SKL2001 acts as an agonist for the Wnt/β-catenin signaling pathway and exhibits anti-cancer properties. It achieves stabilization of β-catenin within cells by disrupting the interaction between Axin and β-catenin. Additionally, SKL2001 upregulates Axin2 expression, a downstream component of the Wnt/β-catenin pathway, while not affecting NF-κB, p53 reporter activities, or GSK-3β activity. It promotes osteoblast differentiation at concentrations of 20 and 40 μM and inhibits preadipocyte differentiation at 5, 10, and 30 μM, through the activation of the Wnt/β-catenin pathway. At these same concentrations, SKL2001 also maintains the stability of intracellular β-catenin in 3T3-L1 cells[1]. At a concentration of 40 μM, SKL2001 markedly suppresses the proliferation of HCT116 spheroids without inducing cytotoxic effects, and this suppression can be reversed. Additionally, SKL2001 induces cell cycle arrest in HCT116 spheroids. Furthermore, at the same concentration, SKL2001 promotes the formation of round-shaped spheroids and the expression of E-cadherin[2].
SKL2001 细胞实验
Cell Line
Concentration
Treated Time
Description
References
MLO-Y4 cells
60 µM
24 hours
Activate Wnt signaling pathway and promote osteoblast differentiation
Cells. 2022 Feb 28;11(5):831
cultured blastema cells
40 μM
24 h
To test the effect of SKL2001 on Akt phosphorylation, it was found that SKL2001 treatment enhanced Akt phosphorylation.
Commun Biol. 2022 Sep 27;5(1):1018.
mouse primary chondrocytes
40 μM
15 h
SKL2001, as an agonist of the Wnt/β-catenin pathway, was used to reverse the effect of IL-1β on the Wnt/β-catenin pathway. The results showed that SKL2001 significantly inhibited the cell viability of microsphere-treated IL-1β-stimulated chondrocytes and increased cell apoptosis.
Mater Today Bio. 2024 Oct 16;29:101300.
THP-1 macrophages
20 µM
1 h
To verify the effect of SKL2001 on the expression of β-catenin and c-Myc in THP-1 macrophages, the results showed that SKL2001 increased the expression of β-catenin and c-Myc.
Int J Biol Sci. 2024 Jan 1;20(3):848-863.
CRC cells
30 μM
24 h
To investigate the role of β-catenin signaling in the regulation of TFAM expression in CRC cells, 30 μM SKL2001 was added into cell culture medium for 24h. The results showed that SKL2001 significantly upregulated the expression of TFAM.
Cancer Commun (Lond). 2021 Aug;41(8):695-714.
Human memory CD8+ T cells
20 μM
7 days
SKL2001 mildly suppressed cell proliferation, increased the expression of CD27, CD28, and CD62L, while decreasing the expression of KLRG1, indicating it generates more TCM cells through the Wnt pathway.
J Clin Invest. 2022 Jan 18;132(2):e140508.
Human memory CD8+ T cells
20 μM
7 days
SKL2001 significantly increased the proportion of IL-2+ cells and enhanced polyfunctionality, indicating it enhances the polyfunctionality of memory CD8+ T cells through the Wnt pathway.
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