Selective HIF-1 dimerization inhibitor. Blocks protein-protein interaction of recombinant HIF-1α, but not HIF-2α, with HIF-1β (IC50 = 1.3 μM). Inhibits hypoxia-induced HIF-1 activity, and decreases VEGF and CAIX expression in osteosarcoma and breast cancer cells in vitro. Also reduces tubularization of hypoxic HUVECs.

The dimethyl ester of N-oxalyl-d-phenylalanine (NOFD), a specific HIF asparaginyl hydroxylase (FIH) inhibitor with Ki of 83 uM.

Molidustat (BAY 85-3934) is an orally active small molecule inhibitor of hypoxia inducible factor prolyl hydroxylase (HIF-PH) with IC50 of 480 nM, 280 nM and 450 nM for PHD1, PHD2, and PHD3, respectively.