Wnt/β-catenin activator 1 (Compound 5m) is an orally active activator of the Wnt/β-catenin signaling pathway. It induces cell cycle arrest in the G1 phase, inhibits early proliferation of adipocytes, and suppresses adipogenesis in 3T3-L1 cells with an IC50 of 330 nM. In a high-fat diet-fed Syrian golden hamster model, Wnt/β-catenin activator 1 exhibits anti-adipogenic and anti-dyslipidemic activities.