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FG-4592
- Roxadustat - ASP 1517
- Soluble in 0.1N NaOH(aq) and DMSO
- MF: C19H16N2O5
- MW: 352.34
Description
FG-4592 (Roxadustat) is a potent and orally available HIF-PHD inhibitor with IC50 value 591 nM for PHD2. By blocking PHD-mediated degradation of HIF-1α and HIF-2α, it allows stabilized HIF to translocate to the nucleus, binding hypoxia-response elements to activate genes regulating iron metabolism and cell survival.
PHD pharmacology is relevant to obesity, anemia, chronic kidney disease. As a high-quality chemical probe, FG-4592 supports robust mechanistic studies of PHD activity across biochemical, cellular, and disease-model assays.
Key Features
- PHD inhibitor
- IC50: 591 nM
- Chemical probe for PHD pathway studies
- Blocks PHD-mediated degradation of HIF-1α and HIF-2α
Applications
- PHD pharmacology and target-validation studies
- PHD pathway and signaling assays
- Disease-model research related to obesity, anemia
- DNA repair, replication or genome-stability research
More Information
| Parent CAS No. | 808118-40-3 |
|---|---|
| Chemical Name | 2-(4-Hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxamido)acetic acid |
| SMILES | C(O)(=O)CNC(C1=C(O)C2=C(C(C)=N1)C=C(OC1=CC=CC=C1)C=C2)=O |
| MFCD | MFCD21609264 |
| InChi | InChI=1S/C19H16N2O5/c1-11-15-9-13(26-12-5-3-2-4-6-12)7-8-14(15)18(24)17(21-11)19(25)20-10-16(22)23/h2-9,24H,10H2,1H3,(H,20,25)(H,22,23) |
| InChiKey | YOZBGTLTNGAVFU-UHFFFAOYSA-N |
| CID | 11256664 |
| Short Description | PHD inhibitor |
References
- Y Lei et al. Affinity-Based Fluorescence Polarization Assay for High-Throughput Screening of Prolyl Hydroxylase 2 Inhibitors. ACS Med Chem Lett. 2015 Nov 9;6(12):1236-40.
- W Aik et al. Structural basis for inhibition of the fat mass and obesity associated protein (FTO). J Med Chem. 2013 May 9;56(9):3680-8.
- K Wu et al. Stabilization of HIF-1α by FG-4592 promotes functional recovery and neural protection in experimental spinal cord injury. Brain Res. 2016 Feb 1;1632:19-26.
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