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SKL2001 (Synonyms: Wnt Agonist II)

Katalog-Nr.GC16382

SKL2001 ist ein Agonist des Wnt/β-Catenin-Signalwegs mit Anti-Krebs-AktivitÄt. SKL2001 stabilisiert intrazellulÄres β-Catenin durch Unterbrechung der Axin/β-Catenin-Wechselwirkung.

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SKL2001 Chemische Struktur

Cas No.: 909089-13-0

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 2 publications

Description of SKL2001

SKL2001 is an agonist of the Wnt/β-catenin pathway. SKL2001 stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction, and can be applied to regulate mesenchymal stem cell differentiation[1].

SKL2001 (5, 10, and 30μM; 3d) consistently induced the accumulation of intracellular β-catenin and inhibited the expression of C/EBPα and PPARγ. The exposure of 3T3-L1 and ST2 cells to SKL2001 resulted in a concentration-dependent decrease in lipid droplet accumulation in response to insulin[1]. SKL2001 (10, 30μM; 15h) upregulated β-catenin responsive transcription by increasing the intracellular β-catenin protein level and inhibited the phosphorylation of β-catenin at residues Ser33/37/Thr41 and Ser45[1].Treatment of ECs with SKL2001 at 30μM for 12h induced the expressions of MALAT1, ZO-1 and Occludin[2].

SKL2001 (6mg/kg; ip; 7d) treatment results in a decrease in the permeability of the aortic wall of the mice[2].In the doxorubicin mouse model, SKL2001 (4mg/kg; ip; 7d) stimulated rCFs to activate the Wnt/β-catenin pathway, inducing cardiac dysfunction and myocardial fibrosis in mice[3].

References:
[1]. Gwak J, Hwang S G, Park H S, et al. Small molecule-based disruption of the Axin/β-catenin protein complex regulates mesenchymal stem cell differentiation[J]. Cell research, 2012, 22(1): 237-247.
[2]. Yang F, Zhang Y, Zhu J, et al. Laminar flow protects vascular endothelial tight junctions and barrier function via maintaining the expression of long non-coding RNA MALAT1[J]. Frontiers in Bioengineering and Biotechnology, 2020, 8: 647.
[3]. Yuan M, Shi H, Wang B, et al. Targeting SOCS2 alleviates myocardial fibrosis by reducing nuclear translocation of β-catenin[J]. Biochimica et Biophysica Acta (BBA)-Molecular Cell Research, 2024, 1871(7): 119804.

Protocol of SKL2001

Cell experiment [1]:

Cell lines

3T3-L1 and ST2 cells

Preparation Method

SKL2001 (5, 10, and 30μM) was administered to cells during adipocyte differentiation for 3 days. The total proteins were prepared and subjected to western blotting with anti-β-catenin, anti-PPARγ and anti-C/EBPα antibodies.

Reaction Conditions

5, 10, and 30μM; 3d

Applications

SKL2001 consistently induced the accumulation of intracellular β-catenin and inhibited the expression of C/EBPα and PPARγ. The exposure of 3T3-L1 and ST2 cells to SKL2001 resulted in a concentration-dependent decrease in lipid droplet accumulation.
Animal experiment [2]:

Animal models

Arterial Endothelial Barrier Model

Preparation Method

Mice were injected intraperitoneally with SKL2001 (6mg/kg in 100μL of DMSO), XAV939 (4mg/kg in 100μL of DMSO) or DMSO (100μL) daily for 7 days. The arterial endothelial permeability to Evans blue dye was assessed.

Dosage form

6mg/kg; ip; 7d

Applications

Aortic wall permeability to Evans blue was reduced in SKL2001-treated mice.

References:
[1]. Gwak J, Hwang S G, Park H S, et al. Small molecule-based disruption of the Axin/β-catenin protein complex regulates mesenchymal stem cell differentiation[J]. Cell research, 2012, 22(1): 237-247.
[2]. Yang F, Zhang Y, Zhu J, et al. Laminar flow protects vascular endothelial tight junctions and barrier function via maintaining the expression of long non-coding RNA MALAT1[J]. Frontiers in Bioengineering and Biotechnology, 2020, 8: 647.

Chemical Properties of SKL2001

Cas No. 909089-13-0 SDF
Überlieferungen Wnt Agonist II
Chemical Name N-(3-(1H-imidazol-1-yl)propyl)-5-(furan-2-yl)isoxazole-3-carboxamide
Canonical SMILES O=C(C1=NOC(C2=CC=CO2)=C1)NCCCN3C=CN=C3
Formula C14H14N4O3 M.Wt 286.29
Löslichkeit DMF: 25 mg/ml,DMSO: 25 mg/ml,Ethanol: 25 mg/ml,Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of SKL2001

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.493 mL 17.4648 mL 34.9296 mL
5 mM 0.6986 mL 3.493 mL 6.9859 mL
10 mM 0.3493 mL 1.7465 mL 3.493 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 8 reference(s) in Google Scholar.)

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