MG132 (Z-Leu-Leu-Leu-CHO) is an inhibitor of proteasome, and it can enter the cell to reversibly inhibit the activation of proteasome, thereby influencing the course of cell cycle and inducing the apoptosis of cells. Currently, it has been reported that MG132 can induce apoptosis of all kinds of tumorous cells and can be used a anti-tumor drug. This article reviews the mechanisms of the apoptosis of the tumorous cells induced by MG132.