Tazemetostat (EPZ-6438, E7438)是一种有效的，选择性EZH2抑制剂，无细胞试验中Ki 和 IC50分别为2.5 nM 和 11 nM，比作用于EZH1选择性高35倍，比作用于14种其他HMT选择性高4500多倍。 Information Tazemetostat (EPZ-6438) Tazemetostat (EPZ-6438, E7438) is a potent, and selective EZH2 inhibitor with K i and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs. Targets EZH2 (Cell-free assay) 2.5 nM(Ki) In vitro EPZ-6438 concentration-dependently reduces global H3K27Me3 levels in wild-type or SMARCB1 mutant cells, and induces strong antiproliferative effects with IC50 ranging from 32 nM to 1000 nM in SMARCB1-deleted MRT cell lines. EPZ-6438 induces gene expression of neuronal differentiation and cell cycle inhibition, while inhibtis expression of Hedgehog pathway genes, MYC and EZH2. The antiproliferative effect of EPZ-6438 is enhanced by either prednisolone or dexamethasone in several EZH2 mutant lymphoma cell lines. In vivo In SCID mice bearing s.c. G401 xenografts, EPZ-6438 induces tumor stasis during the administration period and produces a significant tumor growth delay with minimal effect on body weight. Cell Research(from reference) Cell lines：Mutant cell lines (G401, A204, G402, KYM-1), Wild type cell line (RD, 293, SJCRH30) Concentrations：~10 μM Incubation Time：7 days