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YW2065 is an inhibitor of Wnt/β-catenin signaling and an activator of AMP-activated protein kinase (AMPK).1 It induces degradation of β-catenin and increases the levels of Axin1 and phosphorylated AMPK and acetyl-CoA carboxylase (ACC), which is a downstream substrate of AMPK, in SW620 colorectal cancer cells when used at a concentration of 3 µM. YW2065 inhibits recombinant human Wnt3a-induced reporter activation in HEK293 cells (IC50 = 2.3 nM) and the growth of SW480 colorectal cancer cells (GI50 = 2.4 nM). In vivo, YW2065 (50 mg/kg) decreases tumor volume and weight in an SW620 mouse xenograft model.
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1. Pyrazole-