MW 390.5 Da. Potent (IC50 = 15 nM for wild-type enzyme; 13 nM for Y641F mutant enzyme) EZH2 inhibitor. Selective versus EZH1 (142-fold). Highly selective (>10,000-fold) against a panel of 10 other human methyltransferases. Inhibits cellular H3K27 methylation and activates Ezh2 target gene p16 expression in diffuse large B-cell lymphoma cells (DLBLC). Selectively inhibits growth and promotes cell cycle arrest and apoptosis of DLBLC cells with Y641 EZH2 mutations.
MW 390.5 Da. Potent (IC50 = 15 nM for wild-type enzyme; 13 nM for Y641F mutant enzyme) EZH2 inhibitor. Selective versus EZH1 (142-fold). Highly selective (>10,000-fold) against a panel of 10 other human methyltransferases. Inhibits cellular H3K27 methylation and activates Ezh2 target gene p16 expression in diffuse large B-cell lymphoma cells (DLBLC). Selectively inhibits growth and promotes cell cycle arrest and apoptosis of DLBLC cells with Y641 EZH2 mutations.
Soluble in DMSO to 50 mM.
Potent (IC50 = 15 nM for wild-type enzyme; 13 nM for Y641F mutant enzyme) EZH2 inhibitor. Selective versus EZH1 (142-fold). Highly selective (>10,000-fold) against a panel of 10 other human methyltransferases. Inhibits cellular H3K27 methylation and activates Ezh2 target gene p16 expression in diffuse large B-cell lymphoma cells (DLBLC). Selectively inhibits growth and promotes cell cycle arrest and apoptosis of DLBLC cells with Y641 EZH2 mutations.
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Chemical structure of EI1, EZH2 inhibitor, 1418308-27-6
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