Wnt-C59 (C59)

Catalog No.S7037

For research use only.

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.

Wnt-C59 (C59) Chemical Structure

CAS No. 1243243-89-1

Selleck's Wnt-C59 (C59) has been cited by 98 publications

Purity & Quality Control

Choose Selective PORCN Inhibitors

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.
Targets
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
HT1080 Ml71SpVv[3Srb36gZZN{[Xl? MmrtTY5pcWKrdHnvckBw\iCyb4LjeZBqdmViYXP0bZZqfHliKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gbJVu[W5iSGSxNFgxKGOnbHzzJIF{e2W|c3XkJIF{KHO3cIDy[ZN{cW:wIH;mJHdvfDODLX3l[IlifGWmIIP1dIVzKHSxcDDmcIF{cCCjY4Tpeol1gSCkeTDTWGYhdHWlaX\ldoF{\SCjc4PhfUwhUUN3MDC9JFAvODd2IH7NMi=> NEHRS5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkWyNlk1Pid-Mk[1NlI6PDZ:L3G+
HEK293T M3yxVWZ2dmO2aX;uJIF{e2G7 MUKyNkBpenN? M4HyeWlvcGmkaYTpc44hd2ZicH;yZ5VxcW6nIHnuJGhGUzJ7M2SgZ4VtdHNidILhcpNn\WO2ZXSge4l1cCCZboSzRU1mgHC{ZYPzbY5oKH[nY4TvdkBie3Onc4Pl[EBieyC|dYDwdoV{e2mxbjDv[kBYdnRxYnX0ZU1k[XSnbnnuJJNq\26jbHnu[{Bi\nSncjCyNkBpenNiYomgV5Vx\XJvdH;wJIZt[XOqIILldI9zfGW{IHflcoUh[XO|YYmsJGlEPTBiPTCxJI5ONg>? NEH2UIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[zNFM3Pid-Mkm2N|A{PjZ:L3G+
A673 MXfxTHRUKGG|c3H5 MWnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC M2m0Z5FJXFNiYYPzZZk> NFL5d2NyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Assay
Methods Test Index PMID
Western blot β-catenin / pPKC 26941358
Q-PCR Cyclin D1 31156379
Growth inhibition assay Cell proliferation ; Cell viability 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]

Protocol (from reference)

Cell Research:

[2]

  • 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.

Animal Research:

[1]

  • Animal Models: Female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors
  • Dosages: 10 mg/kg
  • Administration: orally

Solubility (25°C)

In vitro

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.

5mg/mL

Chemical Information

Molecular Weight 379.45
Formula

C25H21N3O

CAS No. 1243243-89-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=NC=CC(=C1)C2=CC=C(C=C2)CC(=O)NC3=CC=C(C=C3)C4=CN=CC=C4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02679001 Completed Drug: TNF inhibitor/TCZ Rheumatoid Arthritis Hoffmann-La Roche March 24 2016 --

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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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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