Application

iCRT3 has been used to inhibit the interactions between β-catenin and transcription factor (TCF).

iCRT3 has been used:for β- catenin inhibition in dual luciferase assayto inhibit β-catenin /TCF interactions and their transcriptional activityas wingless/tailess (wnt) antagonist, to determine Wnt/β-catenin signaling is essential for PROX1-mediated regulation of forkhead box protein C2 (FOXC2)(3)catenin inhibition in dual luciferase assayto inhibit β- catenin /TCF interactions and their transcriptional activityas wingless/tailess (wnt) antagonist, to determine Wnt/β-catenin signaling is essential for PROX1-mediated regulation of forkhead box protein C2 (FOXC2)

Biochem/physiol Actions

The key mediator of Wnt signaling is the transcriptional co-activator b-catenin. In the cytoplasm, b-catenin is tightly bound to a complex that includes Axin and GSK-3b. Stimulation causes b-catenin stabilization, translocation to the nucleus and association with TCF4 to initiate transcription of responsive genes, referred to as Catenin Responsive Transcription (CRT). Virtually all Wnt-associated cancers are the result of misregulated CRT. Three inhibitors of CRT (iCRT) were identified in a screen that employed RNAi based knockdown of Axin, which stimulates CRT without affecting upstream mechanisms such as GSK activity, transduction by disheveled / frizzled, etc. These compounds are potent inhibitors of CRT reporter genes, as well as endogenous gene targets. The compounds also disrupt b-catenin-TCF4 interaction in a dose dependent manner, and cause G0/G1 arrest in colon tumor lines.

General description

iCRT3 is a small cell-permeable oxazole compound. It blocks cytokine secretion in lipopolysaccharide (LPS)-stimulated macrophages.

Packaging

5, 25 mg in glass bottle