EPZ011989 is a potent and orally active Zeste Homolog 2 ( EZH2 ) inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a K i value of <3 nM. EPZ011989 shows robust methyl mark inhibition and anti-tumor activity. EPZ011989 can be used for the research of various cancers. EPZ011989 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.