Chemical Name: 5-[[2,5-Dimethyl-1-(3-pyridinyl)-1H-pyrrol-3-yl]methylene]-3-phenyl-2,4-thiazolidinedion
Biological ActivityiCRT 14 is a potent inhibitor of β-catenin-responsive transcription (CRT) (IC50 = 40.3 nM in assays of Wnt pathway activity). Thought to directly influence the interaction between β-catenin and TCF4. Induces marked G0/G1 cell cycle arrest in HCT-116 and HT29 cell lines. Also acts as transfection enhancer; enhances transgene expression in PC-3 cells by 16 to 35-fold using nonviral systems.
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An RNAi-based chemical genetic screen identifies three small-molecule inhibitors of the Wnt/wingless signaling pathway.
Gonsalves et al.
Winning WNT: race to Wnt signaling inhibitors.
Watanabe and Dai
Enhancement of transgene expression by the β-catenin inhibitor iCRT14.
Spivack et al.
Citations for iCRT 14
The citations listed below are publications that use Tocris products. Selected citations for iCRT 14 include:
5 Citations: Showing 1 - 5
Aging differentially modulates the Wnt pro-survival signalling pathways in vascular smooth muscle cells.
Authors: Brown Et al.
Aging Cell 2019;18:e12844
Trypanosoma cruzi Exploits Wnt Signaling Pathway to Promote Its Intracellular Replication in Macrophages.
Authors: Volpini Et al.
Front Immunol 2018;9:859
Mutant Isocitrate Dehydrogenase 1 Disrupts PKM2-β-Catenin-BRG1 Transcriptional Network-Driven CD47 Expression.
Authors: Gowda Et al.
Mol Cell Biol 2018;38
Sp5 and Sp8 recruit β-catenin and Tcf1-Lef1 to select enhancers to activate Wnt target gene transcription.
Authors: Kennedy Et al.
Proc Natl Acad Sci U S A 2016;113:3545
Differential modulation of the oligodendrocyte transcriptome by sonic hedgehog and bone morphogenetic protein 4 via opposing effects on histone acetylation.
Authors: Wu Et al.
J Neurosci 2012;32:6651
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HCT116 cells were treated with different concentrations of iCRT-14 for 24 hours and the cells were used for transwell assays to investigate the effects of Wnt inhibitor on cell migration.