FH535 is a β-catenin pathway inhibitor. FH535 represses pancreatic cancer xenograft growth and angiogenesis. FH535 increases the radiosensitivity and reverses epithelial-to-mesenchymal transition of radioresistant esophageal cancer cell line KYSE-150R. FH535 inhibited metastasis and growth of pancreatic cancer cells. FH535 selectively inhibits cell proliferation and potentiates imatinib-induced apoptosis in myeloid leukemia cell lines.