2-(4-(2-Methylpyridin-4-yl)phenyl)-N-4-(pyridin-3-yl)phenyl)acetamide ≥98%, crystalline solid (Wnt-C59)
Fornitore: Cayman Chemical
Synonyms:
2-(4-(2-Methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide, Wnt-C59, Wnt Antagonist, C59
Wnt-C59 is a potent inhibitor of PORCN
Porcupine (PORCN) is a membrane bound O-acyltransferase that mediates palmitoylation of Wnt family proteins. This step is required for secretion and biologic activity of Wnt proteins, which have roles in embryonic development and cancer. Wnt-C59 is a potent inhibitor of PORCN, as measured by prevention of Wnt3A activation (IC50 = 74 pM). As palmitoylation of Wnt is required for its secretion, Wnt-C59 completely blocks Wnt3A secretion into culture media. Wnt-C59 prevents activation of all evaluated Wnt family members.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.2 It blocks the progression of both basal-like and triple-negative breast cancers while downregulating Wnt/β-catenin pathway target genes in mice.
Attenzione: This product is not for human or veterinary use.
Formula:
C₂₅H₂₁N₃O Peso molecolare: 379,45 g/mol Temperatura di stoccaggio: Congelamento |
MDL Number:
MFCD22201167 CAS Number: 1243243-89-1 |
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