Home Metabolism AhR antagonist CH-223191 For research use only.

CH-223191

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

CH-223191 Chemical Structure

CH-223191 Chemical Structure

CAS No. 301326-22-7

Purity & Quality Control

Products often used together with CH-223191

PD98059

CH-223191 and PD98059 abolish TCDD-induced ERK1/2 phosphorylation and cell proliferation in human colon cancer cells.

Xie G, et al. Am J Physiol Gastrointest Liver Physiol. 2012 May 1;302(9):G1006-15.

FICZ

CH223191 is intraperitoneally administered 1 hr before FICZ application to modulate AhR activation.

Zhao C, et al. PLoS Pathog. 2021 Jul 23;17(7):e1009774.

GNF351

CH-223191 and GNF351 are AhR antagonists that completely inhibit the VRCZ-induced transcription of CYP1A1 and COX-2 in HaCaT cells.

Ikeya S, et al. Sci Rep. 2018; 8: 5050.

CH-223191 Related Products

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
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]
Kinase Assay 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 Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot hpol κ / γH2AX 26651356
In Vivo
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]
Animal Research Animal Models Male ICR mice
Dosages 10 mg/kg/day
Administration p.o.

Chemical Information & Solubility

Molecular Weight 333.39 Formula

C19H19N5O
CAS No. 301326-22-7 SDF Download CH-223191 SDF
Smiles CC1=CC=CC=C1N=NC2=CC(=C(C=C2)NC(=O)C3=CC=NN3C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 67 mg/mL ( (200.96 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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