SKL2001

Catalog No.S8320

SKL2001 Chemical Structure

Molecular Weight(MW): 286.29

SKL2001 is a novel agonist of the Wnt/β-catenin pathway. It disrupts the Axin/β-catenin interaction.

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3 Customer Reviews

  • G. Enforced Wnt signaling by SKL-2001 restored cell growth in miR-520e overexpression A549 cells

    Biochem Biophys Res Commun, 2017, 486(1):49-56. SKL2001 purchased from Selleck.

    C and D. Forced Wnt/b-catenin signaling by SKL-2001 restored the cell growth in FOXD2-AS1 knockdown NSCLC cells.

    Biochem Biophys Res Commun, 2017(484):586e591. SKL2001 purchased from Selleck.

  • (D) Overexpression of CASC2 suppressed the protein expression of β-catenin, Cyclin-D1, and c-Myc in U251 cells and the effect could be reversed by SKL2001. (E) CASC2 overexpression restrained the proliferation, migration, and invasion capacity in U251 cells and SKL2001 could reverse the effect of CASC2.

    Neuropsychiatr Dis Treat, 2017, 13:1805-1813. SKL2001 purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description SKL2001 is a novel agonist of the Wnt/β-catenin pathway. It disrupts the Axin/β-catenin interaction.
Targets
Wnt/β-catenin [1]
(Cell-free assay)
In vitro

SKL2001 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, which would mark it for proteasomal degradation, without affecting CK1 and GSK-3β enzyme activities. SKL2001 disrupted the Axin/β-catenin interaction, which is a critical step for CK1- and GSK-3β-mediated phosphorylation of β-catenin at Ser33/37/Thr41 and Ser45. The treatment of mesenchymal stem cells with SKL2001 promoted osteoblastogenesis and suppressed adipocyte differentiation, both of which were accompanied by the activation of Wnt/β-catenin pathway. SKL2001 did not affect either NF-κB or p53 reporter activity and inhibits β-catenin phosphorylation without affecting GSK-3β activity[1].

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: HEK293 reporter and control cell lines
  • Concentrations: 20 μM
  • Incubation Time: 15 h
  • Method: The HEK293 reporter and control cell lines were established. The HEK293 reporter cells were inoculated into 384-well plates at 10 000 cells per well and grown for 24 h. Next, each compound in the chemical library (∼270 000) was added to at a final concentration of 20 μM. After 15 h, the plates were assayed for firefly luciferase activity.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 57 mg/mL (199.09 mM)
Ethanol 57 mg/mL (199.09 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
7mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 286.29
Formula

C14H14N4O3

CAS No. 909089-13-0
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Wnt/beta-catenin Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID