Sirtuins family is a class of NDA+ dependent protein deacetylases that play a key role in the regulation of several aspects of biological processes, such as cell cycle regulation, autophagy, immune and inflammatory response. Many studies have shown that sirtuins2 as a key player in the cancer pathway is of great significance in tumorigenesis. This review summarizes the newly discovered, in recent years, some SIRT2 inhibitors for cancer target structure, action mechanism, biological activity, substrate specificity, and signaling pathways.