Inhibition or resistance of cell death often leads to the occurrence of tumors.46,47 Therefore, the regulation of the apoptosis signaling pathway is one of the crucial methods to improve cancer treatment.48 Then, we focus on summarizing some representative small-molecule compounds that ultimately induce cancer cell death through the regulation of some crucial apoptotic signaling pathways and targets, such as TNF-related ligands and their receptors, Bcl-2 family, Apaf-1 and Cyt-C, NF-κB pathway, p53, etc. (Fig. 2). The gene discussed is APAF1; the disease is cancer.