tcsc1654 EI1

EI1 (KB-145943) is a potent and selective EZH2 inhibitor with IC₅₀ of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.

IC50 & Target: IC50: 15 nM (EZH2 wild type), 13 nM (EZH2 Y641F mutant type)

In Vitro: In DLBCL cells, EI1 (KB-145943) inhibits cellular H3K27 methylation and activates Ezh2 target gene p16 expression. In mouse embryonic fibroblasts, EI1 (KB-145943) also inhibit H3K27me3 and cell proliferation. In addition, EI1 (KB-145943) selectively inhibits the growth of DLBCL cells carrying Ezh2 mutation, and causes cell cycle arrest and apoptosis^[1].