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HIFs

" in MedChemExpress (MCE) Product Catalog:

361

Inhibitors & Agonists

3

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6

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3

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17

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1

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56

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28

Isotope-Labeled Compounds

13

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2

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-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-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-100543
    Zenidolol
    40+ Cited Publications

    ICI-118551

    Adrenergic Receptor Apoptosis Caspase Bcl-2 Family HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease Neurological Disease Inflammation/Immunology
    Zenidolol (ICI-118551) is a selective β2-adrenergic receptor antagonist with Ki values of Zenidolol for β2, β1 and β3 adrenergic receptors of 0.7, 49.5 and 611 nM, respectively. Zenidolol exerts antitumor effects via inducing apoptosis, inhibiting tumor sphere formation, and downregulating the HIF pathway by blocking β2-AR on tumor cells. Zenidolol exhibits a unique pulmonary vessel-specific vasodilatory effect in mouse models. Zenidolol can be used as an intraocular pressure-lowering agent in ophthalmic disease research .
    Zenidolol
  • 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-108697
    PT2399
    10+ Cited Publications

    HIF/HIF Prolyl-Hydroxylase Cancer
    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 .
    PT2399
  • 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-103227
    Desidustat
    2 Publications Verification

    ZYAN1

    HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    Desidustat is an orally active HIF hydroxylase inhibitor. Desidustat can be used for the research of various disorders including anemia of different types and conditions associated with ischemia/hypoxia .
    Desidustat
  • 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-12519
    Oltipraz
    20+ Cited Publications

    RP 35972; NSC 347901

    HIF/HIF Prolyl-Hydroxylase HIV Keap1-Nrf2 Parasite Cancer
    Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.
    Oltipraz
  • HY-19621

    HIF/HIF Prolyl-Hydroxylase Cancer
    THS-044 is a modulator of the formation of the HIF2α/ARNT heterodimer. THS-044 binding stabilizes the HIF2α PAS-B folded state (KD = 2 μM), for regulating HIF2 activity in endogenous and pathological settings, and does not bind to HIF1α or ARNT PAS-B. THS-044 can be used for the study of diseases related to hypoxia .
    THS-044
  • 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-15641
    FG-2216
    5+ Cited Publications

    IOX3; YM311

    HIF/HIF Prolyl-Hydroxylase Metabolic Disease
    FG-2216 (IOX3) is a potent and orally active inhibitor of HIF prolyl hydroxylase-2 (PHD2), with an IC50 of 3.9 μM. FG-2216 induces robust erythropoietin and modest fetal hemoglobin in vivo .
    FG-2216
  • 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-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-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-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-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-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-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-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-111547

    HIF/HIF Prolyl-Hydroxylase Cancer
    M1001 is a weak hypoxia-inducible factor-2α (HIF-2α) agonist. M1001 can bind to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 can be used in chronic kidney disease research .
    M1001
  • 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-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-168641

    PROTACs Apoptosis HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology Cancer
    PROTAC HIF-1α degrader-1 (compound V2) is a potent hypoxia-inducible factor-1α (HIF-1α) PROTAC degrader with an IC50 value of 7.54 µM. PROTAC HIF-1α degrader-1 shows anti-proliferative activity. PROTAC HIF-1α degrader-1 decreases the HIF-1α protein expression. PROTAC HIF-1α degrader-1 induces apoptosis .
    PROTAC HIF-1α degrader-1
  • 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-153016
    HIF-2α agonist 2
    1 Publications Verification

    HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    HIF-2α agonist 2 (compound 10) is a HIF-2α agonist with an EC50 value of 1.68 μM at the dose of 20 μM. HIF-2α agonist 2 is non-cytotoxic against 786-O-HRE-Luc cells. HIF-2α agonist 2 can be used for oxygen metabolism research .
    HIF-2α agonist 2
  • 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-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-147029

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF1 agonist-1 (compound F4) is a potent HIF1 agonist with an EC50 value of 0.9 μM. HIF1 agonist-1 can be used for researching anticancer .
    HIF1 agonist-1
  • 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-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-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-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-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-P1888

    HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    HIF-1 alpha (556-574) is a short hypoxia-inducible factor-1 (HIF-1) 19 residues fragment. HIF-1 functions as master regulator of response to oxygen homeostasis .
    HIF-1 alpha (556-574)
  • 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-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; NKT2152

    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
  • HY-18370

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-3, an allosteric inhibitor of hypoxia inducible factor-2α (HIF-2α), exhibits an IC50 of 0.4 µM and a KD of 1.1 µM. Anticancer agent .
    HIF-2α-IN-3
  • HY-29090

    HIF/HIF Prolyl-Hydroxylase Cancer
    ML228 analog is an analog of ML228 (HY-12754). ML228 is a potent activator of HIF .
    ML228 analog

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