Wnt-C59 is a very potent and highly selective Wnt signaling antagonist with an IC50 ~ 74 pM in the Wnt signaling reporter assay. It prevents palmitylation of Wnt proteins by Porcupine (a membrane-bound O-acyltransferase), thereby blocking Wnt protein secretion and activity. Wnt-C59 displayed good bioavailability as once daily oral administration and blocked progression of mammary tumors in MMTV-WNT1 transgenic mice model while downregulating Wnt/β-catenin target genes. Because Wnt-C59 exhibits much better potency and selectivity than the reported IWP series of Porcupine/Wnt inhibitors, it serves as the better Wnt pathway inhibitor for in vitro and in vivo studies.
CAS Number: 1243243-89-1
Molecular Weight: 379.45
Chemical Name: 2-(4-(2-methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 50 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
Wnt-C59 was used at 0.1-0.2 µM to completely block Wnt protein secretion. When used at 0.5 µM, it can be used functionally replace the Dkk protein in many assay conditions.
Wnt-C59 was used to dose mice orally at 5-10 mg/kg once per day or 5 mg/kg twice per day.
- Proffitt KD, et al. Pharmacological inhibition of the Wnt acyltransferase PORCN prevents growth of WNT-driven mammary cancer. (2012) Cancer Res. In press.
- Chen D, et al. (N-(HETERO)ARYL,2-(HETERO)ARYL-SUBSTITUTED ACETAMIDES FOR USE AS WNT SIGNALING MODULATORS. PCT WO/2010/101849.
- Chen B, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. (2009) Nat Chem Biol. 5(2):100-7.
- Dodge ME, et al. Diverse chemical scaffolds support direct inhibition of the membrane bound O-acyltransferase Porcupine. (2012) J Biol Chem. 287 (27), pp. 23246–23254
- Willems E, et al. Small-molecule inhibitors of the Wnt pathway potently promote cardiomyocytes from human embryonic stem cell-derived mesoderm. (2011) Circ Res.109(4):360-4.
Products are for research use only. Not for human use.
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