| Description: |
SKL2001 is an agonist of the Wnt/β-catenin pathway, with anti-cancer activity. |
| Target: |
Wnt/β-catenin[1] |
| 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[1]. 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[2]. |
| Cell Assay: |
ST2 cells are cultured on glass chamber slides and then treated with DMSO or SKL2001 for 15 h. After treatment, the cells are washed with PBS, fixed with 4% formaldehyde, permeabilized in 0.3% Triton X-100, and blocked in 4% bovine serum albumin for 1 h. The cells are stained with anti-β-catenin antibody and then analyzed by confocal microscopy using a microscope[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.
[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. |
