Wnt-C59 (C59)
Catalog No.S7037
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.
-Exp-Cel-Res-20170118.gif)
3 Customer Reviews
-
Migration of L428 cells (b) and KM-H2 (c) after 72 h pretreatment with 5 μm Wnt-C59 or DMSO with (+CM) or without (−CM) the simultaneous stimulation with the respective cHL-CM for 24 h (mean±s.d., n=3, one-way ANOVA and Dunn’s post hoc test). Note the inhibition of migration by porcupine inhibitors, which is rescued by CM. (d) Invasion of L428 or KM-H2 cells after 72 h pretreatment with 5 μm Wnt-C59 or DMSO (mean±s.d., n=3 two-way ANOVA and Bonferroni’s post hoctest). (e) Adhesion of DMSO- or Wnt-C59-pretreated L428 cells on either HUVECs (white) or collagen I (gray) (mean±s.d., n=5, 2-way ANOVA and Bonferroni’s post hoc test). Note the decrease of adhesion after WNT inhibition (*P<0.05 and ***P<0.001).
Oncogene, 2017, 36(1):13-23. Wnt-C59 (C59) purchased from Selleck.
(B) Wnt3a, β-catenin, and cyclin D1 expression in hAMSCs was determined by western blotting. hAMSCs were pre-treated with or without Wnt-C59 (100 nM), 1 h before HA (0.6 mg/ml, 36 h) treatment. hAMSCs lysates were then prepared and subjected to western blotting using antibodies specific to wnt3a, β-catenin, and cyclin D1. Quantification graphs (relative density) reflected the intensity of respective proteins to β-actin. Data are shown as means±S.D. (n=3). Control culture received medium alone. *p<0.05, **p<0.01 vs control. #p<0.05, ##p<0.01 vs HA group.
Exp Cell Res, 2016, 345(2):218-29.. Wnt-C59 (C59) purchased from Selleck.
-
Application of XAV939 or Wnt-c59 with FGF2 blocks the accumulation of nuclear b-catenin in MGPCs, and increases levels of p38MAPK in Muller glia, whereas levels of cFos are unaffected. a, b, Eyes were injected with four consecutive daily injections of FGF2 6 XAV939 or Wnt-c59, BrdU 24 h after the last injection of FGF2, and retinas harvested 24 h later. Wnt-c59 (treated). a, b-catenin in the nuclei of Sox91 Muller glia/MGPCs on 70% grayscale background.
Dev Neurobiol, 2016, 76(9):983-1002. . Wnt-C59 (C59) purchased from Selleck.
Purity & Quality Control
Choose Selective Wnt/beta-catenin 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 |
|
||||||||||||||||
| 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 |
|
||||||||||||||||
| 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
| Cell Research: |
+ Expand
|
|---|---|
| Animal Research: |
+ Expand
|
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. |
5mg/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 | 379.45 |
|---|---|
| Formula | C25H21N3O |
| CAS No. | 1243243-89-1 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
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.
