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HIF

Hypoxia-inducible factor 1-alpha, also known as HIF-1-alpha, is a subunit of a heterodimeric transcription factor hypoxia-inducible factor 1 (HIF-1) that is encoded by the HIF1A gene. It is a basic helix-loop-helix PAS domain containing protein, and is considered as the master transcriptional regulator of cellular and developmental response to hypoxia. The dysregulation and overexpression of HIF1A by either hypoxia or genetic alternations have been heavily implicated in cancer biology, as well as a number of other pathophysiologies, specifically in areas of vascularization and angiogenesis, energy metabolism, cell survival, and tumor invasion. Two other alternative transcripts encoding different isoforms have been identified.

  • PX-478
    T6961685898-44-6
    PX-478 is a HIF-1α inhibitor with selectivity, oral activity, and blood-brain barrier permeability. PX-478 has antitumor activity and also protects pancreatic β-cell function in diabetes mellitus and is used in type 2 diabetes mellitus research.
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  • Hydroxycitric acid tripotassium hydrate
    T115896100-05-6
    Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) effectively inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation, and anti-tumor effects. Hydroxycitric acid tripotassium hydrate(Potassium citrate monohydrate) (Potassium citrate monohydrate) is the major active ingredient of Garcinia cambogia and a derivative of citric acid. Hydroxycitric acid tripotassium hydrate(Potassium citrate monohydrate) competitively inhibits ATP citrate lyase with weight loss benefits.
    • $76
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  • Sodium Aescinate
    T302720977-05-3
    Sodium Aescinate (Escin sodium salt) is extracted from Aesculus wilsonii.
    • $50
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  • 2-Methoxyestradiol
    T2220362-07-2
    2-Methoxyestradiol (2-ME2) is an orally bioavailable estradiol metabolite with potential antineoplastic activity. 2-Methoxyestradiol inhibits angiogenesis by reducing endothelial cell proliferation and inducing endothelial cell apoptosis. This agent also inhibits tumor cell growth by binding to tubulin, resulting in antimitotic activity, and by inducing caspase activation, resulting in cell cycle arrest in the G2 phase, DNA fragmentation, and apoptosis.
    • $50
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  • AKB-6899
    T297971007377-55-0In house
    AKB-6899 is an inhibitor of prolyl hydroxylase domain 3 (PHD3) and increases the soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages. AKB-6899 leads to stabilization of HIF-2α which induces sVEGFR-1 production from tumor-associated macrophages and decreases tumor growth.
    • $68
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  • HIF-2α agonist 2
    T678312750141-15-0In house
    HIF-2α agonist 2 is an HIF-2α agonist with an EC50 value of 1.68 μM for HIF-2α. HIF-2α agonist 2 can promote the stability of the ARNT A/B ring in the 3z structure of HIF-2a-ARNT complex without cytotoxicity to 786-o-Reha-Luc cells. HIF-2α agonist 2 can be used in the study of oxygen metabolism and is closely related to the occurrence of cancer.
    • $51
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  • ENMD-1198
    T15234864668-87-1In house
    ENMD-119 is a 2-methoxyestradiol analog with antiproliferative and antiangiogenic activity. It is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.
    • $1,520
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  • M1002
    T61822823830-85-9In house
    M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist that enhances the affinity of HIF-2alpha and ARNT for transcriptional activation.M1002 alters the Tyr2 conformation of the HIF-281alpha PAS-B structural domain and acts synergistically with inhibitors of the prolyl hydroxylase structural domain (PHD).
    • $44
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  • PT-2385
    T78481672665-49-4In house
    PT-2385 is a selective HIF-2α inhibitor (Kd<50 nM).
    • $61
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  • Cinnamaldehyde
    T4S1551104-55-2
    1. Cinnamaldehyde (Cinnamic Aldehyde) has antipyretic activity. 2. Cinnamaldehyde is a sedative agent. 3. Cinnamaldehyde inhibits invasive capabilities of MDA-MB-435S cells was correlated with down-regulating the expression of miR-27a. 4. Cinnamaldehyde induces the generation of reactive oxygen species and exerts vasodilator and anticancer effects. 5. Cinnamaldehyde appears to be a promising candidate as an adjuvant in combination therapy with 5-fluorouracil (5-FU) and oxaliplatin (OXA), two chemotherapeutic agents used in CRC treatment. The possible mechanisms of its action may involve the regulation of drugmetabolizing genes. 6. Cinnamaldehyde plays a certain role in inhibiting the occurrence and progression of melanoma and its action mechanism may be manifested by inhibiting expression of VEGF and HIF-α, thus blood vessel simulation and formation of new blood vessels of melanoma cells, and growth of tumors accordingly.
    • $30
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  • VH-298
    TQ01212097381-85-4
    VH-298 is a potent inhibitor of VHL that stabilizes HIF-α and elicits a hypoxic response via a different mechanism, that is the blockade of the VHL:HIF-α protein-protein interaction downstream of HIF-α hydroxylation by PHD enzymes.
