Description
SKL2001 is an activator of Wnt/β-catenin signaling. It increases β-catenin responsive transcription in a cell-based reporter assay in a concentration-dependent manner, increases β-catenin protein levels in HEK293 cells when used at concentrations of 10 and 30 μM, and disrupts the interaction between Axin and β-catenin. SKL2001 increases alkaline phosphatase (ALP) activity and mineralization in multipotent mesenchymal ST2 cells in a concentration-dependent manner, indicating increased osteoblastogenesis. SKL2001 (40 μM) reduces HCT116 and HT-29 spheroid growth and inhibits proliferation of HCT116 and HT-29 cells. It induces cell cycle arrest at the G
0/G
1 phase and increases E-cadherin and β-catenin protein levels in HCT116 cells when used at a concentration of 40 μM.
Uses
SKL2001 is an agonist of the Wnt/β-catenin pathway, with anti-cancer activity. SKL2001 stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction[1].
References
[1] Gwak J, et al. Small molecule-based disruption of the Axin/β-catenin protein complex regulates mesenchymal stem cell differentiation. ell Res. 2012 Jan;22(1):237-47. DOI:
10.1038/cr.2011.127[2] Ohashi W, et al. SKL2001 suppresses colon cancer spheroid growth through regulation of the E-cadherin/β-Catenin complex. Biochem Biophys Res Commun. 2017 Nov 25;493(3):1342-1348. DOI:
10.1016/j.bbrc.2017.09.161
