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HIF inhibitor

" in MedChemExpress (MCE) Product Catalog:

282

Inhibitors & Agonists

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4

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1

Biochemical Assay Reagents

10

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1

Inhibitory Antibodies

40

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25

Isotope-Labeled Compounds

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GMP Molecules

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15893
    DMOG
    75+ Cited Publications

    Dimethyloxallyl Glycine

    HIF/HIF Prolyl-Hydroxylase Autophagy Cancer
    DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation?in vitro and in vivo . DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG?acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal . DMOG induces cell autophagy .
    DMOG
  • HY-N6782
    Oligomycin
    Maximum Cited Publications
    105 Publications Verification

    Oxidative Phosphorylation ATP Synthase Fungal Antibiotic Infection Cancer
    Oligomycin, an antifungal antibiotic, is an inhibitor of H +-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells .
    Oligomycin
  • HY-10231
    PX-478
    90+ Cited Publications

    HIF/HIF Prolyl-Hydroxylase Autophagy Cancer
    PX-478 is an orally active HIF-1α inhibitor with potent antitumor activities. PX-478 can cross the blood-brain barrier .
    PX-478
  • HY-125840
    Belzutifan
    10+ Cited Publications

    PT2977; MK-6482

    HIF/HIF Prolyl-Hydroxylase Cancer
    Belzutifan (PT2977) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. Belzutifan, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. Belzutifan is a potential treatment for clear cell renal cell carcinoma (ccRCC) .
    Belzutifan
  • HY-15836
    BAY 87-2243
    25+ Cited Publications

    HIF/HIF Prolyl-Hydroxylase Ferroptosis Cancer
    BAY 87-2243 is a highly potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor.
    BAY 87-2243
  • HY-B0219
    Allopurinol
    10+ Cited Publications

    Xanthine Oxidase Infection Neurological Disease Inflammation/Immunology Cancer
    Allopurinol is a potent and orally active xanthine oxidase inhibitor with an IC50 value of 0.2-50 μM. Allopurinol can be used in the research of hyperuricemia and gout. Allopurinol decreases the expression of HIF-1α and HIF-2α protein. Allopurinol shows anti-depressant and anti-nociception activity. Anti-leishmanial effect .
    Allopurinol
  • HY-13671
    LW6
    55+ Cited Publications

    HIF-1α inhibitor; LW8

    HIF/HIF Prolyl-Hydroxylase Apoptosis Cancer
    LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC50 value of 4.4 μM, and it is also an inhibitor of MDH2. LW6 decreases HIF-1α protein expression without affecting HIF-1β expression.
    LW6
  • HY-12867
    PT-2385
    50+ Cited Publications

    HIF/HIF Prolyl-Hydroxylase Cancer
    PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM .
    PT-2385
  • HY-121172
    1,4-DPCA
    1 Publications Verification

    HIF/HIF Prolyl-Hydroxylase Cancer
    1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM .
    1,4-DPCA
  • HY-100575
    Acriflavine
    5+ Cited Publications

    Acriflavinium chloride 3,6-Acridinediamine mix

    Environmental Pollutants Fluorescent Dye Monocarboxylate Transporter Bacterial Fungal HIF/HIF Prolyl-Hydroxylase SARS-CoV Infection Cancer
    Acriflavine (Acriflavinium chloride) is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine is an antiseptic agent. Acriflavine is a potent HIF-1 inhibitor that prevents the dimerization of HIF-1α and HIF-1β subunits. Acriflavine inhibits the interaction between monocarboxylate transporter 4 (MCT4) and Basigin. Acriflavine is used in cancer research, such as breast cancer, brain tumor and chronic myeloid leukemia. Acriflavine is a potent papain-like protease (PLpro) inhibitor, which inhibits SARS-CoV-2 .
    Acriflavine
  • HY-N0596
    Panaxadiol
    4 Publications Verification

    20(R)-Panaxadiol

    PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT Cancer
    Panaxadiol (20(R)-Panaxadiol) is an orally active HIF-1α/STAT3 inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities .
    Panaxadiol
  • HY-110266
    GN44028
    5+ Cited Publications

    HIF/HIF Prolyl-Hydroxylase Cancer
    GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers .
    GN44028
  • HY-B0219A
    Allopurinol sodium
    10+ Cited Publications

    Xanthine Oxidase Infection Neurological Disease Inflammation/Immunology Cancer
    Allopurinol sodium is a potent and orally active xanthine oxidase inhibitor with an IC50 value of 0.2-50 μM. Allopurinol sodium can be used in the research of hyperuricemia and gout. Allopurinol sodium decreases the expression of HIF-1α and HIF-2α protein. Allopurinol sodium shows anti-depressant and anti-nociception activity. Anti-leishmanial effect .
    Allopurinol sodium
  • HY-153017

