HIF Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
S8138	Molidustat (BAY 85-3934)	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.	eLife, 2025, RP107419 Nat Cancer, 2024, 10.1038/s43018-024-00761-w Science Advances, 2024, eadq2366
S8441	CAY10585 (LW 6)	CAY10585 (LW 6) is a hypoxia-inducible factor 1(HIF) inhibitor which potently inhibits HIF-1α accumulation by degrading HIF-1α without affecting the HIF-1a mRNA levels during hypoxia. LW6 inhibits HIF and MDH2 expression with IC50 values of 4.4 and 6.3 μM, respectively.	Nat Commun, 2025, 16(1):4681 EMBO Mol Med, 2025, 17(6):1289-1324 Adv Biol Regul, 2025, 96:101098
S8352	PT2385	PT2385 is a HIF-2α antagonist with luciferase EC50 of 27 nM and no significant off-target activity.	Cell Stem Cell, 2025, S1934-5909(25)00338-8 Mater Today Bio, 2025, 35:102450 Materials Today Bio, 2025, 102450
S8771	IDF-11774	IDF-11774 is a hypoxia-inducible factor-1 (HIF-1) inhibitor. It reduces the HRE-luciferase activity of HIF-1α (IC50 = 3.65 μM) and blocks HIF-1α accumulation under hypoxia in HCT116 human colon cancer cells.	Elife, 2025, 13RP101912 Cell Death Discovery, 2025, 380 Cell Death Discov, 2025, 11(1):380
S7979	FG-2216	FG-2216 is a potent, and orally active HIF prolyl 4-hydroxylase inhibitor with IC50 of 3.9 μM for PHD2. Phase 2.	Nat Commun, 2024, 15(1):7483 J Photochem Photobiol B, 2020, 210:111980 FASEB J, 2020, 34(2):2344-2358
S8171	Daprodustat (GSK1278863)	Daprodustat (GSK1278863) is an orally administered hypoxia-inducible factor-prolyl hydroxylase (HIF-PH) inhibitor. Phase 2.	Emerg Microbes Infect, 2025, 2563067 Emerging Microbes & Infections, 2025, 2563067 Biological & Pharmaceutical Bulletin, 2025, 1794-1802
S8443	MK-8617	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.	FEBS J, 2024, 10.1111/febs.17379 PeerJ, 2023, 11:e15591 bioRxiv, 2021, 10.1101/2021.08.26.456853
S6490	Vadadustat	Vadadustat (AKB-6548, B-506, PG-1016548) is a novel, titratable, oral HIF-PH inhibitor.	Proceedings of the National Academy of Sciences, 2022, e2210779119 Drug Test Anal, 2020, 10.1002/dta.2917
S9656	Enarodustat (JTZ-951)	Enarodustat (JTZ-951) is a potent and orally active HIF prolyl hydroxylase inhibitor with IC50 of 0.22 μM for PHD2 and EC50 of 5.7 μM for EPO release from Hep3B cells. It has the potential for the treatment of renal anemia.	Molecular Medicine, May 1, 2023, 61 Molecular Medicine, 2023, 61 Mol Med, 2023, 29(1):61
S6684	IOX4	IOX4 is a potent and selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with IC50 of 1.6 nM. This compound induces HIFα in various mouse tissues and human cell lines.	The Journal of Immunology, July 15, 2023, 261-273 The Journal of Immunology, July 15 2023, 261-273 Cell Host Microbe, 2025, 33(1):71-88.e9
S6400	Glucosamine	Glucosamine (2-amino-2-deoxy-D-glucose) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids. It is commonly used as a treatment for osteoarthritis. This compound treatment selectively downregulates HIF-1α at the protein level in YD-8 cells via interference of production of the citric acid cycle metabolites.	Cell Death Dis, 2020, 11(7):503 Cell Death & Disease, 2020, 503
S2937	SYP-5	SYP-5 is an inhibitor of Hypoxia-inducible factor-1 (HIF-1) that suppresses tumor cell migration and invasion, as well as tumor angiogenesis.	Chemico-Biological Interactions, 2023, 110262 Chem Biol Interact, 2022, 369:110262
S0729	TP0463518	TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with Ki of 5.3 nM for human PHD2. This compound inhibits human PHD1, human PHD3 and monkey PHD2 with IC50 of 18 nM, 63 nM and 22 nM, respectively.
