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Description

A cell-permeable, hydroxyquinoline HIF Prolyl Hydroxylase (PHD) inhibitor that displays an IC50 = 2 µ,M in a cell-based assay using a reporter produced by fusing HIF-1alpha oxygen degradable domain (ODD) to luciferase. This compound (5 µ,M) is shown to significantly stabilize HIF-1alpha in vitro and upregulate known HIF target genes, Epo and VEGF, in SH-SY5Y human neuroblastoma cell lines. It also exerts a neuroprotective effect (IC50 = 0.25 µ,M in an oxidative stress model using cortical neurons.