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1 inhibitor-4 is a HIF-1 inhibitor (IC50: 560 nM). HIF-1 inhibitor-4 reduces the HIF-1α protein level without affecting its mRNA level .
    HIF-1 inhibitor-4
  • HY-W088075
    Acriflavine hydrochloride
    5+ Cited Publications

    Acriflavinium chloride hydrochloride

    Fluorescent Dye HIF/HIF Prolyl-Hydroxylase Bacterial SARS-CoV Monocarboxylate Transporter Fungal Infection Cancer
    Acriflavine (Acriflavinium chloride) hydrochloride is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine hydrochloride is an antiseptic agent. Acriflavine hydrochloride is a potent HIF-1 inhibitor that prevents the dimerization of HIF-1α and HIF-1β subunits. Acriflavine hydrochloride inhibits the interaction between monocarboxylate transporter 4 (MCT4) and Basigin. Acriflavine hydrochloride is used in cancer research, such as breast cancer, brain tumor and chronic myeloid leukemia. Acriflavine hydrochloride is a potent papain-like protease (PLpro) inhibitor, which inhibits SARS-CoV-2 .
    Acriflavine hydrochloride
  • HY-P2657

    HIF/HIF Prolyl-Hydroxylase Proton Pump Endogenous Metabolite Cancer
    Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
    Verucopeptin
  • HY-N0242
    Fraxinellone
    4 Publications Verification

    PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT Inflammation/Immunology Cancer
    Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1 .
    Fraxinellone
  • HY-159644

    AB521

    HIF/HIF Prolyl-Hydroxylase VEGFR Cancer
    Casdatifan (AB521) is an orally active and selective allosteric small-molecule inhibitor of hypoxia-inducible factor 2α (HIF-2α). Casdatifan inhibits pro-tumor gene transcription by blocking the heterodimerization of HIF-2α with ARNT, and significantly suppresses tumor growth in clear cell renal cell carcinoma (ccRCC) models either as a monotherapy or in combination with agents such as Zimberelimab (HY-P99109). Casdatifan is applicable for the research of ccRCC .
    Casdatifan
  • HY-18371
    TC-S 7009
    1 Publications Verification

    HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    TC-S 7009 is a potent and selective HIF-2α inhibitor with a Kd of 81 nM. TC-S 7009 is more selective for HIF-2α than HIF-1α (Kd ? 5 μM). TC-S 7009 disrupts HIF-2α heterodimerization, decreases DNA-binding activity, and reduces HIF-2α target gene expression .
    TC-S 7009
  • HY-156106

    HIF/HIF Prolyl-Hydroxylase Ligands for E3 Ligase E1/E2/E3 Enzyme Cancer
    VHL-IN-1 (Compound 30) is an E3 ligase VHL inhibitor with a Kd value of 37 nM. VHL-IN-1 blocks VHL-mediated ubiquitination and degradation of HIF-1α. VHL-IN-1 stabilizes the protein levels of HIF-1α and hydroxylated HIF-1α, and induces the transcriptional activity of HIF-1α. VHL-IN-1 can be used for PROTAC development. VHL-IN-1 is applicable for cancer research .
    VHL-IN-1
  • HY-100693
    SYP-5
    2 Publications Verification

    HIF/HIF Prolyl-Hydroxylase Cancer
    SYP-5 is a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis.
    SYP-5
  • HY-44809

    HIF/HIF Prolyl-Hydroxylase Bacterial Cardiovascular Disease Infection Inflammation/Immunology
    Izilendustat is a potent prolyl hydroxylase inhibitor. Izilendustat competitively inhibits HIFPH2 activity, blocks HIF-1α degradation, stabilizes HIF-1α and HIF-2α proteins, and upregulates downstream target gene expression. Izilendustat can reduce intestinal inflammation and damage, enhance the ability of phagocytes to clear pathogens, and improve ischemia-related pathological phenotypes. Izilendustat can be used for the research of inflammatory bowel disease, ischemic vascular disease and anemia .
    Izilendustat
  • HY-148860

    HIF-2α-IN-8

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-8 is a potent and orally active HIF2α inhibitor with IC50 values of 9, 37, 246 nM for HIF2α SPA, HIF2α iScript, HIF2α HRE RGA, respectively. HIF-2α-IN-8 shows antitumor activity .
    NVP-DFF332
  • HY-P1420
    TAT-cyclo-CLLFVY
    2 Publications Verification

    HIF/HIF Prolyl-Hydroxylase Cancer
    TAT-cyclo-CLLFVY is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM .
    TAT-cyclo-CLLFVY
  • HY-139287
    M1002
    2 Publications Verification

