PTK7/β-catenin-IN-6 (Compound 03653) acts as an inhibitor of the PTK7/β-catenin interaction, thereby disrupting the Wnt signaling pathway. It has demonstrated anticancer effects specifically targeting colorectal cancer (CRC) [1].

PTK7/β-catenin-IN-6 (25 μM) modulates the expression of genes associated with Wnt signaling pathways linked to cell proliferation and migration, inhibits β-catenin's transcriptional activity, and suppresses the Wnt signaling cascade [1]. At concentrations ranging from 0-100 μM, PTK7/β-catenin-IN-6 induces a G0/G1 cell cycle arrest by inhibiting the production of CyclinA2, CyclinE2, and CDK, consequently reducing the proliferation of HCT116, SW480, and MEF cells, with IC50 values of 20.1, 19.6, and 46.3 μM, respectively [1]. In a cell proliferation assay, incubation of HCT116, SW480, and MEF cells with 0-100 μM of PTK7/β-catenin-IN-6 for 24 hours resulted in decreased cellular proliferation [1]. Western blot analysis of HCT116 and SW480 cells exposed to 0-100 μM of the compound for 24 hours showed reduced levels of CyclinA2, CyclinE2, and CDK [1]. RT-PCR conducted on HCT116 and SW480 cells with 25 μM concentration for 24 hours revealed increased mRNA levels of PLAUR, FOSL1, and NRP1, while AXIN2 mRNA levels decreased [1].