SKL2001

SKL2001 is a specific small molecule activator (agonist) of the Wnt/β-catenin pathway, stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction; strongly activates β-catenin responsive transcription, upregulates TOPflash reporter activity without effect on the activity of FOPFlash with mutated β-catenin/Tcf-binding elements, as well as either NF-κB or p53 reporter activity; upregulates the expression of Axin2, inhibits N-terminal β-catenin phosphorylation without affecting GSK-3β activity; suppresses preadipocyte differentiation, the alternative mesenchymal differentiation pathway. (In Vitro) :SKL2001 is an agonist of the Wnt/β-catenin pathway, and also upregulates the expression of Axin2, a downstream target of the Wnt/β-catenin pathway, but shows no effect on NF-κB, p53 reporter activity and GSK-3β activity. SKL2001 causes osteoblast differentiation (20 and 40 μM) and suppresses preadipocyte differentiation (5, 10, and 30 μM) via the activation of the Wnt/β-catenin pathway. SKL2001 (5, 10, and 30 μM) stabilizes intracellular β-catenin in 3T3-L1 cells. SKL2001 (40 μM) significantly inhibits the proliferation of HCT116 spheroids independently of cytotoxicity and the inhibition is reversible; SKL2001 cuases cell cycle arrest in HCT116 spheroids. SKL2001 (40 μM) enhances round-shape spheroid formation and E-cadherin expression.