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Formula | C19H19N5O |
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Molecular Weight | 333.39 | CAS No. | 301326-22-7 | |
Solubility (25°C)* | In vitro | DMSO | 67 mg/mL (200.96 mM) | |
Ethanol | 5 mg/mL (14.99 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | 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] |
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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] |
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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 |
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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.
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