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Isoforms Recommended: HIF-1α HIF
Results for "

HIF-1α

" in MedChemExpress (MCE) Product Catalog:

95

Inhibitors & Agonists

1

Screening Libraries

1

Biochemical Assay Reagents

15

Peptides

18

Natural
Products

1

Recombinant Proteins

6

Isotope-Labeled Compounds

2

Antibodies

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13671
    LW6
    15+ Cited Publications

    HIF- inhibitor; LW8

    HIF/HIF Prolyl-Hydroxylase Apoptosis Cancer
    LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC50 of 4.4 μM. LW6 decreases HIF-1α protein expression without affecting HIF-1β expression.
    LW6
  • HY-115903A

    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 [1].
    <em>HIF-1</em>α-IN-2 hydrochloride
  • HY-115903

    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 [1].
    <em>HIF-1</em>α-IN-2
  • HY-149635

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1α-IN-6 (compound 3s) is a HIF-1α inhibitor with IC50 values of 0.6 and 53.3 nM observed in MiaPaCa-2 and MDA-MB-231 cells. HIF-1α-IN-6 can inhibit HIF-1α expression by decreasing the level of HIF-1α mRNA [1].
    <em>HIF-1</em>α-IN-6
  • 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 [1].
    <em>HIF-1</em>α-IN-7
  • HY-147813

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1α-IN-3 (Compound (S)-3f) is a hypoxia-selective HIF-1α inhibitor. HIF-1α-IN-3 shows strong antiestrogenic potency [1].
    <em>HIF-1</em>α-IN-3
  • 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 [1].
    <em>HIF-1</em>α-IN-4
  • 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 [1].
    <em>HIF-1</em>α-IN-5
  • 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 [1].
    Dimethyl-bisphenol A
  • 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 [1].
    <em>HIF</em>-IN-<em>1</em>
  • HY-16031B

    NSC710464 dihydrochloride

    HIF/HIF Prolyl-Hydroxylase Cancer
    AFP464 (dihydrochloride) (NSC710464 (dihydrochloride)) is the hydrochloride form of AFP464 and is a potent HIF-1α inhibitor with an IC50 value of 0.25 μM. It is also an activator of aryl hydrocarbon receptor (AhR).
    AFP464 dihydrochloride
  • 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 [1] .
    FM19G11
  • 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 [1].
    <em>HIF</em>-<em>1</em> inhibitor-4
  • HY-146540

    HIF/HIF Prolyl-Hydroxylase Apoptosis MDM-2/p53 Cancer
    GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth [1].
    GEM-5
  • HY-142693

    HIF/HIF Prolyl-Hydroxylase Metabolic Disease
    Angiogenesis agent 1 (compound C-31) is a salidroside-derivated glycoside analogue. Angiogenesis agent 1 is an activator of the HIF-1α pathway. Angiogenesis agent 1 has the potential for the research of diabetic hind limb ischemia [1].
    Angiogenesis agent <em>1</em>
  • HY-110266
    GN44028
    4 Publications Verification

    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 [1] .
    GN44028
  • HY-12519
    Oltipraz
    10+ 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-12519S

    RP 35972-d3; NSC 347901-d3

    Isotope-Labeled Compounds HIF/HIF Prolyl-Hydroxylase HIV Keap1-Nrf2 Cancer
    Oltipraz-d3 is the deuterium labeled Oltipraz. 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-d3
  • HY-P5915

    HIF/HIF Prolyl-Hydroxylase Cancer
    FAM-DEALA-Hyp-YIPMDDDFQLRSF-NH2, a 5-FAM labeled HIF-1α peptide, is a substrate of VHL. FAM-DEALA-Hyp-YIPMDDDFQLRSF-NH2 binds to VHL protein with a KD of 3 nM. Ex/Em (λ) = 485/520 nm [1].
    FAM-DEALA-Hyp-YIPMDDDFQLRSF-NH2
  • HY-N2425

