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SKL2001 is a small-molecule agonist of the Wnt/β-catenin signaling pathway. It was discovered through a cell-based chemical screening assay of a synthetic chemical library by researchers at Kookmin University and SK Biopharmaceuticals. SKL2001 acts by disrupting the interaction between Axin and β-catenin within the β-catenin destruction complex. This disruption prevents the phosphorylation of β-catenin at residues Ser33/37/Thr41 and Ser45 by CK1 and GSK-3β, thereby protecting β-catenin from proteasomal degradation. Consequently, intracellular β-catenin accumulates and translocates to the nucleus, activating Wnt/β-catenin-dependent transcription. SKL2001 has been widely used as a research tool to study mesenchymal stem cell differentiation (promoting osteoblastogenesis and suppressing adipogenesis), tissue regeneration, and potential anti-cancer therapies (such as in colorectal cancer).
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