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. 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
  2. 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
  3. 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
  4. 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
  5. 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
  6. GSK1278863 (Daprodustat)

    Catalog No. A12671
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    HIF-prolyl hydroxylase Inhibitor
    GSK1278863 is a novel HIF-prolyl hydroxylase inhibitor. Learn More
  7. 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
  8. 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
  9. 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
  10. 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
  11. 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
  12. 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
  13. 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
  14. 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
  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. 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
  17. 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
  18. 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
  19. 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
  20. 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
  21. 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
  22. 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

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