Wnt-C59 (C59)

Catalog No.S7037

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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2 Customer Reviews

  • (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.

    Dev Neurobiol, 2016, 76(9):983-1002. . Wnt-C59 (C59) purchased from Selleck.

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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.
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
human HT1080 cells NYK3Z|VOTnWwY4Tpc44h[XO|YYm= M4GzV2lvcGmkaYTpc44hd2ZicH;yZ5VxcW6nIHHjeIl3cXS7IDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJIh2dWGwIFjUNVA5OCClZXzsd{Bie3Onc4Pl[EBieyC|dYDwdoV{e2mxbjDv[kBYdnR|QT3t[YRq[XSnZDDzeZBmeiC2b4Cg[oxie2hiYXP0bZZqfHliYomgV3RHKGy3Y3nm[ZJie2ViYYPzZZktKEmFNUC9O{41\S1yNTFOwG0v NIT4dJkzPjV{Mkm0Oi=>

... Click to View More Cell Line Experimental 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

Animal Research:[1]
+ Expand
  • Animal Models: Female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors
  • Formulation: 0.5% methylcellulose and 0.1% Tween-80
  • Dosages: 10 mg/kg
  • Administration: orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 76 mg/mL (200.28 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID