HIF

Choose Selective HIF Inhibitors

HIF Signaling Pathway Map

HIF Signaling Pathways

HIF Products

  • All (32)
  • HIF Inhibitors (16)
  • HIF Antibodies (1)
  • HIF Activators (2)
  • HIF Antagonists (2)
  • HIF Agonists (1)
  • HIF Modulators (10)
  • New HIF Products
Catalog No. Product Name Information Product Use Citations Product Validations
S0729 TP0463518 TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with Ki of 5.3 nM for human PHD2. TP0463518 inhibits human PHD1, human PHD3 and monkey PHD2 with IC50 of 18 nM, 63 nM and 22 nM, respectively.
S1233 2-Methoxyestradiol (2-MeOE2) 2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines. Phase 2.
Cell Death Differ, 2021, 10.1038/s41418-021-00885-x
Cancers (Basel), 2021, 13(20)5232
Cell Death Discov, 2021, 7(1):242
S2410 Paeoniflorin (NSC 178886) Paeoniflorin (NSC 178886) is a herbal constituent extracted from the root of Paeonia albiflora Pall. Paeoniflorin reduces COX-2 expression. Paeoniflorin alleviates liver fibrosis by inhibiting HIF-1α through mTOR-dependent pathway.
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Immunopharmacol Immunotoxicol, 2021, 1-9
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.
S3233 Emetine hydrochloride Emetine hydrochloride (NSC 33669), a principal alkaloid extracted from the root of ipecac clinically used as an emetic and antiprotozoal drug, reduces HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α), PDK1, RhoA, Rho-kinases (ROCK1 and ROCK2) and BRD4. Emetine hydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect.
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. Glucosamine(GS) 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
S6684 IOX4 IOX4 is a potent and selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with IC50 of 1.6 nM. IOX4 induces HIFα in various mouse tissues and human cell lines.
S7309 BAY 87-2243 BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. BAY 87-2243 inhibits mitochondrial complex I activity, thus triggering a mitophagy-dependent ROS increase leading to necroptosis and ferroptosis. BAY 87-2243 exerts antitumor activity. Phase 1.
Theranostics, 2021, 11(1):209-221
Cancers (Basel), 2021, 13(12)2883
Cell Death Dis, 2021, 13(1):1
S7612 PX-478 2HCl PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. PX-478 2HCl induces apoptosis and has anti-tumor activity. Phase 1.
Proc Natl Acad Sci U S A, 2021, 118(15)e2101080118
Front Immunol, 2021, 12:753092
Aging (Albany NY), 2021, 13(7):10431-10449
S7946 KC7F2 KC7F2 is a selective HIF-1α translation inhibitor with IC50 of 20 μM in a cell-based assay.
Immunity, 2021, S1074-7613(21)00115-1
Aging (Albany NY), 2021, 13(17):21547-21570
Exp Cell Res, 2021, S0014-4827(21)00262-7
S7958 Lificiguat (YC-1) 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).
Mol Ther Nucleic Acids, 2021, 23:1078-1092
Front Cell Dev Biol, 2021, 9:671081
J Immunol Res, 2021, 2021:8887437
S8441 LW 6 LW 6 (CAY10585, AC1-001) 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.
Bioengineered, 2021, 10.1080/21655979.2021.2002499
Ann Rheum Dis, 2020, 79(1):112-122
Oncol Rep, 2020, 44(4):1627-1637
S8449 VH298 VH298 is a potent VHL (Von Hippel-Lindau, the E3 ligase) inhibitor that stabilizes HIF-α. VH298 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. VH-298 can be used in PROTAC technology.
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.
Biochem Biophys Res Commun, 2021, 572:72-79
Basic & Clinical Medicine, 2020, 40(9): 1212-1217
Basic & Clinical Medicine, 2020, 40-9
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. Enarodustat has the potential for the treatment of renal anemia.
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.
A5251 PHD1/prolyl hydroxylase Rabbit Recombinant mAb PHD1/prolyl hydroxylase Rabbit Recombinant mAb detects endogenous level of total PHD1/prolyl hydroxylase.
