iCRT14

Catalog No.S8704 Batch:S870401

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Technical Data

Formula

C21H17N3O2S
Molecular Weight 375.44 CAS No. 677331-12-3
Solubility (25°C)* In vitro DMSO 37 mg/mL (98.55 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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].
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 Assay:

[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 Study:

[2]
  • Animal Models

    HCT116 and HT29 xenograft models (implanted tumor cells in athymic nude mice)

  • Dosages

    50 mg/kg

  • Administration

    i.p.

Selleck's iCRT14 has been cited by 4 publications

Upregulation of β-catenin signaling represents a single common pathway leading to the various phenotypes of spinal degeneration and pain [ Bone Res, 2023, 11(1):18] PubMed: 37059724
Regulation of the WNT-CTNNB1 signaling pathway by severe fever with thrombocytopenia syndrome virus in a cap-snatching manner [ mBio, 2023, e0168823.] PubMed: 37882780
β-catenin regulates HIV latency and modulates HIV reactivation [ PLoS Pathog, 2022, 18(3):e1010354] PubMed: 35255110
Cytoplasmic SHMT2 drives the progression and metastasis of colorectal cancer by inhibiting β-catenin degradation [ Theranostics, 2021, 11(6):2966-2986] PubMed: 33456583

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.