    Cholinesterase (ChE) Metabolic Disease
    Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC50 for CYP2D6 is 0.761 μM, and the Ki is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system [1]
    Rhodiosin
  • HY-122094

    HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease Cancer
    Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. Steppogenin can be sued for the research of angiogenic diseases, such as those involving solid tumors [1].
    Steppogenin
  • HY-N0242
    Fraxinellone
    1 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 [1].
    Fraxinellone
  • HY-156106

    PROTACs Ligands for E3 Ligase HIF/HIF Prolyl-Hydroxylase Cancer
    VHL-IN-1 (compound 30) is a ubiquitin E3 ligase von Hippel-Lindau (VHL) inhibitor (dissociation constant Kd=37 nM) that stabilizes and induces HIF-1α transcriptional activity. VHL-IN-1 has potential as a HIF-1α stabilizer and degrader of proteolytically targeted chimeras (PROTACs) [1].
    VHL-IN-<em>1</em>
  • HY-P1888A

    HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease
    HIF-1 alpha (556-574) TFA is a short hypoxia-inducible factor-1 (HIF-1) 19 residues fragment. HIF-1 functions as master regulator of response to oxygen homeostasis [1].
    <em>HIF-1</em> alpha (556-574) (TFA)
  • HY-P10223

    HIF/HIF Prolyl-Hydroxylase Cancer
    Cyclo CRVIIF 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 65 and 123 μM, respectively [1].
    Cyclo(CRVIIF)
  • HY-16560
    Camptothecin
    35+ Cited Publications

    Campathecin; (S)-(+)-Camptothecin; CPT

    Topoisomerase ADC Cytotoxin MicroRNA Influenza Virus Apoptosis Fungal Antibiotic Infection Cancer
    Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM [1]. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells .
    Camptothecin
  • 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 [1].
    Cyclo(CRLLIF)
  • HY-P10221

    HIF/HIF Prolyl-Hydroxylase Cancer
    Cyclo CKLIIF 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 2.6 and 2.2 μM, respectively [1].
    Cyclo(CKLIIF)
  • 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] .
    <em>1</em>,4-DPCA
  • HY-B0219
    Allopurinol
    4 Publications Verification

    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 [1] .
    Allopurinol
  • HY-B0219A
    Allopurinol sodium
    4 Publications Verification

    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 [1] .
    Allopurinol sodium
  • HY-B0413S
    Fenbendazole-d3
    2 Publications Verification

    HIF/HIF Prolyl-Hydroxylase Parasite Microtubule/Tubulin Antibiotic Infection
    Fenbendazole-d3 is a deuterium labeled Fenbendazole. Fenbendazole-d3 is a HIF-1α agonist and activates the HIF-1α-related GLUT1 pathway. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53[1][2][3][4].
    Fenbendazole-d3
  • HY-N0234
    Bavachinin
    2 Publications Verification

    7-O-Methylbavachin; Bavachinin A

    Amyloid-β PPAR HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC50 value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity. [1] .
    Bavachinin
  • HY-N10330

    HIF/HIF Prolyl-Hydroxylase VEGFR Cancer
    7-Hydroxyneolamellarin A is a natural product that could be derived from sponge Dendrilla nigra. 7-Hydroxyneolamellarin A is a potent hypoxia-inducible factor-1α (HIF-1α) inhibitor. 7-Hydroxyneolamellarin A attenuates the accumulation of hypoxia-inducible factor-1α (HIF-1α) protein and inhibits vascular epidermal growth factor (VEGF) transcriptional activity. 7-Hydroxyneolamellarin A can be used in research of cancer [1].
    7-Hydroxyneolamellarin A
  • HY-10231
    PX-478
    30+ 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 [1] .
    PX-478
  • HY-17412S

    Isotope-Labeled Compounds Antibiotic Others
    Minocycline-d6 hydrochloride is deuterated labeled Minocycline hydrochloride (HY-17412). Minocycline hydrochloride is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor [1].
    Minocycline-d6 hydrochloride
  • HY-16031

