HIF

Catalog No.Inhibitor Name HIFHIF1Other
A15530FG-2216
****
****
A15359KC7F2
**
**
A11237Roxadustat
A100122-Methoxyestradiol
Microtubule Associated
A14319PX-478 2HCl
A12978BAY 87-2243

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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  1. FG-4592 (Roxadustat)

    Catalog No. A11237
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    HIF-PHs inhibitor
    FG-4592 is a novel hypoxia inducible factor prolyl hydroxylase inhibitor, in CKD anemia. Learn More
  2. HIF-2α-IN-1

    Catalog No. A20631
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    HIF-2α inhibitor
    HIF-2α-IN-1 is a HIF-2α inhibitor has an IC50 of less than 500 nM in HIF-2α scintillation proximity assay. IC50 value: ?? 500 nM Target: HIF-2α. Learn More
  3. VH-298

    Catalog No. A20326
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    VHL:HIF-α interaction inhibitor
    VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with a Kd value of 80 to 90 nM, used in PROTAC technology. Learn More
  4. PT2399

    Catalog No. A19787
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    HIF-2α antagonist
    PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo. Learn More
  5. GN44028

    Catalog No. A19693
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    HIF-1 inhibitor
    GN44028 is a hypoxia inducible factor (HIF)-1 inhibitor, with an IC50 of 14 nM. Learn More
  6. M1001

    Catalog No. A19443
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    HIF-2α agonist
    M1001 is a weak agonist of HIF-2α, directly binds to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 enhances the stabilities of HIF-2α-ARNT complex. Learn More
  7. Prolyl Hydroxylase inhibitor 1

    Catalog No. A19227
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    HIF-PHD inhibitor
    Prolyl Hydroxylase inhibitor 1 (Compound 15i) is an orally active hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) inhibitor with an IC50 of 62.23 nM. Antianemia agent. Learn More
  8. AFP464

    Catalog No. A20978
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    HIF-1α inhibitor
    AFP464, is an active HIF-1α inhibitor with an IC50 of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator. Learn More
  9. PT-2385

    Catalog No. A21561
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    HIF-2α inhibitor
    PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM. Learn More
  10. (Rac)-PT2399

    Catalog No. A21376
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    HIF-2α inhibitor
    (Rac)-PT2399 (Compound 10e), the racemate of PT2399, acts as a potent and specific hypoxia-inducible factor 2a (HIF-2α) inhibitor with an IC50 of 0.01 μM. Learn More
  11. EL-102

    Catalog No. A20925
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    HIF1α inhibitor
    EL102 is a inhibitor of HIF1α , Which can inhibit tubulin polymerisation and decreased microtubule stability. Learn More
  12. ZINC13466751

    Catalog No. A12522
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    HIF-1α/von Hippel-Lindau interaction inhibitor
    ZINC13466751 is a potent inhibitor of HIF-1α/von Hippel-Lindau interaction with an IC50 of 2.0 ?M. Learn More
  13. MK-8617

    Catalog No. A12618
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    pan HIF PHD1-3 inhibitor
    MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2. Learn More
  14. SYP-5

    Catalog No. A13031
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    HIF-1 inhibitor
    SYP-5 is a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis. Learn More
  15. IOX 2

    Catalog No. A11924
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    HIF-PHD inhibitor
    IOX2 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. Learn More
  16. DMOG

    Catalog No. A13998
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    HIF-PH inhibitor
    DMOG is a cell permeable, competitive inhibitor of HIF-PH. It acts to stabilize HIF-1α expression at normal oxygen tensions in cultured cells, at concentrations between 0.1 and 1 mM. Learn More
  17. Oroxylin A

    Catalog No. A14367
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    Oroxylin A is an O-methylated flavone, It has demonstrated activity as a dopamine reuptake inhibitor and is also a negative allosteric modulator of the benzodiazepine site of the GABAA receptor. Learn More
  18. ML 228

    Catalog No. A15360
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    HIF activator
    ML-228 is an activator of the HIF signaling pathway, as demonstrated by HIF response element (HRE) reporter assay, HIF-1α nuclear translocation assay, and increased VEGF expression. Learn More
  19. KC7F2

    Catalog No. A15359
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    HIF inhibitor
    KC7F2 is an inhibitor of HIF-1α protein translation, but not transcription, that suppresses phosphorylation of two key regulators of protein synthesis, eukaryotic translation initiation factor 4E binding protein 1 (4EBP1) and p70 S6 kinase (S6K). Learn More
  20. Chetomin

