iCRT3

製品コードS8647 バッチS864702

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C23H26N2O2S

分子量 394.53 CAS No. 901751-47-1
Solubility (25°C)* 体外 DMSO 78 mg/mL (197.7 mM)
Ethanol 78 mg/mL (197.7 mM)
Water Insoluble
体内 (毎回新しく調製した物を用意してください)
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.9mg/ml
5% DMSO 95% Corn oil
1.9mg/ml
* <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.

溶剤液(一定の濃度)を調合する

生物活性

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

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HCT116 cells
濃度 25, 50, 75 μM
反応時間 1 days
実験の流れ

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.

動物実験 動物モデル C57BL/6 mice
投薬量 5 mg/kg and 10 mg/kg
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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