    • $39
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  • Dapagliflozin
    T2389461432-26-8
    Dapagliflozin (BMS-512148) is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.
    • $42
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  • Lificiguat
    T4381170632-47-0
    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).
    • $43
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  • Deferoxamine
    T12435870-51-9
    Deferoxamine(Desferrioxamine B) is an iron chelator (binds Fe(III) and many other metal cations) that inhibits neuronopathy, may be used to modify the reduction of iron accumulation and deposition in tissues, and may improve neurological dysfunction by inhibiting ferroptosis and neuroinflammation following traumatic brain injury.Desferrioxamin-B has antioxidant, antiproliferative, Deferoxamine has antioxidant, antiproliferative, and antitumor activities, and can induce HIF-1α production, apoptosis and autophagy in cancer cells.Desferrioxamin-B can be used in the treatment of acute iron toxicity and COVID-19 related diseases.
    • $64
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  • Cucurbitacin B
    T34046199-67-3
    Cucurbitacin B (Cuc B) has profound in vitro and in vivo antiproliferative effects against human pancreatic Y cells. It inhibited AKT signaling activation through up-regulation of PTEN. Cucurbitacin B is an effective inhibitor of HIF-1 and provide new perspectives into the mechanism of its anticancer activity. Cucurbitacin B inhibits proliferation and induces apoptosis via STAT3 pathway inhibition in A549 lung Y cells.
    • $44
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  • IDF-11774
    T55371429054-28-3
    IDF-11774 is a HIF-1 inhibitor.It reduces hif-1α HRE luciferase activity (IC50 = 3.65 μM).
    • $55
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  • BAY 87-2243
    T24881227158-85-1
    BAY 87-2243 is a potent and selective inhibitor of hypoxia-inducible factor-1 (HIF-1).
    • $38
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  • Ganetespib
    T2309888216-25-9
    Ganetespib (STA-9090) is a synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.
    • $61
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  • DMOG
    T193989464-63-1
    DMOG (Dimethyloxalylglycine), an antagonist of the α-ketoglutarate cofactor, is an inhibitor for HIF prolyl hydroxylase.
    • $47
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  • LW6
    T3494934593-90-5
    LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor.
    • $39
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  • KC7F2
    T3169927822-86-4
    KC7F2 is a potent HIF-1 pathway inhibitor with potential anti-cancer activity.
    • $43
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  • Roxadustat
    T2515808118-40-3
    Roxadustat (FG-4592) is an orally bioavailable, hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI), with potential anti-anemic activity.
    • $30
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  • Vomifoliol
    TN525023526-45-6
    Vomifoliol is most likely the immediate precursor of dehydrovomifoliol, because of the organism converted abscisic acid (ABA), to dehydrovomifoliol as the major metabolise, and a cell-free extract exhibits vomifoliol dehydrogenase activity. Vomifoliol and
    • $1,289
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  • Adaptaquin
    T22022385786-48-1
    Adaptaquin is an inhibitor of the hypoxia-inducing factor prolyl hydroxylase (HIF-PH) [1] [2].
    • $47
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  • Manassantin A
    TN448988497-87-4
    Manassantin A is a high potent HIF-1 inhibitor, it protects the gastric mucosa from ethanol-induced acute gastric injury, and suggest that these protective effects might be associated with COX/PGE2 stimulation, inhibition of iNOS production and NF-κB act
    • $1,280
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  • Panaxynol
    TN204081203-57-8
    Panaxynol is the most potent antiplatelet agent in ginseng and its mechanism of action is chiefly due to the inhibition of thromboxane formation.
    • $710
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  • Myricanol
    TN460333606-81-4
    Myricanol can elicit growth inhibitory and cytotoxic effects on lung cancer cells, it can significantly decelerate tumor growth in vivo by inducing apoptosis.
    • $1,410
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  • HIF-2α-IN-2
    T115611672666-82-8
    HIF-2α-IN-2 is a hypoxia-inducible factor (HIF-2α) inhibitor (IC50: 16 nM in scintillation proximity assay).
    • $108
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  • Carvedilol
    T044772956-09-3
    Carvedilol (SKF 105517) Phosphate is the phosphate salt form of carvedilol, a racemic mixture and adrenergic blocking agent with antihypertensive activity and devoid of intrinsic sympathomimetic activity. The S enantiomer of carvedilol nonselectively binds to and blocks beta-adrenergic receptors, thereby exerting negative inotropic and chronotropic effects, and leading to a reduction in cardiac output. In addition, both enantiomers of carvedilol bind to and block alpha 1-adrenergic receptors, thereby causing vasodilation and reducing peripheral vascular resistance.
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    • Chetomin
      T68041403-36-7
      Chetomin (BRN0077366) is an inhibitor of HIF-1 by weaken transcription of HIF-1, disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar concentrations.
      • $98
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    • HIF-1 inhibitor-4
      T67767333357-56-5
      HIF-1 inhibitor-4 (HIF-1 inhibitor-4) is a HIF-1 inhibitor with IC50 of 560 nM. HIF-1 inhibitor-4 reduces the HIF-1α protein level without affecting its mRNA level.
