An inhibitor of Wnt production that impairs Wnt pathway activity (IC50 = 40 nM in vitro) by inactivating Porcupine

IWP-3 – 1 mg

Brand:
Cayman
CAS:
687561-60-0
Storage:
-20
UN-No:
Non-Hazardous - /

Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{17947,14336,13185} Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription. IWP-3 is an inhibitor of Wnt production that impairs Wnt pathway activity in vitro with an IC50 value of 40 nM.{17505} IWP-3 inactivates porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins, which is essential for their signaling ability and secretion.{17505} At 5 μM, IWP-3 has been shown to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 (LRP6) and the scaffold protein Dishevelled, preventing the accumulation of β-catenin.{17505} By inhibiting Wnt signaling, IWP-3 has been used to promote cardiomyocyte generation from human embryonic stem cells (EC50 = 1.2 μM).{23267}  

 

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Description

An inhibitor of Wnt production that impairs Wnt pathway activity (IC50 = 40 nM in vitro) by inactivating Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins; promotes stem cell differentiation

Formal name: 2-[[3-(4-fluorophenyl)-3,4,6,7-tetrahydro-4-oxothieno[3,2-d]pyrimidin-2-yl]thio]-N-(6-methyl-2-benzothiazolyl)-acetamide

Synonyms:  Inhibitor of Wnt Production-3

Molecular weight: 484.6

CAS: 687561-60-0

Purity: ≥98%

Formulation: A crystalline solid

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

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