    HIF/HIF Prolyl-Hydroxylase Cancer
    M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist, and can enhance the expression of HIF-2 target genes. M1002 shows synergy with prolyl-hydroxylase domain (PHD) inhibitors .
    M1002
  • HY-115746

    DMBPA

    HIF/HIF Prolyl-Hydroxylase Cancer
    Dimethyl-bisphenol A (DMBPA) is a potent HIF-1α inhibitor. Dimethyl-bisphenol A can decrease Vegfa mRNA expression .
    Dimethyl-bisphenol A
  • HY-124473

    Naphthafluorescein

    HIF/HIF Prolyl-Hydroxylase Cancer
    Naphthofluorescein inhibits the interaction between HIF-1 and Mint3. Naphthofluorescein suppresses Mint3-dependent HIF-1 activity and glycolysis in cancer cells and macrophages without cytotoxicity in vitro and adverse effect in vivo . Naphthofluorescein is also a fluorescent pH-sensitive probe that can be used for functional Cerenkov imaging .
    Naphthofluorescein
  • HY-15672

    HIF/HIF Prolyl-Hydroxylase Neurological Disease Cancer
    FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC50 of 80 nM in HeLa cells. FM19G11 modulates other signaling pathways, including mTOR and PI3K/Akt/eNOS, when the HIF-1α pathway is inactivated under normoxic conditions .
    FM19G11
  • HY-P10426

    HIF/HIF Prolyl-Hydroxylase VEGFR Cancer
    cyclo(CLLFVY) is an inhibitor for hypoxia inducible factor-1 (HIF-1), with IC50 of 19 μM (in U2OS) and 16 μM (in MCF-7). cyclo(CLLFVY) binds to the PAS-B domain of HIF-1α, inhibits HIF-1 dimerization and transcriptional activity. cyclo(CLLFVY) downregulates the expression of hypoxia response genes, such as VEGF and CAIX, exhibits antitumor against the HIF-1 associated cancers .
    cyclo(CLLFVY)
  • HY-P10221A

    HIF/HIF Prolyl-Hydroxylase Cancer
    Cyclo(CKLIIF) TFA is an inhibitor of HIF-1α and HIF-2α. The KD values of Cyclo(CKLIIF) TFA for the PAS-B domains of HIF1-α and HIF2-α are 2.6 μM and 2.2 μM, respectively. Cyclo(CKLIIF) TFA disrupts the protein-protein interaction between HIF-1α and HIF-1β. Cyclo(CKLIIF) TFA can be used in cancer research .
    Cyclo(CKLIIF) TFA
  • HY-115903
    HIF-1α-IN-2
    4 Publications Verification

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation .
    HIF-1α-IN-2
  • HY-19949
    HIF-2α-IN-1
    1 Publications Verification

    HIF/HIF Prolyl-Hydroxylase Metabolic Disease
    HIF-2α-IN-1 (compound 9b) is a HIF-2α inhibitor (IC50=1.7 μM, SPA/scintillation proximity assay) .
    HIF-2α-IN-1
  • HY-123422

    HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    GSK360A is a potent and orally active HIF-PHD inhibitor with IC50 values of 10, 100, and 126 nM for PHD1, PHD2, and PHD3, respectively. GSK360A activates the HIF-1 alpha pathway and protect the failing heart after myocardial infarction (MI) .
    GSK360A
  • HY-146144

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-IN-1 (Compound 3c) is a hypoxia-inducible factor (HIF)-1 inhibitor. HIF-IN-1 suppresses HIF-1α protein accumulation without affecting the levels of HIF-1α mRNA. HIF-IN-1 shows no obvious cytotoxicity .
    HIF-IN-1
  • HY-151344

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1/2α-IN-2 is an inhibitor of HIF-1/2α. HIF-1/2α-IN-2 decrease HIF-1/2α levels and induces iron starvation response by targeting Iron Sulfur Cluster Assembly 2 (ISCA2) .
    HIF-1/2α-IN-2
  • HY-151465

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1α-IN-4 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-4 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-4 can be used in the research of cancer .
    HIF-1α-IN-4
  • HY-136748
    HIF-2α-IN-4
    1 Publications Verification

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-4 is a potent inhibitor of hypoxia inducible factor-2α (HIF-2α) translation, with an IC50 of 5 μM. HIF-2α-IN-4 decreases both constitutive and hypoxia-induced HIF-2α protein expression. HIF-2α-IN-4 links its 5'UTR iron-responsive element to oxygen sensing .
    HIF-2α-IN-4
  • HY-177078

    HIF/HIF Prolyl-Hydroxylase Cancer
    Davotifan (Compound A17) is a bicyclic compound. Davotifan is an inhibitor of HIF-2α. Davotifan can be studied in research for HIF-2α-related cancer .
    Davotifan
  • HY-15893R

