| Description | iCRT14 is a β-catenin/Tcf inhibitor with a Ki value of 54 ± 5.2 μM in homogeneous fluorescence polarization (FP) assay. | |||||||||
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| Targets |
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| In vitro | iCRT14 suppresses the transcriptional activity of canonical Wnt signaling, downregulates Wnt/β-catenin-induced target genes, and inhibits the growth of colorectal cancer cells in vitro[1]. iCRT14 shows a modest reduction in the amount of Dvl but has no effect on Dvl phosphorylation itself. iCRT14 inhibits the Wnt responsive STF16-luc reporter in mammalian HEK293 cells with an IC50 of 40.3 nM. iCRT14 can also interfere with TCF binding to DNA in addition to its ability to influence TCF-β-catenin interaction[2]. | |||||||||
| Assay |
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| In vivo | Administration of iCRT14 to the HCT116 and HT29 xenograft models reveals a marked decrease in CycD1, coincided with reduced proliferation of the tumors. Furthermore, these effects are correlated with a marked reduction (∼50%) in the initial growth rate of tumors within the first 3 wk (∼day 19) of compound administration. After day 19, however, the rate of tumor growth is comparable with that of DMSO-treated control. Throughout the course of the study, the mice does not display any signs of systemic toxicity or weight loss that would indicate off-target or nonspecific effects. The compound may be metabolized rapidly in vivo, thus reducing its bioavailability[2]. |
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