Currently, researchers have synthesized two classical selective small molecule tankyrase-1 inhibitors, IWR 1 and XAV 939. IWR 1 inhibits the 50% inhibitory concentration (IC50) of tankyrase-1 to 131 nM. XAV 939 is an inhibitor of PARP and potently inhibits tankyrase-1 activity by an IC50 of 11 nM. Studies have shown that XAV 939 intervention can reduce the activity of β-catenin and the extent of epithelial-mesenchymal transition, and improve the survival rate of mice treated with bleomycin. Therefore, tankyrase-1 will become a potential research drug for tumor-targeted therapy.