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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C19H19N5O |
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分子量 | 333.39 | CAS No. | 301326-22-7 | |
Solubility (25°C)* | 体外 | DMSO | 67 mg/mL (200.96 mM) | |
Ethanol | 2 mg/mL warmed with 50ºC water bath (5.99 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. |
製品説明 | CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM. |
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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] |
キナーゼアッセイ | Luciferase Reporter Gene Assay | |
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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. |
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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. |
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]
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。