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 50 publications

Metabolic landscape of head and neck squamous cell carcinoma informs a novel kynurenine/Siglec-15 axis in immune escape [ Cancer Commun (Lond), 2024, 10.1002/cac2.12545] PubMed: 38734931
Metabolic landscape of head and neck squamous cell carcinoma informs a novel kynurenine/Siglec-15 axis in immune escape [ Cancer Commun (Lond), 2024, 44(6):670-694] PubMed: 38734931
Bifidobacterium breve-derived indole-3-lactic acid ameliorates colitis-associated tumorigenesis by directing the differentiation of immature colonic macrophages [ Theranostics, 2024, 14(7):2719-2735] PubMed: 38773969
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
Ruthenium drug BOLD-100 regulates BRAFMT colorectal cancer cell apoptosis through AhR/ROS/ATR signaling axis modulation [ Mol Cancer Res, 2024, 10.1158/1541-7786.MCR-24-0151] PubMed: 39083088
Urolithin A-mediated augmentation of intestinal barrier function through elevated secretory mucin synthesis [ Sci Rep, 2024, 14(1):15706] PubMed: 38977770
Benvitimod upregulates filaggrin, involucrin and loricrin expressions via aryl hydrocarbon receptor-OVO-like 1 axis [ Arch Dermatol Res, 2024, 316(8):585] PubMed: 39207509
Endothelial AHR activity prevents lung barrier disruption in viral infection [ Nature, 2023, 621(7980):813-820] PubMed: 37587341
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

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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.