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IWP-O1 is an inhibitor of porcupine (PORCN), an enzyme that catalyzes palmitoylation of Wnt proteins.1 It inhibits Wnt signaling in L-Wnt-STF cells (IC50 = 80 pM in a reporter assay) and phosphorylation of Dishevelled-2 (Dvl2) and Dvl3 in HeLa cells when used at a concentration of 1 µM. IWP-O1 (1 µM) enhances the cytotoxicity of the glycolysis inhibitors 2-deoxyglucose (2-DG) and lonidamine (Item No. 14640) in CAL 27 oral squamous cell carcinoma (OSCC) cells.2
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1. Development of a triazole class of highly potent Porcn inhibitors. Bioorg. Med. Chem. Lett. 26(24), 5891-5895 (2016).
2. The Wnt signaling pathway inhibitors improve the therapeutic activity of glycolysis modulators against tongue cancer cells. Int. J. Mol. Sci. 23(3), 1248 (2022).