Home Stem Cells & Wnt Wnt/beta-catenin inhibitor iCRT14

iCRT14

Catalog No.S8704

For research use only.

iCRT14 is a β-catenin/Tcf inhibitor with a Ki value of 54 ± 5.2 μM in homogeneous fluorescence polarization (FP) assay.

iCRT14 Chemical Structure

CAS No. 677331-12-3

Selleck's iCRT14 has been cited by 2 Publications

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Biological Activity

Description iCRT14 is a β-catenin/Tcf inhibitor with a Ki value of 54 ± 5.2 μM in homogeneous fluorescence polarization (FP) assay.
Targets
β-catenin/Tcf [1]
54 μM(Ki)
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
Methods Test Index PMID
Western blot BIRC5 / Myc / Axin2 ; caspase 3 / cleaved caspase 3 / cleaved PARP ; Snail / pS9-GSK-3β / GSK-3β / Akt1 / Akt2 24995804 26711268
Growth inhibition assay Cell viability 24995804
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].

Protocol (from reference)

Cell Research:

[2]
  • Cell lines: Rat2 cells
  • Concentrations: 25 and 50 μM
  • Incubation Time: 2 h
  • Method:

    Rat2 cells are pretreated with iCRTs at the indicated doses and stimulated for 2 h with Wnt3a or Wnt5a. Cell lysate is harvested for western analysis of Dvl2 phosphorylation.
Animal Research:

[2]
  • Animal Models: HCT116 and HT29 xenograft models (implanted tumor cells in athymic nude mice)
  • Dosages: 50 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 375.44
Formula

C21H17N3O2S
CAS No. 677331-12-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=C(N1C2=CN=CC=C2)C)C=C3C(=O)N(C(=O)S3)C4=CC=CC=C4

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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