EPZ011989 is a cell permeable, metabolically stable and orally available EZH2 inhibitor, a compound with oral exposure and metabolic stability that is able to elicit robust methyl mark inhibition and antitumor activity. It binds potently and selectively to the mutant and wild-type EZH2 with Ki values < 3 nM, and highly selective over closely-related EZH1 (>15-fold selectivity) and 20 other histone methyltransferases (HMTs) (>3000-fold selectivity) tested. Demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma. Reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with IC50s below 100 nM.

KEYWORDS: EPZ011989 hydrochloride | Supplier | EZH2 inhibitor | EPZ-011989 | EPZ 011989 | CT-EPZ989 | CAS [2095432-26-9] | [1598383-40-4] | Histone | HMTase | Inhibitor | Enzymes