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182707

Sigma-Aldrich

AhR Antagonist III, GNF351

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).

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Synonym(s):
AhR Antagonist III, GNF351, 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

Quality Level

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 50 mg/mL

shipped in

wet ice

storage temp.

2-8°C

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form

solid

form

solid

form

solid

form

solid

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

assay

≥98% (HPLC)

assay

≥99% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

solubility

DMSO: 50 mg/mL

solubility

DMSO: 50 mg/mL

solubility

DMSO: 25 mg/mL, water: 25 mg/mL

solubility

DMSO: 50 mg/mL, clear, colorless

shipped in

wet ice

shipped in

ambient

shipped in

ambient

shipped in

ambient

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).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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