Wnt-C59 (C59)

Catalog No.S7037

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

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Wnt-C59 (C59) Chemical Structure

Wnt-C59 (C59) Chemical Structure
Molecular Weight: 379.45

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Quality Control & MSDS

Product Information

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Product Description

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.
Targets Porcn [1]
IC50 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]
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]
Features

Protocol(Only for Reference)

Cell Assay: [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 Study: [1]

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
Solubility 0.5% methylcellulose/0.2% Tween 80, , 30 mg/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.
1

References

[1] Proffitt KD, et al. Cancer Res, 2013, 73(2), 502-507.

[2] Wend P, et al. EMBO Mol Med, 2013, 5(2), 264-279.

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Chemical Information

Download Wnt-C59 (C59) SDF
Molecular Weight (MW) 379.45
Formula

C25H21N3O

CAS No. 1243243-89-1
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 76 mg/mL (200 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 0.5% methylcellulose/0.2% Tween 80, 30 mg/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 Name 2-(4-(2-methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide

Research Area

Tech Support & FAQs

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