iCRT3

Catalog No.S8647

iCRT3 Chemical Structure

Molecular Weight(MW): 394.53

iCRT3 is an antagonist of Wnt/β-catenin signaling with an IC50 of 8.2 nM in the Wnt responsive STF16-luc reporter assays.

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Biological Activity

Description iCRT3 is an antagonist of Wnt/β-catenin signaling with an IC50 of 8.2 nM in the Wnt responsive STF16-luc reporter assays.
Targets
Wnt/β-catenin [1]
(in STF16 assay)
8.2 nM
In vitro

iCRT3 is a small molecule inhibitor of the Wnt pathway which binds to β-catenin interfering with its interaction with TCF. iCRT3 significantly reduces the LPS-induced Wnt/β-catenin activity and also inhibits TNF-α production and IκB degradation in a dose-dependent manner. iCRT3 does not influence the transcriptional activity of FOP-Flash luciferase reporter, which harbors mutations in the DNA binding sites for TCF (β-cat response element), showing specificity of the response. It inhibits cytokine production in LPS-stimulated macrophages[1][2].

In vivo Intraperitoneal administration of iCRT3 to C57BL/6 mice, subjected to cecal ligation and puncture-induced sepsis, decreases the plasma levels of proinflammatory cytokines and organ injury markers in a dose-dependent manner. The histological integrity of the lungs is improved with iCRT3 treatment, along with reduced lung collagen deposition and apoptosis. In addition, iCRT3 treatment also decreases the expression of the cytokines, neutrophil chemoattractants, as well as the MPO activity in the lungs of septic mice[2].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: HCT116 cells
  • Concentrations: 25, 50, 75 μM
  • Incubation Time: 1 days
  • Method:

    HCT116 cells were cultured in McCoy's 5A medium supplemented with 10% FBS. Cells were treated with specified concentrations of compounds for 1 d and lysed in 50 μL cell lysis buffer at 75℃ for 10 min.


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • Animal Models: C57BL/6 mice
  • Formulation: 5% DMSO in normal saline
  • Dosages: 5 mg/kg and 10 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (197.7 mM)
Ethanol 78 mg/mL (197.7 mM)
Water 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 394.53
Formula

C23H26N2O2S

CAS No. 901751-47-1
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

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Wnt/beta-catenin Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID