IOX2 is a potent, selective and cell permeable inhibitor of hypoxia inducible factor 1α (HIF1α) prolyl hydroxylase-2 (PHD2). It inhibits PHD2 with an IC₅₀ ~21 nM, and exhibits over 100-fold selectivity against JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH. IOX2 is active in cells, inhibiting HIF-1α hydroxylation in RCC4 cells at 50 μM.

How to Use:

•  In vitro:  IOX2 was usually used at 10-50µM final concentration in vitro
•  In vivo: n/a

Reference:

1. 1. Murray JK, et al. Dipeptidyl-quinolone derivatives inhibit hypoxia inducible factor-1α prolyl hydroxylases-1, -2, and -3 with altered selectivity. (2010) J Comb Chem. 12(5):676-86.

1. 2. SGC website: http://www.thesgc.org/scientists/chemical_probes/IOX2

1. 3. Tian YM, et al. Differential sensitivity of hypoxia inducible factor hydroxylation sites to hypoxia and hydroxylase inhibitors. (2011) J Biol Chem. 286(15):13041-51.