    NSC710464 free base

    HIF/HIF Prolyl-Hydroxylase Cancer
    AFP464 free base (NSC710464 free base), is an active HIF-1α inhibitor with an IC50 of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator.
    AFP464 free base
  • HY-N1098

    HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    Velutin is an aglycone extracted from Flammulina velutipes, with inhibitory activity against melanin biosynthesis. Velutin reduces osteoclast differentiation and down-regulates HIF-1α through the NF-κB pathway [1] .
    Velutin
  • HY-B0413
    Fenbendazole
    5 Publications Verification

    Parasite HIF/HIF Prolyl-Hydroxylase Microtubule/Tubulin Antibiotic Infection
    Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 [1].
    Fenbendazole
  • HY-119264A

    HIF/HIF Prolyl-Hydroxylase Ras Cancer
    PRLX-93936 dihydrochloride (Compound 16) is a HIF-1α inhibitor with anticancer activity. PRLX-93936 can inhibit the activated Ras pathway and can be used in the study of relapsed or refractory multiple myeloma [1] .
    PRLX-93936 dihydrochloride
  • 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-N0596

    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 [1] .
    Panaxadiol
  • HY-15468
    IOX2
    5+ Cited Publications

    HIF/HIF Prolyl-Hydroxylase Cancer
    IOX2 is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC50 of 22 nM. IOX2 regulates platelet function and arterial thrombosis by upregulating HIF-1α expression and inhibiting ROS production. IOX2 can be used in the study of thrombotic diseases [1] .
    IOX2
  • HY-15468A

    HIF/HIF Prolyl-Hydroxylase Cardiovascular Disease Cancer
    IOX2 sodium is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC50 of 22 nM. IOX2 sodium regulates platelet function and arterial thrombosis by upregulating HIF-1α expression and inhibiting ROS production. IOX2 sodium can be used in the study of thrombotic diseases [1] .
    IOX2 sodium
  • HY-P2324
    Gramicidin A
    1 Publications Verification

    Bacterial HIF/HIF Prolyl-Hydroxylase Antibiotic Infection Cancer
    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) [1] .
    Gramicidin A
  • HY-17412S1

    Isotope-Labeled Compounds Infection Neurological Disease Inflammation/Immunology Cancer
    Minocycline-d6 sulfate is deuterated labeled Minocycline (HY-17412A). Minocycline is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor that can penetrate the blood-brain barrier. Minocycline has bacteriostatic, anti-cancer, anti-inflammatory, neuroprotective properties and antidepressant effects.
    Minocycline-d6 sulfate
  • HY-107553

    HSP Apoptosis Cancer
    Chetomin, an active component of Chaetomium globosum, is a heat shock protein 90/hypoxia-inducible factor 1 alpha (Hsp90/HIF1α) pathway inhibitor. Chetomin is a potent, nontoxic non-small cell lung cancer cancer stem cells (NSCLC CSC)-targeting molecule [1].
    Chetomin
  • HY-N5136

    Apoptosis PI3K Akt mTOR Cancer
    Ruscogenin suppresses HCC metastasis by reducing the expression of MMP-2, MMP-9, uPA, VEGF and HIF-1α via regulating the PI3K/Akt/mTOR signaling pathway [1]. And Ruscogenin alleviates LPS-induced pulmonary endothelial cell apoptosis by su
    25(R,S)-Ruscogenin
  • HY-P2324A

    Antibiotic Bacterial Infection
    Gramicidin A (TFA) is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A (TFA) is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A (TFA) induces degradation of hypoxia inducible factor 1 α (HIF-1α) [1] .
    Gramicidin A TFA
  • HY-15205
    Ganetespib
    25+ Cited Publications

    STA-9090

    HSP Apoptosis Cancer
    Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3 [1] .
    Ganetespib

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