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  • 182707 - AhR Antagonist III, GNF351 - Calbiochem

182707 Sigma-Aldrich

AhR Antagonist III, GNF351 - Calbiochem

AhR Antagonist III, GNF351, is a cell-permeable, high-affinity aryl hydrocarbon receptor (AhR) antagonist (IC50 = 62 nM in mouse liver cytosol expressing humanized AhR).

Synonym: AhR Antagonist III, GNF351 - Calbiochem, N-(2-(3H-Indol-3-yl)ethyl)-9-isopropyl-2-(5-methyl-3-pyridyl)-7H-purin-6-amine, N-(2-(1H-Indol-3-yl)ethyl)-9-isopropyl-2-(5-methylpyridin-3-yl)-9H-purin-6-amine

  • Empirical Formula (Hill Notation) C24H25N7

  • Molecular Weight 411.50



Related Categories Antagonists, Cell Biology, Cell Signaling and Neuroscience, Endothelins, Peptides and Proteins,
Quality Level   100
assay   ≥98% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   +2C to +8C
color   off-white
solubility   DMSO: 50 mg/mL
shipped in   wet ice


General description

A cell-permeable purine compound that acts as a high-affinity aryl hydrocarbon receptor (AhR) antagonist (IC50 = 62 nM in mouse liver cytosol expressing humanized AhR) and lacks any agonist activity even at higher doses. Reportedly binds with high affinity to the ligand-binding pocket of AhR and blocks the binding of an array of exogenous and endogenous ligands. Shown to non-covalently interact with Ser317, His291, and Ser365 in human and with Ser311, His285, and Ser359 in mouse AhR. Represses AhR transcriptional activity via the dioxin response element (DRE)-dependent and independent mediated responses in human and mouse cells (IC50 = 8.5 nM in HepG2 40/6 cells).


10 mg in Glass bottle

Packaged under inert gas


Toxicity: Standard Handling (A)

Other Notes

Smith, K.J., et al. 2011. J. Pharmacol. Exp. Ther. 338, 318.

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