Wnt-C59 (C59)

For research use only.

Catalog No.S7037

47 publications

Wnt-C59 (C59) Chemical Structure

Molecular Weight(MW): 379.45

Wnt-C59 (C59) is a PORCN inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase with IC50 of 74 pM in HEK293 cells.

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Selleck's Wnt-C59 (C59) has been cited by 47 publications

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Biological Activity

Description Wnt-C59 (C59) is a PORCN inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase with IC50 of 74 pM in HEK293 cells.
Porcn [1]
(HEK293 cells )
74 pM
In vitro

Wnt-C59 (C59) is claimed to inhibit PORCN enzyme activity at nanomolar concentrations. Wnt-C59 (10 nM) blocks the palmitoylation-dependent Wnt–WLS interaction in HeLa cells transfected with either WNT3A-V5 or WNT8A-V5 plasmids. Wnt-C59 (100 nM) prevents incorporation of palmitate into WNT3A in HeLa cells transfected with WNT3A-V5, consistent with inhibition of PORCN activity. Wnt-C59 (100 nM) inhibits the activity of all splice variants of murine PORCN in PORCN-null HT1080 cells transfected with PORCN. Wnt-C59 is a nanomolar inhibitor of mammalian PORCN acyltransferase activity and blocks activation of all evaluated human Wnts. Wnt-C59 does not significantly inhibit the proliferation of any of 46 tested cancer cell lines in vitro at concentrations that completely inhibit PORCN. [1] Wnt-C59 is capable to significantly inhibit proliferation and comparable to the ICG-001 treated NMuMG (NMG) cells. Wnt-C59 inhibits sphere formation by threefold in NMuMG (NMG) cells, which is dependent on Wnt10b-secretion. Wnt-C59 inhibits proliferation of human MDA-MB 231 cells by >50%. [2] Wnt-C59 (a Porcupine inhibitor) blocks radiolabel incorporation of [125I]iodo-pentadecanoate in mouse L-Wnt3a cells transfected with Flag-Porcupine. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HT1080 cells NFzFSXlHfW6ldHnvckBie3OjeR?= NVXyUXc1UW6qaXLpeIlwdiCxZjDwc5JkfXCrbnWgZYN1cX[rdImgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hcHWvYX6gTHQyODhyIHPlcIx{KGG|c3Xzd4VlKGG|IIP1dJBz\XO|aX;uJI9nKFewdEPBMY1m\GmjdHXkJJN2eGW{IITvdEBndGG|aDDhZ5Rqfmm2eTDifUBUXEZibIXjbYZmemG|ZTDhd5NigSxiSVO1NF04NjSnLUC1JO69VS5? NX7o[FJ{OjZ3MkK5OFY>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
β-catenin / pPKC; 

PubMed: 26941358     

Western blotting analysis in cortical neurons on day 18. Each WNT inhibitor inhibited Wnt/β-catenin-dependent signaling during the SFEBq differentiation procedure, but C59 also inhibited Wnt/β-catenin independent signaling.

Cyclin D1; 

PubMed: 31156379     

C59 treatment significantly decreased the levels of cyclin D1 mRNA (0.66 ± 0.032, *p < 0.05 compared to control levels). However, exogenous Wnt3a prevented this decrease and recovered cyclin D1 mRNA to the levels in control cells, which were significantly different than those in C59-treated cells (1.16 ± 0.032, **p < 0.01).

Growth inhibition assay
Cell proliferation; 

PubMed: 25980501     

Cell proliferation influenced by concentrations of Wnt-C59 treatment. Wnt-C59 has a clear inhibitory effect on the growth of HK1 cells.

Cell viability; 

PubMed: 31156379     

Cytotoxicity was evaluated through assessment of mitochondrial functionality with an MTT assay. Treatment with C59 for 24 h at concentrations over 100 μM reduced SH-SY5Y vitality, causing a mortality rate of up to 40% at the 200 μM concentration (0.6 ± 0.011, ***p < 0.001). Although a slight decrease in SH-SY5Y vitality was observed at 100 μM, this difference was not significant.

25980501 31156379
In vivo Wnt-C59 concentration remains greater than 10-fold above the in vitro IC50 for at least 16 hours following a single oral dose (5 mg/kg) in mice. Wnt-C59 (10 mg/kg) prevents growth of MMTV-WNT1 tumors in female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors. Wnt-C59 (10 mg/kg) decreases Wnt pathway activity and decreased proliferation in MMTV-WNT1 tumors in female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors as evident by decreased expression of β-catenin target gene expression. [1] Wnt-C59 (10%) topically administered 4 weeks decreases the size of dysplasia of SmoM2-expressing cells in adult K14CREER/Rosa–SmoM2 mice. [4]


Cell Research:


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  • Cell lines: NMuMG (NMG) and MDA-MB 231 cells
  • Concentrations: --
  • Incubation Time: 48 hours
  • Method:

    Seed cells at a concentration of 4×103/well in 100 μL culture medium containing various amouts of Wnt-C59. Incubate cells for 48 hours at 37 ℃. Add 10 μL/well cell proliferation reagent and incubate for 4 hours at 37 ℃. Shake thoroughly for 1 min on a shaker. Measure the absorbance of the samples in a microplate (ELISA) reader.

    (Only for Reference)
Animal Research:


- Collapse
  • Animal Models: Female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors
  • Dosages: 10 mg/kg
  • Administration: orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 76 mg/mL (200.28 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

* 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 379.45


CAS No. 1243243-89-1
Storage powder
in solvent
Synonyms N/A
Smiles CC1=NC=CC(=C1)C2=CC=C(CC(=O)NC3=CC=C(C=C3)C4=CC=CN=C4)C=C2

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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O

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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.

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Frequently Asked Questions

  • Question 1:

    I want to use Wnt-C59 for i.p. injection, can you advise how to dissolve it?

  • Answer:

    S7037 Wnt-C59 can be dissolved in 2% DMSO+30% PEG 300+5% Tween 80+ddH2O at 5 mg/ml as a clear solution. After stayed for a while, the precipitation will go out. So it is recommended to prepare the solution just before use.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID