EZH2/HSP90-IN-29 is a dual inhibitor for EZH2 and HSP90 , with IC 50 s of 6.29 nM and 60.1 nM, for EZH2 and HSP90 , respectively. EZH2/HSP90-IN-29 increases apoptosis /necrosis-related gene expression, induces cell cycle arrest at M phase and inhibits reactive oxygen species (ROS) catabolism pathway. EZH2/HSP90-IN-29 is able to cross the blood-brain-barrier (BBB).