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Description

A cell-permeable imidazo-pyrazine based compound that acts as a potent and reversible inhibitor of PI4KIIIbeta (IC50 = 5.7 nM). Displays excellent selectivity over PI4KIIIalpha (IC50 = 1.7 µ,M) and several other lipid kinases (IC50 >10 µ,M). Shown to dose-dependently decrease PI4P levels, reduce oxysterol-binding protein (OSBP) localization to replication organelles (ROs) and inhibit cholesterol shuttling to ROs (at 1 µ,M in BGM and HeLaR19 cells transfected with CVB3) at multiplicity of infection (MOI). Exhibits uniformly potent and broad spectrum antienteroviral activity across a wide range of species (EC50 = 4-31 nM) and is inactive against RNA, DNA, and retroviruses.

Structure formula

2-Fluoro-4-(2-methyl-8-(3-(methylsulfonyl)benzylamino)imidazo[1,2-a]pyrazin-3-yl)phenol

Contents

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