New-generation oral HIF-PHD inhibitor (IC50 value 591 nM for inhibition of PHD2 in a fluorescence polarization assay) for the treatment of anemia in patients with chronic kidney disease (CKD) by promoting erythropoiesis. FG-4592 (Roxadustat) treatment significantly inhibited tert-Butyl hydroperoxide (TBHP)-induced apoptosis and increases the survival of neuronal PC-12 cells by stabilization of HIF-1α. FG 4592 is also shown to inhibit Fat Mass and Obesity Associated Protein (FTO; IC50 value 9.8 μM).

KEYWORDS: FG-4592 | supplier | PHD inhibitor | Roxadustat | ASP 1517 | FG4592 | ASP1517 | CAS [808118-40-3] | Hypoxia-signaling cascade | PHD (HIF) | Inhibitor | anemia | chronic kidney disease | CKD | erythropoiesis | survival | HIF-1α | Fat | Obesity Associated Protein | FTO