S3589New Bendazol Bendazol (2-Benzylbenzimidazole, Dibazol, Dibazole, Bendazole, Tromasedan) is a hypotensive drug that enhances NO synthase activity in renal glomeruli and collecting tubules. Bendazol inhibits the progression of form-deprivation myopia (FDM) and suppresses the upregulation of HIF-1α.
S5742 Deferoxamine mesylate (Ba 33112) Deferoxamine mesylate (Ba 33112, Desferrioxamine B, DFOM, NSC 644468) is the mesylate salt of Deferoxamine, which forms iron complexes and is used as a chelating agent. Deferoxamine is a ferroptosis inhibitor that stabilizes HIF-1α expression and improves HIF-1α transactivity in hypoxic and hyperglycemic states in vitro. Deferoxamine decreases beta-amyloid (Aβ) deposition and induces autophagy.
Nat Immunol, 2021, 22(9):1107-1117
Nat Commun, 2021, 12(1):647
CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
S8351 PT2399 PT2399 is a potent and orally available antagonist of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β.
S8352 PT2385 PT2385 is a HIF-2α antagonist with luciferase EC50 of 27 nM and no significant off-target activity.
Lab Invest, 2021, 10.1038/s41374-021-00703-5
S1232 M1001 M1001 is a weak agonist of hypoxia-inducible factor-2α (HIF-2α) that binds to the HIF-2α PAS-B domain with Kd of 667 nM.
S1007 Roxadustat (FG-4592) Roxadustat (FG-4592) is an HIF-α prolyl hydroxylase inhibitor in a cell-free assay, stabilizes HIF-2 and induces EPO production. Roxadustat potentiates RSL3 induced ferroptosis. Phase 3.
Cell Rep, 2021, 35(3):109020
JCI Insight, 2021, 6(18)e133690
Cells, 2021, 10(6)1425
S2431 TMTD (Tetramethylthiuram disulfide) TMTD (Tetramethylthiuram disulfide) can reduce the growth performance of chickens through decreasing liver index, whereas increasing kidney, cardiac, and spleen index, and induces tibial dyschondrolplasia (TD) by changing the expressions of VEGF, HIF-1α and WNT4. TMTD (Tetramethylthiuram disulfide) is widely used in rubber processing as an ultra accelerator for low-temperature cures and in agriculture as an important pesticide.
S2919 IOX2 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.
J Biol Chem, 2021, S0021-9258(21)00710-9
J Proteomics, 2020, 211:103558
Cell Rep, 2019, 29(10):3009-3018
S5804 N-Acetylcysteine amide 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.
Nat Commun, 2021, 12(1):647
Int J Biochem Cell Biol, 2020, 121:105703
Pancreatology, 2019, 19(2):258-265
S6490 Vadadustat Vadadustat (AKB-6548, B-506, PG-1016548) is a novel, titratable, oral HIF-PH inhibitor.
Drug Test Anal, 2020, 10.1002/dta.2917
S7483 DMOG 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.
Cells, 2021, 10(6)1359
Aging (Albany NY), 2021, 13(8):11705-11726
Cell Prolif, 2021, e13158
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.
FASEB J, 2020, 34(2):2344-2358
J Photochem Photobiol B, 2020, 210:111980
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. Phase 2.
Cell Rep, 2021, 35(3):109020
J Bone Miner Res, 2021, 10.1002/jbmr.4272
Front Immunol, 2021, 12:678354
S8171 Daprodustat (GSK1278863) Daprodustat (GSK1278863) is an orally administered hypoxia-inducible factor-prolyl hydroxylase (HIF-PH) inhibitor. Phase 2.
Cell Rep, 2021, 35(3):109020
FASEB J, 2020, 34(2):2344-2358
Cancer Res, 2019, 79(10):2564-2579
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.
bioRxiv, 2021, 10.1101/2021.08.26.456853
FASEB J, 2020, 34(2):2344-2358
FASEB J, 2019, 33(11):12630-12643
S0729 TP0463518 TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with Ki of 5.3 nM for human PHD2. TP0463518 inhibits human PHD1, human PHD3 and monkey PHD2 with IC50 of 18 nM, 63 nM and 22 nM, respectively.
