PTK7/β-catenin-IN-6 (Compound 03653) is an inhibitor for PTK7/β-catenin interaction, which inhibits the Wnt signaling pathway, and exhibits an anticancer activity against colorectal cancer (CRC).
PTK7/β-catenin-IN-6 (25 μM) misregulates the β-catenin responsive transcription and inihibits the Wnt signaling pathway through regulating the mRNA expressions of Wnt signaling related genes, which are associated with cell proliferation and migration[1].PTK7/β-catenin-IN-6 (0-100 μM) arrests the cell cycle in G0/G1 phase through block of CyclinA2, CyclinE2 and CDK production, inhibits proliferations of HCT116, SW480 and MEF with IC50s of 20.1, 19.6 and 46.3 μM, respectively[1].
References:
[1]. Ganier L, et al., Discovery of Small-Molecule Inhibitors of the PTK7/β-Catenin Interaction Targeting the Wnt Signaling Pathway in Colorectal Cancer. ACS Chem Biol. 2022 May 20;17(5):1061-1072.