| S1007 |
Roxadustat (FG-4592)
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Roxadustat (FG-4592) is an HIF-α prolyl hydroxylase inhibitor in a cell-free assay, stabilizes HIF-2 and induces EPO production. This compound also potentiates RSL3 induced ferroptosis. Phase 3.
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Immunity, 2025, S1074-7613(25)00139-6
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Cell Stem Cell, 2025, S1934-5909(25)00338-8
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Mol Cell, 2025, 85(15):2973-2987.e6
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| S2919 |
IOX2
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IOX2 (JICL38) is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM in a cell-free assay, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH.
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Cell Rep Med, 2024, 5(2):101400
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Int J Mol Sci, 2024, 26(1)117
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Oncogene, 2022, 41(13):1944-1958
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| S8138 |
Molidustat (BAY 85-3934)
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Molidustat (BAY 85-3934) is a potent hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor with IC50 of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD, respectively. This compound is in Phase 2.
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Nat Cancer, 2024, 10.1038/s43018-024-00761-w
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J Med Chem, 2024, 67(6):4525-4540
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Sci Adv, 2024, 10(35):eadq2366
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| S8443 |
MK-8617
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MK-8617 is an orally active pan-inhibitor of Hypoxia-inducible factor prolyl hydroxylase 1−3 (HIF PHD1−3), inhibiting PHD1, 2, 3 with IC50s of 1.0, 1.0 and 14 nM, respectively.
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FEBS J, 2024, 10.1111/febs.17379
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PeerJ, 2023, 11:e15591
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bioRxiv, 2021, 10.1101/2021.08.26.456853
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| S8171 |
Daprodustat (GSK1278863)
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Daprodustat (GSK1278863) is an orally administered hypoxia-inducible factor-prolyl hydroxylase (HIF-PH) inhibitor. Phase 2.
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Emerg Microbes Infect, 2025, 2563067
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Sci Adv, 2024, 10(35):eadq2366
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Cell Rep, 2021, 35(3):109020
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| S7979 |
FG-2216
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FG-2216 is a potent, and orally active HIF prolyl 4-hydroxylase inhibitor with IC50 of 3.9 μM for PHD2. Phase 2.
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Nat Commun, 2024, 15(1):7483
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J Photochem Photobiol B, 2020, 210:111980
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FASEB J, 2020, 34(2):2344-2358
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| S6490 |
Vadadustat
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Vadadustat (AKB-6548, B-506, PG-1016548) is a novel, titratable, oral HIF-PH inhibitor.
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Drug Test Anal, 2020, 10.1002/dta.2917
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| S7483 |
DMOG (Dimethyloxallyl Glycine)
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DMOG (Dimethyloxalylglycine) is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolylhydroxylase, leading to stabilisation and accumulation of HIF-1α protein in the nucleus. DMOG enhances autophagy.Solutions are unstable and should be fresh-prepared.
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Nucleic Acids Res, 2025, 53(14)gkaf669
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Cell Commun Signal, 2025, 23(1):364
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Front Pharmacol, 2025, 16:1502269
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| S5804 |
N-Acetylcysteine amide (NACA)
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N-acetylcysteine amide is a membrane penetrating antioxidant with anti-inflamatory activity through regulation of activation of NF-κB and HIF-1α as well as modulation of ROS.
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Pharmacol Res, 2025, 219:107902
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iScience, 2025, 28(3):111964
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Pharmacol Res Perspect, 2025, 13(3):e70120
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