    Catalog No. A15358
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    HIF inhibitor
    Chetomin is reported to be an antibiotic metabolite of Chaetomium spp. which contains bacteriostatic effects on Gram-positive bacteria. Learn More
  21. 2-Methoxyestradiol

    Catalog No. A10012
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    Apoptotic, antiproliferative and antiangiogenic agent
    2-Methoxyestradiol is an apoptotic, antiproliferative and antiangiogenic agent. Induces p53-induced apoptosis via two pathways: activation of p38 and NF-κB; and activation of JNK and AP-1 leading to Bcl-2 phosphorylation. Learn More
  22. FG-2216

    Catalog No. A15530
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    HIF-prolyl hydroxylase inhibitor
    FG-2216 is a potent HIF-prolyl hydroxylase inhibitor with IC50 of 3.9 uM for PDH2 enzyme; orally bioavailable and induced significant and reversible Epo induction in vivo, Learn More
  23. FM19G11

    Catalog No. A12883
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    HIFα inhibitor
    FM19G11 is an inhibitor of Hypoxia Inducible Factors α (HIFα), which are transcription factors that respond to changes in available oxygen in the cellular environment. Learn More
  24. HIF-C2

    Catalog No. A12921
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    HIF-2 inhibitor
    HIF-C2 is a potent and selective allosteric inhibitor of hypoxia inducible factor-2 (HIF-2) Learn More
  25. BAY 87-2243

    Catalog No. A12978
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    HIF inhibitor
    BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I. Learn More
  26. PX-478 HCl

    Catalog No. A14319
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    HIF-1alpha inhibitor
    PX-478 is HIF-1alpha inhibitor, is also an orally active small molecule with potential antineoplastic activity. PX-478 has excellent activity against established human tumor xenografts, providing tumor regressions with prolonged growth delays which correlate positively with HIF-1 levels. PX-478 is a highly water soluble molecule, with good i.v., i.p. and p.o. antitumor activity. Learn More
  27. Molidustat

    Catalog No. A14404
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    HIF-PH inhibitor
    Molidustat is a novel inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase (PH) which stimulates erythropoietin (EPO) production and the formation of red blood cells. Learn More
  28. Echinomycin

    Catalog No. A14021
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    HIF-1α inhibitor
    Hypoxia-inducible factor-1 (HIF-1) is a transcription factor that controls genes involved in glycolysis, angiogenesis, migration, and invasion. Echinomycin is a cell-permeable inhibitor of HIF-1-mediated gene transcription Learn More
  29. PT2977

    Catalog No. A18465
    HIF-2alpha inhibitor
    PT2977 is HIF-2alpha inhibitor with an IC50 of 9 nM. Learn More
  30. Desidustat

    Catalog No. A16921
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    HIF hydroxylase inhibitor
    Desidustat is an antianaemic drug candidate. It is an inhibitor of HIF hydroxylase extracted from patent WO 2014102818 A1, compound example 2. Learn More
  31. IDF-11774

    Catalog No. A16845
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    HIF-1 inhibitor
    Biological Activity Description 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. Learn More
  32. Vadadustat

    Catalog No. A16794
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    HIF prolyl-hydroxylase inhibitor
    Vadadustat, also known as AKB-6548 and PG-1016548, is a potent Hypoxia-inducible factor-proline dioxygenase inhibitor. Learn More
  33. LW6 (CAY10585)

    Catalog No. A12882
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    HIF-1 inhibitor
    LW6 is a novel HIF-1 inhibitor with an IC50 of 4.4 uM. Learn More
  34. HIF-2a Translation Inhibitor

    Catalog No. A16181
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    HIF-2a translation inhibitor
    HIF-2a translation inhibitor (IC50 value 5 uM); Decreases HIF-2a protein and HIF-2a target gene expression in normoxia and hypoxia independent of HIF-2a mRNA expression or HIF-2a protein stability, and independent of mTOR activity. Moreover, the translation inhibitor 76 enhances binding of IRP1 to the HIF-2a IRE (Iron-Responsive Element). Learn More
  35. DASA-58

    Catalog No. A15895
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    PKM2 Activator
    DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator. Learn More
  36. GSK1278863 (Daprodustat)

    Catalog No. A12671
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    HIF-prolyl hydroxylase Inhibitor
    GSK1278863 is a novel HIF-prolyl hydroxylase inhibitor. Learn More
  37. JNJ-42041935

    Catalog No. A15793
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    HIF-PHD Inhibitor II
    JNJ-42041935 is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes. Learn More

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