The Hippo signaling is a highly conserved pathway that plays important roles in tumorigenesis, stem cell self-renewal and differentiation, organ size control, and many other biological processes. Functions of the Hippo signaling pathway are regulated by complicated intracellular and extracellular signaling networks. When activated, the Hippo pathway functions as a tumor suppressor. However, dysregulation of this pathway contributes to increased cell proliferation and decreased apoptosis and differentiation. Therefore, regulation of Hippo signaling by pharmacological modulators may be a promising anticancer strategy. Here, we summarize potential anti-cancer drugs that target components of the Hippo pathway or regulate interactions between the Hippo signaling pathway and other signaling pathways.