The invention provides a small molecular activator taking human M2 type pyruvate kinase (M2 type pyruvate kinase, PKM2) as a target spot and application of the small molecular activator, and belongs to the technical field of pharmacy. According to the small molecular activator, the PKM2 is taken as the target spot, and the small molecule activator is screened by combining virtual screening based on butt joint and in-vitro biological activity evaluation. In-vitro activity test results show that two screened compounds have good PKM2 activation activity and good cancer cell inhibition activity, and discovered small molecules can provide a basis for research and development of new drugs for treating PKM2 related diseases, such as cervical cancer, breast cancer, ovarian cancer, prostate cancer,liver cancer, lung cancer, pancreatic cancer, colorectal cancer, leukemia, melanoma and multiple myeloma. A lead compound of the small molecular activator can be further optimized in structure, and arelatively good application prospect is achieved.