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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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.
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Choose Selective Wnt/beta-catenin Inhibitors
|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.|
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.  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%.  Wnt-C59 (a Porcupine inhibitor) blocks radiolabel incorporation of [125I]iodo-pentadecanoate in mouse L-Wnt3a cells transfected with Flag-Porcupine. 
|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.  Wnt-C59 (10%) topically administered 4 weeks decreases the size of dysplasia of SmoM2-expressing cells in adult K14CREER/Rosa–SmoM2 mice. |
|In vitro||DMSO||76 mg/mL (200.28 mM)|
|In vivo||Add solvents to the product individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
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Frequently Asked Questions
I want to use Wnt-C59 for i.p. injection, can you advise how to dissolve it?
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.