Catalog No.: PC-21938Not For Human Use, Lab Use Only.
Tazemetostat (EPZ-6438) is a potent, selective, SMA-competitive and orally available EZH2 inhibitor with IC50 of 11 and 16 nM in peptide assay and nucleosome assay, respectively.
Tazemetostat (EPZ-6438) is a potent, selective, SMA-competitive and orally available EZH2 inhibitor with IC50 of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat (EPZ-6438) inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with Ki of 2.5 nM, inhibits rat EZH2 with IC50 of 4 nM. Tazemetostat (EPZ-6438) selectively inhibits intracellular lysine 27 of histone H3 (H3K27) methylation in a concentration- and time-dependent manner in both EZH2 wild-type and mutant lymphoma cells. Tazemetostat (EPZ-6438) treatment causes dose-dependent tumor growth inhibition in EZH2-mutant NHL xenograft-bearing mice.
