iCRT3

Catalog No.S8647 Batch:S864703

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Technical Data

Formula

C23H26N2O2S
Molecular Weight 394.53 CAS No. 901751-47-1
Solubility (25°C)* In vitro DMSO 78 mg/mL (197.7 mM)
Ethanol 78 mg/mL (197.7 mM)
Water 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 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 (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[2]
  • Animal Models

    C57BL/6 mice

  • Dosages

    5 mg/kg and 10 mg/kg

  • Administration

    i.p.

Selleck's iCRT3 has been cited by 8 publications

Functional analysis of a first hindlimb positioning enhancer via Gdf11 expression [ Front Cell Dev Biol, 2024, 12:1302141] PubMed: 38559809
CRIP1 suppresses BBOX1-mediated carnitine metabolism to promote stemness in hepatocellular carcinoma [ EMBO J, 2022, 41(15):e110218] PubMed: 35775648
CDK7/12/13 inhibition targets an oscillating leukemia stem cell network and synergizes with venetoclax in acute myeloid leukemia [ EMBO Mol Med, 2022, e14990] PubMed: 35253392
STRAP is a Critical Mediator of APC Mutation-Induced Intestinal Tumorigenesis through a Feed-Forward Mechanism [ Gastroenterology, 2021, S0016-5085(21)03489-2] PubMed: 34520730
CST1 Promoted Gastric Cancer Migration and Invasion Through Activating Wnt Pathway [ Cancer Manag Res, 2021, 13:1901-1907] PubMed: 33658852
Efficient and robust induction of retinal pigment epithelium cells by tankyrase inhibition regardless of the differentiation propensity of human induced pluripotent stem cells [ Biochem Biophys Res Commun, 2021, 552:66-72] PubMed: 33743349
Ribosomal S6 protein kinase 4 promotes radioresistance in esophageal squamous cell carcinoma [ J Clin Invest, 2020, 130(8):4301-4319] PubMed: 32396532
Conditional cell reprogramming involves non-canonical β-catenin activation and mTOR-mediated inactivation of Akt [Suprynowicz FA PLoS One, 2017, 12(7):e0180897] PubMed: 28700668

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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.