Product Overview
IOX2 is a novel and potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM in a cell-free assay, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH. The hypoxia inducible factor (HIF) system is related to the signaling of low oxygen (hypoxia) in animals. The levels of HIF-α isoforms are controlled by an oxygen-dependent manner by the activity of the HIF prolyl-hydroxylases (PHD or EGLN enzymes), which are Fe(II) and 2-oxoglutarate (2OG) dependent oxygenases. IOX2 inhibits HIF-1α hydroxylation in RCC4 cells at 50 μM.