SKL2001

Cas No.:	909089-13-0
Synonyms:	SKL2001,SKL-2001,SKL 2001
SMILES:	O=C(C1=NOC(C2=CC=CO2)=C1)NCCCN3C=CN=C3
Formula:	C14H14N4O3
M.Wt:	286.29
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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.