CH-223191

製品コードS7711 バッチS771106

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₉H₁₉N₅O

分子量

333.39

CAS No.

301326-22-7

Solubility (25°C)*

体外

DMSO

67 mg/mL (200.96 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

0.85mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 17 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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	CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM.
in vitro	CH-223191 blocks TCDD-mediated nuclear translocation and DNA binding of AhR, and also causes the inhibition of TCDD-induced cytochrome P450 enzyme activity. ^[1] In human glioblastoma cells, CH-223191downregulates the TGF-beta/Smad pathway, and reduces clonogenic survival and invasiveness. ^[2] In SK-N-SH human-derived neuronal cells, CH223191 counteracts the TCDD-induced suppression of neuronal acetylcholinesterase expression. ^[3] In endothelial cells, CH-223191 potentiates ICAM-1 expression and prevents RelB nuclear translocation. ^[4]
in vivo	CH-223191 (10 mg/kg/day, p.o.) potently prevents TCDD-caused cytochrome P450 induction, liver toxicity, and wasting syndrome in mice. ^[1]

製品説明

CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM.

in vitro

CH-223191 blocks TCDD-mediated nuclear translocation and DNA binding of AhR, and also causes the inhibition of TCDD-induced cytochrome P450 enzyme activity. ^[1]

In human glioblastoma cells, CH-223191downregulates the TGF-beta/Smad pathway, and reduces clonogenic survival and invasiveness. ^[2]

In SK-N-SH human-derived neuronal cells, CH223191 counteracts the TCDD-induced suppression of neuronal acetylcholinesterase expression. ^[3]

In endothelial cells, CH-223191 potentiates ICAM-1 expression and prevents RelB nuclear translocation. ^[4]

in vivo

CH-223191 (10 mg/kg/day, p.o.) potently prevents TCDD-caused cytochrome P450 induction, liver toxicity, and wasting syndrome in mice. ^[1]

プロトコル(参考用のみ)

キナーゼアッセイ	Luciferase Reporter Gene Assay
キナーゼアッセイ	The cells are lysed with lysis buffer (20 mM Tris-HCl, pH 7.8, 1% Triton X-100, 150 mM NaCl, and 2 mM dithiothreitol). The cell lysate is mixed with luciferase activity assay reagent and luminescence produced for 5 s is measured using a luminometer.
細胞アッセイ	細胞株	HepG2 cells
	濃度	30 nM
	反応時間	1 h
	実験の流れ	HepG2 cells were treated with the various concentrations of CH-223191 or flavone for 1 h and then with 3 nM TCDD for 24 h, and then luciferase activity was assayed.
動物実験	動物モデル	Male ICR mice
	投薬量	10 mg/kg/day
	投与方法	p.o.

参考

[4] de Souza AR, et al. Toxicol Sci. 2014, 140(1), 204-223.

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カスタマーフィードバック

: Data from [Data independently produced by , , J Biomed Nanotechnol, 2018, 14(12):2172-2184]

: Data from [Data independently produced by , , Oncol Lett, 2018, 16(3):3849-3857]

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：

Sustained AhR activity programs memory fate of early effector CD8+ T cells [ Proc Natl Acad Sci U S A, 2024, 121(11):e2317658121]	PubMed: 38437537
Mechanical confinement promotes heat resistance of hepatocellular carcinoma via SP1/IL4I1/AHR axis [ Cell Rep Med, 2023, 4(8):101128]	PubMed: 37478857
Macrophages facilitate tumor cell PD-L1 expression via an IL-1β-centered loop to attenuate immune checkpoint blockade [ MedComm (2020), 2023, 4(2):e242]	PubMed: 37009412
Macrophages facilitate tumor cell PD-L1 expression via an IL-1β-centered loop to attenuate immune checkpoint blockade [ MedComm (2020), 2023, 4(2):e242]	PubMed: 37009412
Aryl hydrocarbon receptor is a proviral host factor and a candidate pan-SARS-CoV-2 therapeutic target [ Sci Adv, 2023, 9(22):eadf0211]	PubMed: 37256962
Unraveling the differential impact of PAHs and dioxin-like compounds on AKR1C3 reveals the EGFR extracellular domain as a critical determinant of the AHR response [ Environ Int, 2022, 158:106989]	PubMed: 34991250
The AhR-SRC axis as a therapeutic vulnerability in BRAFi-resistant melanoma [ EMBO Mol Med, 2022, 14(12):e15677]	PubMed: 36305167
Porphyromonas gingivalis infection promotes inflammation via inhibition of the AhR signalling pathway in periodontitis [ Cell Prolif, 2022, e13364.]	PubMed: 36446468
Expansion of Human Megakaryocyte-Lineage Progeny via Aryl Hydrocarbon Receptor Antagonism with CH223191 [ Stem Cell Rev Rep, 2022, 10.1007/s12015-022-10386-0]	PubMed: 35687264
MBL Binding with AhR Controls Th17 Immunity in Silicosis-Associated Lung Inflammation and Fibrosis [ J Inflamm Res, 2022, 15:4315-4329]	PubMed: 35923908

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。