CH 223191

The aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor that up-regulates many xenobiotic metabolizing enzymes, particularly in response to planar aromatic hydrocarbons.¹ CH 223191 is a potent and specific antagonist of AhR that blocks activation by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD, IC₅₀ = 0.03 µM).² It prevents the induction of cytochrome P450 1A1 by TCDD in HepG2 cells and in livers of mice.² Through its effects on AhR, CH 223191 suppresses Th17 cell differentiation both in vitro and in vivo and alters the expression of homeobox transcription factors necessary for the differentiation of embryonic stem cells to cardiomyocytes.^3,4

WARNING This product is not for human or veterinary use.

1. Gu, Y.Z., Hogenesch, J.B., and Bradfield, C.A. The PAS superfamily: Sensors of environmental and developmental signals. Annu. Rev. Pharmacol. Toxicol. 40, 519-561 (2000).

2. Kim, S.H., Henry, E.C., Kim, D.K., et al. 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. Mol. Pharmacol. 69(6), 1871-1878 (2006).

3. Veldhoen, M., Hirota, K., Christensen, J., et al. Natural agonists for aryl hydrocarbon receptor in culture medium are essential for optimal differentiation of Th17 T cells. J. Exp. Med. 206(1), 43-49 (2009).

4. Wang, Q., Chen, J., Ko, C.I., et al. Disruption of aryl hydrocarbon receptor homeostatic levels during embryonic stem cell differentiation alters expression of homeobox transcription factors that control cardiomyogenesis. Environ. Health Perspect. 121(11-12), 1334-1343 (2013).