 potently inhibits wild type EZH2, mutant EZH2 Y641N and EZH1 with IC50 of 0. 24 nM, 0. 51 nM and 6. 1 nM, respectively. It decreases cellular levels of H3K27me3 with an EC50 of 70 nM, and triggers cell cycle arrest and apoptosis across a large cell panel representing various non Hodgkins lymphoma (NHL) subtypes. a variety
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