EZH2 inhibitors are categorized as disrupting the structural integrity of the Polycomb Repressive Complex 2 (PRC2) and targeting EZH2 methyltransferase activity, such as tazemetostat and valemetostat, function by directly reducing levels of trimethylated histone H3K27me3 through the inhibition methyltransferase activity of EZH2.777,778 Moreover, GSK126 the other kind of EZH2 inhibitor, which disrupts protein-protein interactions among PRC2 subunits, has achieved phase I clinical trials for the treatment of various cancers (NCT02082977). Here, EZH2 is linked to cancer.