S1233 2-Methoxyestradiol (2-MeOE2) 2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines. Phase 2.
Cell Death Differ, 2021, 10.1038/s41418-021-00885-x
Cancers (Basel), 2021, 13(20)5232
Cell Death Discov, 2021, 7(1):242
S2410 Paeoniflorin (NSC 178886) Paeoniflorin (NSC 178886) is a herbal constituent extracted from the root of Paeonia albiflora Pall. Paeoniflorin reduces COX-2 expression. Paeoniflorin alleviates liver fibrosis by inhibiting HIF-1α through mTOR-dependent pathway.
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Immunopharmacol Immunotoxicol, 2021, 1-9
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.
S3233 Emetine hydrochloride Emetine hydrochloride (NSC 33669), a principal alkaloid extracted from the root of ipecac clinically used as an emetic and antiprotozoal drug, reduces HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α), PDK1, RhoA, Rho-kinases (ROCK1 and ROCK2) and BRD4. Emetine hydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect.
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. Glucosamine(GS) 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
S6684 IOX4 IOX4 is a potent and selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with IC50 of 1.6 nM. IOX4 induces HIFα in various mouse tissues and human cell lines.
S7309 BAY 87-2243 BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. BAY 87-2243 inhibits mitochondrial complex I activity, thus triggering a mitophagy-dependent ROS increase leading to necroptosis and ferroptosis. BAY 87-2243 exerts antitumor activity. Phase 1.
Theranostics, 2021, 11(1):209-221
Cancers (Basel), 2021, 13(12)2883
Cell Death Dis, 2021, 13(1):1
S7612 PX-478 2HCl PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. PX-478 2HCl induces apoptosis and has anti-tumor activity. Phase 1.
Proc Natl Acad Sci U S A, 2021, 118(15)e2101080118
Front Immunol, 2021, 12:753092
Aging (Albany NY), 2021, 13(7):10431-10449
S7946 KC7F2 KC7F2 is a selective HIF-1α translation inhibitor with IC50 of 20 μM in a cell-based assay.
Immunity, 2021, S1074-7613(21)00115-1
Aging (Albany NY), 2021, 13(17):21547-21570
Exp Cell Res, 2021, S0014-4827(21)00262-7
S7958 Lificiguat (YC-1) 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).
Mol Ther Nucleic Acids, 2021, 23:1078-1092
Front Cell Dev Biol, 2021, 9:671081
J Immunol Res, 2021, 2021:8887437
S8441 LW 6 LW 6 (CAY10585, AC1-001) 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.
Bioengineered, 2021, 10.1080/21655979.2021.2002499
Ann Rheum Dis, 2020, 79(1):112-122
Oncol Rep, 2020, 44(4):1627-1637
S8449 VH298 VH298 is a potent VHL (Von Hippel-Lindau, the E3 ligase) inhibitor that stabilizes HIF-α. VH298 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. VH-298 can be used in PROTAC technology.
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.
Biochem Biophys Res Commun, 2021, 572:72-79
Basic & Clinical Medicine, 2020, 40(9): 1212-1217
Basic & Clinical Medicine, 2020, 40-9
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. Enarodustat has the potential for the treatment of renal anemia.
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.
A5251 PHD1/prolyl hydroxylase Rabbit Recombinant mAb PHD1/prolyl hydroxylase Rabbit Recombinant mAb detects endogenous level of total PHD1/prolyl hydroxylase.
S3589New Bendazol Bendazol (2-Benzylbenzimidazole, Dibazol, Dibazole, Bendazole, Tromasedan) is a hypotensive drug that enhances NO synthase activity in renal glomeruli and collecting tubules. Bendazol inhibits the progression of form-deprivation myopia (FDM) and suppresses the upregulation of HIF-1α.
