A potent inhibitor of PORCN (IC50 = 74 pM)

Wnt-C59 – 1 mg

Brand:
Cayman
CAS:
1243243-89-1
Storage:
-20
UN-No:
Non-Hazardous - /

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/β-catenin pathway target genes in mice.{27062,27063}  

 

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Description

A potent inhibitor of PORCN (IC50 = 74 pM), completely blocking Wnt secretion into culture media; prevents activation of all evaluated Wnt family members; effective in vivo as well as in vitro; blocks the progression of breast cancer while downregulating Wnt/β-catenin pathway target genes in mice

Formal name: 4​-​(2​-methyl​-4​-​pyridinyl)​-​N​-​[4​-​(3​-​pyridinyl)​phenyl]​-benzeneacetamide

Synonyms:  PORCN Inhibitor II

Molecular weight: 379.5

CAS: 1243243-89-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Acyltransferases||Research Area|Cancer|Cell Signaling|Wnt Signaling||Research Area|Cell Biology|Cell Signaling|Wnt Signaling

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