BCL2 is a member of B cell lymphoma 2 (BCL2) family, which are key regulators in intrinsic apoptosis. BCL2 consists of a hydrophobic pocket to which BH3 helixes bind and the binding blocks the apoptosis signal and prevents the cells from death. Increased expression or overexpression under the treatment has been reported in many cancers. Inhibition of BCL2 activity is a promising approach for cancer therapy.