      • $41
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    • ZINC13466751
      T13398117953-17-0
      ZINC13466751 is a potent HIF-1α/von Hippel-Lindau interaction inhibitor(IC50 of 2.0 µM).
      • $68
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    • Acriflavine Hydrochloride
      T198328063-24-9
      Acriflavine Hydrochloride (Acriflavine HCl) is a HIF-1α inhibitor. It acts by targeting HIF-1α-mediated pathways and decreasing the level of PGK1, VEGF, and HIF-1α in vitro and in vivo.
      • $41
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    • Moracin P
      TN1952102841-46-3
      Moracin P exhibits potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1), which is a key mediator during adaptation of cancer cells to tumour hypoxia.
      • $689
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    • Oligomycin
      T214941404-19-9
      Oligomycin is an antifungal antibiotic that is an inhibitor of H+-ATP synthetase. The Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibited HIF-1alpha expression in hypoxic tumor cells.
      • $42
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    • Vadadustat
      T46511000025-07-9
      Vadadustat is a novel, titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor in development for the treatment of anemia.
      • $42
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    • Moracin O
      TN1951123702-97-6
      Moracin O shows significant neuroprotective, and analgesic activities, it also has a strong protective influence against doxorubicin-induced cardiomyopathy in H9c2 cells with the EC50 value of 4.5 ± 1.3 μM. Moracin O exhibits potent in vitro inhibitory ac
        7-10 days
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      • Naphthofluorescein
        T3695361419-02-1
        Naphthofluorescein (Naphthafluorescein) is a Mint3 inhibitor with potential antitumor and anti-inflammatory activities, inhibits the interaction between HIF-1 and Mint3, inhibits Mint3-dependent HIF-1 activity, and inhibits glycolytic activity in cancer cells and macrophages without showing significant in vitro cytotoxicity or in vivo side effects. Naphthofluorescein is also a fluorescent pH-sensitive probe for functional Cherenkov imaging.
        • $44
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      • SYP-5
        T130501384268-04-5
        SYP-5 is a novel inhibitor of HIF-1, suppresses tumor cells invasion and angiogenesis.
        • $38
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      • Oltipraz
        T015364224-21-1
        Oltipraz (RP 35972) is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties. Oltipraz induces phase II detoxification enzymes, such as glutathione S transferase (GST) and NAD(P)H: quinone oxidoreductase 1 (NQO1). The induction of detoxification enzymes enhances the detoxification of certain cancer-causing agents, thereby enhancing their elimination and preventing carcinogen-induced DNA damages. Although the exact mechanism through which the anti-angiogenesis effect remains to be fully elucidated, oltipraz maybe able to modulate the expression of a number of angiogenic factors, thereby blocking the sustained and focal neovascularization in multiple tumor cell types.
        • $31
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      • TC-S 7009
        T170091422955-31-4
        TC-S 7009 is a potent and selective HIF-2α inhibitor (Kd: 81 nM). The affinity of TC-S 7009 to HIF-2α was higher than that of HIF-1α (Kd >> 5μM). TC-S 7009 disrupts HIF-2α heterodimerization, reduces HIF-2α target gene expression, and reduces dna binding activity.
        • $64
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      • HIF-2α-IN-1
        T154821799948-06-3
        HIF-2α-IN-1 is a potent HIF-2α inhibitor with IC50 values less than 500 nM.
        • $122
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      • ML228
        T78361357171-62-0
        ML228 is a potent the Hypoxia Inducible Factor (HIF) pathway activator with EC50 of 1 μM. ML228 potently activates HIF in vitro as well as its downstream target VEGF.
        • $37
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      • Cephaeline
        TN1480483-17-0
        Cephaeline was highly active against protected primary CLL cells (relative IC50's 35nM ) and acted by repressing HIF-1α± and disturbing intracellular redox homeostasis.
        • $189
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      • HIF-2α-IN-3
        T11562313964-19-1
        HIF-2α-IN-3 is a HIF-2α alteration inhibitor with anti-tumor properties and may be used in the study of cardiovascular disease.
        • $117
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      • M1001
        T7802874590-32-6
        M1001 is a HIF-2α agonist.
        • $55
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      • FM19G11
        T36711329932-55-0
        FM19G11 is an inhibitor of hypoxia inducible factor (HIF) α-subunit (IC50 = 80 nM in hypoxia induced luciferase assay).
        • $43
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      • EL-102
        T152051233948-61-2
        EL-102 is a HIF1α inhibitor with anticancer activity that inhibits microtubule protein polymerization and can be used to study prostate cancer.
        • $89
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      • 2,4-DPD
        T769241438-38-4
        2,4-DPD is competitive inhibitor of the oxygen-sensing enzyme HIF-α prolyl hydroxylase (HIF-PH)
        • $42
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      • Acetylarenobufagin
        T10233184673-79-8
        Acetylarenobufagin is a steroidal hypoxia-inducible factor-1 (HIF-1) modulator.
        • $105
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