iCRT14

Catalog No.S8704

iCRT14 Chemical Structure

Molecular Weight(MW): 375.44

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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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 ; 

PubMed: 24995804     


Western blot analysis of BIRC5, MYC and AXIN2 protein levels with and without treatment with the inhibitor. Actin was used as the loading control

caspase 3 / cleaved caspase 3 / cleaved PARP; 

PubMed: 24995804     


Western blots showing cleavage of caspase 3 and PARP in UOCB1 cells after treatment with 20 μM of iCRT14 in comparison to the untreated cells. Actin was used as the loading control.

Snail / pS9-GSK-3β / GSK-3β / Akt1 / Akt2; 

PubMed: 26711268     


iCRT14 (25 μM) was added to the PAE-CTL and PAE-NICD2 cell medium for the last 24 h. The indicated nuclear proteins (D) were analyzed at 72 h after iCRT14 addition.

24995804 26711268
Growth inhibition assay
Cell viability; 

PubMed: 24995804     


UOCB1 cells were treated with iCRT14 for 48 hours before adding (A) Prednisolone (0-500 μg/mL) (B)Etoposide (0-1 μM) (C) 6TG (0-20 μg/mL) (D) Doxorubicin (0-125 nM) and (E) Cytarabine (0-5 μg/mL). Cell viability was assessed at 72 hours. * indicates synergistic drug combination (CI<0.9). Results graphed show the effect of chemotherapy alone, iCRT14 alone and various dose combinations of the inhibitor and chemotherapy. Error bars represent standard deviation of the mean.

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

Cell Research:

[2]

+ Expand
  • 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.


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • Animal Models: HCT116 and HT29 xenograft models (implanted tumor cells in athymic nude mice)
  • Formulation: DMSO
  • Dosages: 50 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 37 mg/mL (98.55 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 375.44
Formula

C21H17N3O2S

CAS No. 677331-12-3
Storage powder
in solvent
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID