A potent inhibitor of PORCN (EC50 = 0.5 nM); displays high stability in human plasma (t1/2 > 24 hours) and in zebrafish

IWP-L6 – 50 mg

Brand:
Cayman
CAS:
1427782-89-5
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} IWP-L6 is a potent inhibitor of PORCN (EC50 = 0.5 nM).{27202} It suppresses the phosphorylation of disheveled 2 in HEK293 cells. IWP-L6 displays high stability in human plasma (t1/2 > 24 hours) and in zebrafish, but it is much less stable in plasma from mice and rats.{27202} In zebrafish, IWP-L6 blocks Wnt/β-catenin-dependent developmental processes, including tailfin regeneration and posterior axis formation.{27202} It also completely prevents branching morphogenesis in cultured mouse embryonic kidneys at doses of 50 nM and above, indicating complete inhibition of Wnt signaling.{27202}  

 

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Description

A potent inhibitor of PORCN (EC50 = 0.5 nM); displays high stability in human plasma (t1/2 > 24 hours) and in zebrafish, but is much less stable in plasma from mice and rats; completely blocks Wnt/β-catenin-dependent developmental processes in zebrafish and in cultured mouse embryonic kidneys

Formal name: N-(5-phenyl-2-pyridinyl)-2-[(3,4,6,7-tetrahydro-4-oxo-3-phenylthieno[3,2-d]pyrimidin-2-yl)thio]-acetamide

Synonyms:  PORCN Inhibitor III|Wnt Pathway Inhibitor XIX

Molecular weight: 472.6

CAS: 1427782-89-5

Purity: ≥98%

Formulation: A crystalline solid

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

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