AhR Inhibitor

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AhR Antagonist
AhR Inhibitor

CH-223191 is a synthetic antagonist for the cytosolic aryl hydrocarborn receptor (AhR) transcription factor [1]. AhR is a ligand-dependent transcriptional factor able to sense a wide range of structurally different exogenous and endogenous molecules.

Mode of action:

CH-223191 exerts a ligand-selective antagonism and appears to be more effective on halogenated aromatic hydrocarbons such as the xenobiotic 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), than on polycyclic aromatic hydrocarbons and non-halogenated aromatic hydrocarbons such as FICZ and ITE, respectively [2]. 

Notably, CH-223191 is a pure AhR antagonist that does not stimulate AhR-dependent transcription even at concentrations up to 100 μM [1], unlike other AhR antagonists which display agonist activity at high concentrations. Moreover, CH-223191 is specific for AhR, displaying no affinity for the estrogen receptor, in contrast to other AhR antagonists [1].

InvivoGen's CH-223191 is of high quality, guaranteed free of bacterial contamination, and has been functionally tested on HepG2-Lucia™ AhR and HT29-Lucia™ AhR reporter cells.

Key features of CH-223191:

  • A potent and specific AhR antagonist
  • Ligand-selective antagonist activity
  • Each lot is highly pure (≥95%) and functionally tested

References

  1. Kim, S.H. et al., 2006. 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. 69:1871-78.
  2. Zhao B. et al., 2010. CH223191 is a ligand-selective antagonist of the Ah (Dioxin) receptor. Toxicol. Sci. 117:393-403.

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