A potent inhibitor of the Wnt response

IWR-1-endo – 5 mg

Brand:
Cayman
CAS:
1127442-82-3
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. IWR-1-endo is a potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response with an IC50 value of 180 nM.{17505} It inhibits, at 10 μM, Wnt-induced accumulation of β-catenin, leading to proteasomal degradation of this protein through a destruction complex which consists of Apc, Axin2, Ck1, and GSK3β. IWR-1-endo stabilizes the destruction complex, increasing the level of Axin2 protein without changing the levels of Apc or GSK3β.{17505} The IWR compound does not change the de novo synthesis of Axin2, alter the affinity of Axin2 for β-catenin, or inhibit the proteasome. It has a half-life of 60 minutes in murine whole blood and 20 minutes in intact murine hepatocytes.{17948} In in vivo tests, IWR-1-endo inhibits zebrafish tail fin regeneration with a minimum inhibitory concentration of 0.5 μM.{17948} The IWR-1-exo diastereomer exhibits much less activity against the Wnt/β-catenin pathway and has been used as a control.{17505}  

 

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Description

A potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response (IC50 = 180 nM); inhibits Wnt-induced accumulation of β-catenin, leading to proteasomal degradation of this protein

Formal name: 4-[(3aR,4S,7R,7aS)-1,3,3a,4,7,7a-hexahydro-1,3-dioxo-4,7-methano-2H-isoindol-2-yl]-N-8-quinolinyl-benzamide

Synonyms: 

Molecular weight: 409.4

CAS: 1127442-82-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Cell Biology|Cell Signaling|Wnt Signaling||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System

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