Home Stem Cells & Wnt Wnt/beta-catenin antagonist iCRT3 For research use only.

iCRT3

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

iCRT3 Chemical Structure

iCRT3 Chemical Structure

CAS: 901751-47-1

Selleck's iCRT3 has been cited by 8 publications

Purity & Quality Control

Batch: Purity: 99.6%
99.6

iCRT3 Related Products

Signaling Pathway

Wnt/beta-catenin Signaling Pathways

Wnt/beta-catenin Signaling Pathway

Choose Selective Wnt/beta-catenin Inhibitors

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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models C57BL/6 mice
Dosages 5 mg/kg and 10 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 394.53 Formula

C23H26N2O2S
CAS No. 901751-47-1 SDF Download iCRT3 SDF
Smiles CCC1=CC=C(C=C1)C2=NC(=C(O2)C)CSCC(=O)NCCC3=CC=CC=C3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 78 mg/mL ( (197.7 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 78 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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