CH 223191

Biological Activity

Potent aryl hydrocarbon receptor (AhR) antagonist (IC₅₀ = 30 nM). Exhibits no AhR agonist-like activity (at concentrations up to 100 μM). Inhibits 2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD)-induced AhR-dependent transcription in vitro and reduces TCDD-induced toxicity in vivo. Attenuates Th17 differentiation of naive CD4 T cells and promotes expansion of hematopoietic stem cells in vitro.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. CXCR4 activation maintains a stem cell population in tamoxifen-resistant breast cancer cells through AhR signalling.
   Dubrovska A, Hartung A, Bouchez LC
   Br. J. Cancer, 2012;107(1):43-52.
2. Aryl hydrocarbon receptor antagonists promote the expansion of human hematopoietic stem cells.
   Boitano et al.
   Science, 2010;329:1345
3. Novel compound 2-methyl-2H-pyrazole-3-carboxylic acid (2-methyl-4-o-tolylazo-phenyl)-amide (CH-223191) prevents 2,3,7,8-TCDD-induced toxicity by antagonizing the aryl hydrocarbon receptor.
   Kim et al.
   Mol.Pharmacol., 2006;69:1871
4. Natural agonists for aryl hydrocarbon receptor in culture medium are essential for optimal differentiation of TH17 T cells.
   Veldhoen et al.
   J.Exp.Med., 2009;206:43

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