AhR Antagonist III, GNF351

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
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).
产品信息
Form  Off-white solid
Molar mass  411.5
Protect from Light  是的
Packaged under inert gas  是的
Purity  ≥98% by HPLC
Solubility  DMSO
Chemical formula  C24H25N7
商店和运输信息
Storage  +2°C to +8°C
Ship  Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Standard Handling