SKL2001

SKL2001 is an agonist of the Wnt/β-catenin pathway, with anti-cancer activity.

Signaling Pathways >> Stem Cell/Wnt >> β-catenin

Signaling Pathways >> Stem Cell/Wnt >> Wnt

Research Areas >> Cancer

Wnt/β-catenin[1]

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].

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].

[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.

XAV-939 | ICG-001 | Salinomycin | IWR-1 | Wnt-C59 | Berberine chloride hydrate | Pyrvinium pamoate | ETC-159 | BML 284 | IWP-2 | Heparan Sulfate | KYA 1797K | FH535 | CCT251545 | iCRT-14