Abstract: OBJECTIVE To review CDK inhibitors and their use in cancer research or therapy, and help researchers to search for small-molecule CDK inhibitors which best suited for the specific purpose of their research. METHODS Seventeen CDK inhibitors recently developed were reviewed. The targets, commercial availability and IC₅₀ values of each inhibitor were also provided. RESULTS The potent anticancer effects of CDK inhibitors had been revealed in cancer research and clinical therapy. CONCLUSION With the further research, CDK inhibitors will be new anticancer drugs.