S5742 Deferoxamine mesylate (Ba 33112) Deferoxamine mesylate (Ba 33112, Desferrioxamine B, DFOM, NSC 644468) is the mesylate salt of Deferoxamine, which forms iron complexes and is used as a chelating agent. Deferoxamine is a ferroptosis inhibitor that stabilizes HIF-1α expression and improves HIF-1α transactivity in hypoxic and hyperglycemic states in vitro. Deferoxamine decreases beta-amyloid (Aβ) deposition and induces autophagy.
Nat Immunol, 2021, 22(9):1107-1117
Nat Commun, 2021, 12(1):647
CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
S8351 PT2399 PT2399 is a potent and orally available antagonist of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β.
S8352 PT2385 PT2385 is a HIF-2α antagonist with luciferase EC50 of 27 nM and no significant off-target activity.
Lab Invest, 2021, 10.1038/s41374-021-00703-5
S1232 M1001 M1001 is a weak agonist of hypoxia-inducible factor-2α (HIF-2α) that binds to the HIF-2α PAS-B domain with Kd of 667 nM.
S1007 Roxadustat (FG-4592) Roxadustat (FG-4592) is an HIF-α prolyl hydroxylase inhibitor in a cell-free assay, stabilizes HIF-2 and induces EPO production. Roxadustat potentiates RSL3 induced ferroptosis. Phase 3.
Cell Rep, 2021, 35(3):109020
JCI Insight, 2021, 6(18)e133690
Cells, 2021, 10(6)1425
S2431 TMTD (Tetramethylthiuram disulfide) TMTD (Tetramethylthiuram disulfide) can reduce the growth performance of chickens through decreasing liver index, whereas increasing kidney, cardiac, and spleen index, and induces tibial dyschondrolplasia (TD) by changing the expressions of VEGF, HIF-1α and WNT4. TMTD (Tetramethylthiuram disulfide) is widely used in rubber processing as an ultra accelerator for low-temperature cures and in agriculture as an important pesticide.
S2919 IOX2 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.
J Biol Chem, 2021, S0021-9258(21)00710-9
J Proteomics, 2020, 211:103558
Cell Rep, 2019, 29(10):3009-3018
S5804 N-Acetylcysteine amide 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.
Nat Commun, 2021, 12(1):647
Int J Biochem Cell Biol, 2020, 121:105703
Pancreatology, 2019, 19(2):258-265
S6490 Vadadustat Vadadustat (AKB-6548, B-506, PG-1016548) is a novel, titratable, oral HIF-PH inhibitor.
Drug Test Anal, 2020, 10.1002/dta.2917
S7483 DMOG 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.
Cells, 2021, 10(6)1359
Aging (Albany NY), 2021, 13(8):11705-11726
Cell Prolif, 2021, e13158
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.
FASEB J, 2020, 34(2):2344-2358
J Photochem Photobiol B, 2020, 210:111980
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. Phase 2.
Cell Rep, 2021, 35(3):109020
J Bone Miner Res, 2021, 10.1002/jbmr.4272
Front Immunol, 2021, 12:678354
S8171 Daprodustat (GSK1278863) Daprodustat (GSK1278863) is an orally administered hypoxia-inducible factor-prolyl hydroxylase (HIF-PH) inhibitor. Phase 2.
Cell Rep, 2021, 35(3):109020
FASEB J, 2020, 34(2):2344-2358
Cancer Res, 2019, 79(10):2564-2579
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.
bioRxiv, 2021, 10.1101/2021.08.26.456853
FASEB J, 2020, 34(2):2344-2358
FASEB J, 2019, 33(11):12630-12643
S3589New Bendazol Bendazol (2-Benzylbenzimidazole, Dibazol, Dibazole, Bendazole, Tromasedan) is a hypotensive drug that enhances NO synthase activity in renal glomeruli and collecting tubules. Bendazol inhibits the progression of form-deprivation myopia (FDM) and suppresses the upregulation of HIF-1α.
Tags: HIF pathway | HIF cancer | hypoxia-inducible factor cancer | HIF-1 cancer | HIF activation | HIF-1 pathway | hypoxia-inducible factor pathway | HIF-1 activation | HIF-1α pathway | HIF inhibitor review