    Dimethyloxallyl Glycine (Standard)

    HIF/HIF Prolyl-Hydroxylase Autophagy Reference Standards Cancer
    DMOG (Standard) is the analytical standard of DMOG. This product is intended for research and analytical applications. DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo . DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal . DMOG induces cell autophagy .
    DMOG (Standard)
  • HY-B0219R

    Reference Standards Xanthine Oxidase Infection Neurological Disease Inflammation/Immunology Cancer
    Allopurinol (Standard) is the analytical standard of Allopurinol. This product is intended for research and analytical applications. Allopurinol is a potent and orally active xanthine oxidase inhibitor with an IC50 value of 0.2-50 μM. Allopurinol can be used in the research of hyperuricemia and gout. Allopurinol decreases the expression of HIF-1α and HIF-2α protein. Allopurinol shows anti-depressant and anti-nociception activity. Anti-leishmanial effect .
    Allopurinol (Standard)
  • HY-P10222

    HIF/HIF Prolyl-Hydroxylase Cancer
    Cyclo CRLLIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains KD of 14.5 and 10.2 μM, respectively .
    Cyclo(CRLLIF)
  • HY-163370

    HIF/HIF Prolyl-Hydroxylase Neurological Disease
    HIF-1α-IN-7 (Compound D13) is a potent HIF-1α inhibitor. HIF-1α-IN-7 has neuroprotective activity. HIF-1α-IN-7 can be used in Alzheimer's disease research .
    HIF-1α-IN-7
  • HY-115903A
    HIF-1α-IN-2 hydrochloride
    4 Publications Verification

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1α-IN-2 hydrochloride is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 hydrochloride suppresses HIF-1α expression by blocking transcription and protein translation .
    HIF-1α-IN-2 hydrochloride
  • HY-123009

    HIF/HIF Prolyl-Hydroxylase Histone Acetyltransferase Cancer
    KCN1 is a p300/HIF-1α interaction inhibitor. KCN1 inhibits HIF transcriptional activity by binding to the CH1 domain of p300 and preventing the p300/HIF-1α assembly. KCN1 exerts antitumor activities through cell cycle arrest .
    KCN1
  • HY-125840R

    PT2977 (Standard); MK-6482 (Standard)

    HIF/HIF Prolyl-Hydroxylase Reference Standards Cancer
    Belzutifan (Standard) is the analytical standard of Belzutifan. This product is intended for research and analytical applications. Belzutifan (PT2977) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. Belzutifan, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. Belzutifan is a potential treatment for clear cell renal cell carcinoma (ccRCC) .
    Belzutifan (Standard)
  • HY-158826A

    HIF/HIF Prolyl-Hydroxylase Cancer
    EZN-2968 sodium is an antisense oligonucleotide that specifically binds and inhibits the expression of HIF-1α mRNA. EZN-2968 sodium, inhibits tumor cell growth.
    EZN-2968 sodium
  • HY-170027

    HIF/HIF Prolyl-Hydroxylase AMPK Cancer
    LW1564 is an inhibitor for HIF-1α with an IC50 of 1.2 µM in HepG2. LW1564 inhibits mitochondrial respiration, reduces ATP production, stimulates HIF-1α degradation, and inhibits proliferation of various cancer cells with GI50 of 0.4-4.6 μM. LW1564 activates AMPK signaling pathway and inhibits lipid synthesis. LW1564 exhibits antitumor in HepG2 xenograft mouse model .
    LW1564
  • HY-153493A

    Small Interfering RNA (siRNA) Metabolic Disease
    PF-04523655 sodium is a siRNA directed against RTP801 gene. RTP801 sodium is an inhibitor of the mammalian target of rampamycin complex 1 (mTORC1) and downstream transcription factor HIF-1.
    PF-04523655 sodium
  • HY-151466

    HIF/HIF Prolyl-Hydroxylase Monoamine Oxidase Cancer
    HIF-1α-IN-5 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-5 also inhibits MAO-A activity. HIF-1α-IN-5 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-5 can be used in the research of cancer .
    HIF-1α-IN-5
  • HY-148264

    HIF-2α-IN-7

    HIF/HIF Prolyl-Hydroxylase Infection Metabolic Disease Inflammation/Immunology Cancer
    Imdatifan (HIF-2α-IN-7) is a hypoxia inducible factor 2α (HIF-2α) inhibitor. Imdatifan can inhibit HIF-2α with an EC50 value of 6 nM. Imdatifan can be used for the research of various types of diseases including cancer, liver disease, inflammatory disease, pulmonary diseases and iron load disorders .
    Imdatifan

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