S9699	Desidustat	Desidustat (ZYAN1, ZYAN1-1001), an antianaemic drug candidate, is an orally active hypoxia-inducible factor (HIF) prolyl hydroxylase (PHD) inhibitor (HIF-PHI) that stimulates erythropoiesis.
S8617	Acriflavine	Acriflavine is a HIF-1 dimerization inhibitor and have potent inhibitory effects on tumor growth and vascularization. It is used as fluorescent dye for labeling high molecular weight RNA.
E2168	PHD-1-IN-1	PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC50 of 0.034 μM
E1661	Adaptaquin	Adaptaquin is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PHD2), with an IC50 of 2 μM. This compound also inhibits lipid peroxidation and maintains mitochondrial function.
E1712	FM19G11	FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC50 of 80 nM in HeLa cells.
E7505	GN44028	GN44028 is a potent and orally active inhibitor of hypoxia inducible factor (HIF)-1α, with an IC50 of 14 nM. This compound inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, protein accumulation, or HIF-1α/HIF-1β heterodimerization. It also weakens the tumor‐initiating capability and improves the anticancer effects in colorectal cancer treatment.
E1618	TC-S 7009	TC-S 7009 is a potent and selective inhibitor of HIF-2α with a Kd value of 81 nM. This compound is more selective for HIF-2α than HIF-1α. It disrupts HIF-2α heterodimerization, decreases DNA-binding activity, and reduces HIF-2α target gene expression.
S7483	DMOG (Dimethyloxallyl Glycine)	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.	Nucleic Acids Res, 2025, 53(14)gkaf669 Cell Commun Signal, 2025, 23(1):364 Front Pharmacol, 2025, 16:1502269
S7958	YC-1 (Lificiguat)	Lificiguat (YC-1) is an nitric oxide (NO)-independent activator of soluble guanylyl cyclase(sGC) and an inhibitor of Hypoxia-inducible factor-1alpha (HIF-1alpha).	J Transl Med, 2024, 22(1):248 J Transl Med, 2024, 22(1):1003 Hepatol Commun, 2024, 8(1)e0350
S5804	N-Acetylcysteine amide (NACA)	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.	Pharmacol Res, 2025, 219:107902 iScience, 2025, 28(3):111964 Pharmacol Res Perspect, 2025, 13(3):e70120
S2410	Paeoniflorin (NSC 178886)	Paeoniflorin (NSC 178886, Peoniflorin), a herbal constituent extracted from the root of Paeonia albiflora Pall, reduces COX-2 expression. It alleviates liver fibrosis by inhibiting HIF-1α through mTOR-dependent pathway.	Bioengineered, May 2022, 13622-13631 Drug Design, Development and Therapy, August 2017, 2481-2491 Immun Inflamm Dis, 2026, 14(1):e70324
S8449	VH298	VH298 is a potent VHL (Von Hippel-Lindau, the E3 ligase) inhibitor that stabilizes HIF-α. This compound blocks the VHL:HIF-α interaction with Kd of 90 nM in isothermal titration calorimetry (ITC) and 80 nM in a competitive fluorescence polarization assay. It can be used in PROTAC technology.	Cell Rep, 2025, 44(6):115800 Cell Commun Signal, 2025, 23(1):364 Eur J Med Chem, 2024, 268:116202
E0807	NHWD-870	NHWD-870 inhibits CSF1 expression through suppressing BRD4 and its target HIF1α.
S3589	Bendazol	Bendazol (2-Benzylbenzimidazole, Dibazol, Dibazole, Bendazole, Tromasedan) is a hypotensive drug that enhances NO synthase activity in renal glomeruli and collecting tubules. This compound inhibits the progression of form-deprivation myopia (FDM) and suppresses the upregulation of HIF-1α.