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PDE5-IN-3 (compound 11j) is a potent inhibitor of PDE5 (IC50: 1.57 nM). PDE5-IN-3 has a moderate inhibitory effect on EGFR (IC50: 5.827 μM). PDE5-IN-3 markedly inhibits the Wnt/β-catenin pathway with an IC50 value of 1286.96 ng/mL. PDE5-IN-3 induced the intrinsic apoptotic mitochondrial pathway in HepG2 cells, and PDE5-IN-3 exhibited significant antitumor effects.