ms 177

MS177, a potent and rapid EZH2 degrader, functions as a PROTAC comprised of a CRBN ligand, linker, and a powerful enzymatic EZH2 inhibitor C24 (C24 IC50: 12 nM). It successfully targets and depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. Furthermore, MS177 inhibits leukemia cell growth, induces apoptosis, and arrests cell cycle progression.