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  1. 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.
  2. HIF-PHs inhibitor

    FG-4592 is a novel hypoxia inducible factor prolyl hydroxylase inhibitor, in CKD anemia.
  3. 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.
  4. 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.
  5. 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.
  6. HIF-prolyl hydroxylase Inhibitor

    GSK1278863 is a novel HIF-prolyl hydroxylase inhibitor.
  7. HIF-1 inhibitor

    LW6 is a novel HIF-1 inhibitor with an IC50 of 4.4 uM.
  8. 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.
  9. HIF-2 inhibitor

    HIF-C2 is a potent and selective allosteric inhibitor of hypoxia inducible factor-2 (HIF-2)
  10. 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.
  11. HIF-1 inhibitor

    SYP-5 is a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis.
  12. PHD inhibitor

    TM6089 is a unique Prolyl Hydroxylase (PHD) inhibitor which stimulates HIF activity without iron chelation and induces angiogenesis and exerts organ protection against ischemia.
  13. 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.
  14. 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
  15. 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.
  16. 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.
  17. 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.
  18. HIF inhibitor

    Chetomin is reported to be an antibiotic metabolite of Chaetomium spp. which contains bacteriostatic effects on Gram-positive bacteria.
  19. 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).
  20. 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.
  21. 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,
  22. HIF-PHD Inhibitor II

    JNJ-42041935 is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes.
  23. 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).
  24. HIF prolyl-hydroxylase inhibitor

    Vadadustat, also known as AKB-6548 and PG-1016548, is a potent Hypoxia-inducible factor-proline dioxygenase inhibitor.
  25. 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.
  26. 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.
  27. interferon inducer

    Tilorone Dihydrochloride is an antiviral, antineoplastic, and anti-inflammatory agent; Orally active interferon inducer, inhibiting Ebola virus (EBOV).
  28. iron chelator

    Deferoxamine mesylate is an iron chelator that binds free iron in a stable complex, preventing it from engaging in chemical reactions.
  29. Amifostine is a phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia.
  30. HIF-2alpha inhibitor

    PT2977 is HIF-2alpha inhibitor with an IC50 of 9 nM.
  31. PHD2 inhibitor

    OX4 is a potent inhibitor of PHD2 (IC50 = 1.6 nM).
  32. 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.
  33. 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.
  34. HIF-1 inhibitor

    GN44028 is a hypoxia inducible factor (HIF)-1 inhibitor, with an IC50 of 14 nM.
  35. 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.
  36. PHD inhibitor

    TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with a Ki value of 5.3 nM for human PHD2.
  37. 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.
  38. 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.
  39. HIF modulator

    THS-044 binding stabilizes the HIF2α PAS-B folded state, for regulating HIF2 activity in endogenous and clinical settings.
  40. Microtubule-Targeting Agent

    ENMD-119 is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity, and is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.
  41. HIF1α inhibitor

    EL102 is a inhibitor of HIF1α , Which can inhibit tubulin polymerisation and decreased microtubule stability.
  42. HIF-1α inhibitor

    Minocycline hydrochloride is a broad-spectrum tetracycline antibiotic, acting by binding to the bacterial 30S ribosomal subunit and inhibiting protein synthesis.
  43. 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.
  44. 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.
  45. HIF-2α inhibitor

    PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM.
  46. Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α).

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