Wnt-C59 was first disclosed in patent WO2010101849 as a potent Wnt signaling modulator. It has IC₅₀ less than 0.11 nM in Wnt-Luc reporter assay for Wnt pathway inhibition. In the study, Wnt-C59 prevents palmitylation of Wnt proteins by Porcupine (Porcn, a membrane-bound O-acyltransferase), thereby blocking Wnt secretion and activity, similar to Wnt inhibitors IWP-2, IWP-3 and IWP-4. But Wnt-C59 is more potent and selective, and has better chemical/physical properties, suitable for in vitro/in vivo studies.

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