CH-223191

Catalog No.S7711 Batch:S771105

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Technical Data

Formula

C19H19N5O
Molecular Weight 333.39 CAS No. 301326-22-7
Solubility (25°C)* In vitro DMSO 67 mg/mL (200.96 mM)
Ethanol 2 mg/mL (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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM.
Targets
AhR [1]
(in HepG2 cells)
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]

Protocol (from reference)

Kinase Assay:

[1]
  • Luciferase Reporter Gene Assay

    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.

Cell Assay:

[1]
  • Cell lines

    HepG2 cells

  • Concentrations

    30 nM

  • Incubation Time

    1 h

  • Method

    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.
Animal Study:

[1]
  • Animal Models

    Male ICR mice

  • Dosages

    10 mg/kg/day

  • Administration

    p.o.

Customer Product Validation

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's CH-223191 has been cited by 43 publications

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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.