SKL2001

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

SKL2001 Chemical Structure

SKL2001 Chemical Structure

CAS: 909089-13-0

Selleck's SKL2001 has been cited by 44 publications

Purity & Quality Control

Batch: Purity: 99.49%
99.49

SKL2001 Related Products

Choose Selective Wnt/beta-catenin Inhibitors

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
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].
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot β-catenin PPARγ / C/EBPα 21826110
Immunofluorescence β-catenin 21826110

Chemical Information & Solubility

Molecular Weight 286.29 Formula

C14H14N4O3

CAS No. 909089-13-0 SDF Download SKL2001 SDF
Smiles C1=COC(=C1)C2=CC(=NO2)C(=O)NCCCN3C=CN=C3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 57 mg/mL ( (199.09 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 57 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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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

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