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HIF-α1

" in MedChemExpress (MCE) Product Catalog:

99

Inhibitors & Agonists

1

Screening Libraries

2

Fluorescent Dye

1

Biochemical Assay Reagents

10

Peptides

21

Natural
Products

6

Isotope-Labeled Compounds

2

Oligonucleotides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-111387
    IDF-11774
    5 Publications Verification

    HIF/HIF Prolyl-Hydroxylase Cancer
    IDF-11774 is a novel hypoxia-inducible factor α (HIFα)-1 inhibitor with an IC50 of 3.65 μM.
    IDF-11774
  • HY-B0639
    Amifostine
    5+ Cited Publications

    WR2721

    MDM-2/p53 HIF/HIF Prolyl-Hydroxylase Cancer
    Amifostine (WR2721) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine protects cells from damage by scavenging oxygen-derived free radicals. Amifostine reduces renal toxicity and has antiangiogenic action [1] .
    Amifostine
  • HY-B0639A
    Amifostine trihydrate
    5+ Cited Publications

    WR2721 trihydrate

    MDM-2/p53 HIF/HIF Prolyl-Hydroxylase Cancer
    Amifostine trihydrate (WR2721 trihydrate) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine trihydrate selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine trihydrate is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine trihydrate protects cells from damage by scavenging oxygen-derived free radicals. Amifostine trihydrate reduces renal toxicity and has antiangiogenic action [1] .
    Amifostine trihydrate
  • HY-110266
    GN44028
    5 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-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].
    HIF-IN-1
  • HY-13671
    LW6
    20+ 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-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].
    HIF-1α-IN-6
  • 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-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-P10221A

    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) TFA
  • 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-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) [1].
    HIF-1/2α-IN-2
  • HY-115903A
    HIF-1α-IN-2 hydrochloride
    1 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 [1].
    HIF-1α-IN-2 hydrochloride
  • HY-115903
    HIF-1α-IN-2
    1 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 [1].
    HIF-1α-IN-2
  • 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].
    HIF-1 inhibitor-4
  • HY-D2360

    HIF/HIF Prolyl-Hydroxylase HSP Cancer
    O-Carboranylphenoxyacetanilide is a HIF-1α inhibitor and inhibits HIF-1α activation. O-Carboranylphenoxyacetanilide inhibits transcriptional activity of HIF in HeLa cells (IC50: 0.74 μM). O-Carboranylphenoxyacetanilide inhibits HSP60 chaperone activity and HSP60 ATPase activity [1].
    O-Carboranylphenoxyacetanilide
  • 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].
    HIF-1α-IN-3
  • HY-164259

    HIF/HIF Prolyl-Hydroxylase Cancer
    AJM 290 is a Trx-1 inhibitor. AJM 290 is an inhibitor of the HIF-1α COOH-terminal transactivation domain, and blocks HIF-1 binding to DNA [1].
    AJM 290
  • 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].
    HIF-1α-IN-7
  • 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-N0242
    Fraxinellone
    2 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

    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-1
  • HY-139804

    Epigenetic Reader Domain Histone Acetyltransferase HIF/HIF Prolyl-Hydroxylase Cancer
    CTK7A is a curcumin derivative with anticancer activity by inhibiting the HAT activity of p300 and reducing the autoacetylation of p300, thereby affecting its interaction with HIF-1α. The inhibition of CTK7A leads to decreased HIF-1α accumulation and activity, which can be used for cancer treatment research [1].
    CTK7A
  • 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].
    HIF-1α-IN-4
  • HY-18371

    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 [1] .
    TC-S 7009
  • 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-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].
    HIF-1α-IN-5
  • HY-151341

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1/2α-IN-1 is an orally active HIF-2α inhibitor. HIF-1/2α-IN-1 inhibits HIF-2α activity with an IC50 value of 0.92 μM. HIF-1/2α-IN-1 also can decrease HIF-1α levels. HIF-1/2α-IN-1 can be used for the research of clear cell renal cell carcinoma (ccRCC) [1].
    HIF-1/2α-IN-1
  • 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-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-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 [1].
    cyclo(CLLFVY)
  • HY-N0242R

    PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT Inflammation/Immunology Cancer
    Fraxinellone (Standard) is the analytical standard of Fraxinellone. This product is intended for research and analytical applications. 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 (Standard)
  • HY-158826

    RO 707179

    HIF/HIF Prolyl-Hydroxylase Cancer
    EZN-2968 is an antisense oligonucleotide that specifically binds and inhibits the expression of HIF-1α mRNA. EZN-2968, inhibits tumor cell growth.
    EZN-2968
  • 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-18259

    HIF/HIF Prolyl-Hydroxylase Cancer
    103D5R (Compound 15) is an inhibitor for the activation of hypoxia-inducible factor-1 (HIF-1) with an IC50 of 35 µM, through reduction of the HIF-1α protein synthesis. 103D5R inhibits the proliferation of LN229 with IC50 of 26 µM [1].
    103D5R
  • HY-10231
    PX-478
    40+ 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-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-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-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) .
    Gramicidin A
  • HY-15893
    DMOG
    45+ 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 [1]. 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-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-B0219
    Allopurinol
    5+ 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 [1] .
    Allopurinol
  • 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-B0219A
    Allopurinol sodium
    5+ 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 [1] .
    Allopurinol sodium
  • 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-N6782
    Oligomycin
    45+ Cited Publications

    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 [1] .
    Oligomycin
  • 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-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) .
    Gramicidin A TFA

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