IOX4

IOX4 is a potent inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PH2; IC₅₀ = 1.6 nM).¹ It displays >1,000-fold selectivity for PHD2 over other 2OG-dependent dioxygenases, including JMJD isoforms, FBXL11, JARID1C, BBOX1, FIH, and FTO. IOX4 is active in vivo, inhibiting prolyl hydroxylation and increasing HIF-1α levels in cells (IC₅₀ values range from 5.6 to 11.7 µM) and inducing HIF-1α and HIF-2α expression in mice.¹ The induction of HIF expression in mice occurs in the brain as well as in the liver, kidney, and heart, indicating that IOX4 penetrates the blood-brain barrier.¹

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1. Chan, M.C., Atasoylu, O., Hodson, E., et al. Potent and selective triazole-based inhibitors of the hypoxia-inducible factor prolyl-hydroxylases with activity in the murine brain. PLoS One 10(7), e0132004 (2015).