Wnt-C59

Territorial Availability: Available through Bertin Technologies only in France

• Synonyms
  • 4-(2-methyl-4-pyridinyl)-N-[4-(3-pyridinyl)phenyl]-benzeneacetamide
• Correlated keywords
  • cancer signal transduction stem cell research biology intracellular signaling diabetes inhibit inhibitor porcupine PORCN O-acetyltransferases palmitoylation Wnt family protein secretion activity embryo embryonic development WntC59 Wnt3A Wnt-3A activation culture media mediums in vivo vitro intravenous IV oral administration half-life blood block blocking basal-like triple-negatives breasts downregulating downregulates Wnt/?-catenin ?-catenin pathway target gene mouse mice C59 C-59 protein lipidation
• Product Overview:
  Porcupine (PORCN) is a membrane bound O-acyltransferase that mediates palmitoylation of Wnt family proteins.{27064} This step is required for secretion and biologic activity of Wnt proteins, which have roles in embryonic development and cancer.{27064,27062} Wnt-C59 is a potent inhibitor of PORCN, as measured by prevention of Wnt3A activation (IC50 = 74 pM).{27062} As palmitoylation of Wnt is required for its secretion, Wnt-C59 completely blocks Wnt3A secretion into culture media.{27062} Wnt-C59 prevents activation of all evaluated Wnt family members.{27062} This compound is effective in vivo as well as in vitro. Whether given by intravenous (2.5 mg/kg) or oral administration (5 mg/kg), Wnt-C59 displays a half-life in blood of approximately 1.94 hours, and remains greater than 10-fold above the in vitro IC50 concentration for at least 16 hours after a single oral dose.{27062} It blocks the progression of both basal-like and triple-negative breast cancers while downregulating Wnt/?-catenin pathway target genes in mice.{27062,27063}