Aiming at epigenetic modification of EZH2, the earliest EZH2 inhibitor was 3-Deazaneplanocin A. It was reported that 3-Deazaneplanocin A selectively inhibited the H3K27me3 and lysine 20 on histone H4, and reactivated silenced genes in cancer cells.109. This evidence concerns the gene EZH2 and cancer.