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(79)
Angiogenesis Filter
Angiogenesis Chromatin/EpigeneticAMPK
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Aurora Kinase
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DNA Methyltransferase
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Epigenetic Reader Domain
(297)
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HIF
(64)
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(72)
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(42)
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(83)
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(203)
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HIF
Hypoxia-inducible factor 1-alpha, also known as HIF-1-alpha, is a subunit of a heterodimeric transcription factor hypoxia-inducible factor 1 (HIF-1) that is encoded by the HIF1A gene. It is a basic helix-loop-helix PAS domain containing protein, and is considered as the master transcriptional regulator of cellular and developmental response to hypoxia. The dysregulation and overexpression of HIF1A by either hypoxia or genetic alternations have been heavily implicated in cancer biology, as well as a number of other pathophysiologies, specifically in areas of vascularization and angiogenesis, energy metabolism, cell survival, and tumor invasion. Two other alternative transcripts encoding different isoforms have been identified.
Deferoxamine
Cited
T12435870-51-9
Deferoxamine（Desferrioxamine B） is an iron chelator (binds Fe(III) and many other metal cations) that inhibits neuronopathy, may be used to modify the reduction of iron accumulation and deposition in tissues, and may improve neurological dysfunction by inhibiting ferroptosis and neuroinflammation following traumatic brain injury.Desferrioxamin-B has antioxidant, antiproliferative, Deferoxamine has antioxidant, antiproliferative, and antitumor activities, and can induce HIF-1α production, apoptosis and autophagy in cancer cells.Desferrioxamin-B can be used in the treatment of acute iron toxicity and COVID-19 related diseases.
- $64
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CitedBelzutifan
T166791672668-24-4
Belzutifan (MK-6482) is a potential treatment for clear cell renal cell carcinoma (ccRCC). Belzutifan is an orally active and selective HIF-2α inhibitor (IC50: 9 nM). Belzutifan , as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile.
- $64
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PT2399
T12675L1672662-14-4
PT2399 shows effective antitumor activity in vivo. PT2399 is an effective and selective HIF-2α antagonist, which directly binds to the HIF-2α PAS B domain (IC50: 6 nM).
- $100
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Oligomycin Cited
T214941404-19-9
Oligomycin is an antifungal antibiotic that is an inhibitor of H+-ATP synthetase. The Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibited HIF-1alpha expression in hypoxic tumor cells.
- $42
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CitedPX-478 Cited
T6961685898-44-6
PX-478 is a HIF-1α inhibitor with selectivity, oral activity, and blood-brain barrier permeability. PX-478 has antitumor activity and also protects pancreatic β-cell function in diabetes mellitus and is used in type 2 diabetes mellitus research.
- $48
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CitedDapagliflozin Cited
T2389461432-26-8
Dapagliflozin (BMS-512148) is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.
- $42
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CitedRoxadustat Cited
T2515808118-40-3
Roxadustat (FG-4592) is an orally bioavailable, hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI), with potential anti-anemic activity.
- $30
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CitedCephaeline
TN1480483-17-0
Cephaeline was highly active against protected primary CLL cells (relative IC50's 35nM ) and acted by repressing HIF-1α± and disturbing intracellular redox homeostasis.
- $189
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DMOG Cited
T193989464-63-1
DMOG (Dimethyloxalylglycine), an antagonist of the α-ketoglutarate cofactor, is an inhibitor for HIF prolyl hydroxylase.
- $47
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CitedTC-S 7009
T170091422955-31-4
TC-S 7009 is a potent and selective HIF-2α inhibitor (Kd: 81 nM) with significantly higher affinity for HIF-2α than HIF-1α (Kd >> 5μM). TC-S 7009 disrupts HIF-2α heterodimerization, reduces HIF-2α target gene expression, and diminishes DNA binding activity.
- $64
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PT-2385
T78481672665-49-4In house
PT-2385 is a selective inhibitor of HIF-2α with a dissociation constant (Kd) of less than 50 nM (Kd<50 nM).
- $61
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2-Methoxyestradiol Cited
T2220362-07-2
2-Methoxyestradiol (2-ME2) is an orally bioavailable estradiol metabolite with potential antineoplastic activity. 2-Methoxyestradiol inhibits angiogenesis by reducing endothelial cell proliferation and inducing endothelial cell apoptosis. This agent also inhibits tumor cell growth by binding to tubulin, resulting in antimitotic activity, and by inducing caspase activation, resulting in cell cycle arrest in the G2 phase, DNA fragmentation, and apoptosis.
- $50
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CitedCucurbitacin B Cited
T34046199-67-3
Cucurbitacin B (Cuc B) has profound in vitro and in vivo antiproliferative effects against human pancreatic Y cells. It inhibited AKT signaling activation through up-regulation of PTEN. Cucurbitacin B is an effective inhibitor of HIF-1 and provide new perspectives into the mechanism of its anticancer activity. Cucurbitacin B inhibits proliferation and induces apoptosis via STAT3 pathway inhibition in A549 lung Y cells.
- $44
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CitedDemethyleneberberine
T4S080025459-91-0
Demethyleneberberine, which is composed of a potential antioxidant structure, could penetrate the membrane of mitochondria and accumulate in mitochondria either in vitro or in vivo.Demethyleneberberine suppresses CYP2E1, hypoxia inducible factor α, and inducible nitric oxide synthase, which contributes to oxidative stress and restored sirtuin 1 AMP-activated protein kinase peroxisome proliferator-activated receptor-γ coactivator-1α pathway-associated fatty acid oxidation in chronic ethanol-fed mice.
- $61
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Lificiguat Cited
T4381170632-47-0
Lificiguat (YC-1) is an nitric oxide (NO)-independent activator of soluble guanylyl cyclase(sGC) and an inhibitor of Hypoxia-inducible factor-1alpha (HIF-1alpha).
- $43
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CitedKC7F2 Cited
T3169927822-86-4
KC7F2 is a potent HIF-1 pathway inhibitor with potential anti-cancer activity.
- $43
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CitedML228
T78361357171-62-0In house
ML228 is a potent the Hypoxia Inducible Factor (HIF) pathway activator with EC50 of 1 μM. ML228 potently activates HIF in vitro as well as its downstream target VEGF.
- $37
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EL-102
T152051233948-61-2
EL-102 is a HIF1α inhibitor with anticancer activity that inhibits microtubule protein polymerization and can be used to study prostate cancer.
- $89
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Ganetespib Cited
T2309888216-25-9
Ganetespib (STA-9090) is a synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90), exhibiting potential antineoplastic activity.
- $61
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CitedHIF-1α-IN-2
T613492762315-06-8
HIF-1α-IN-2 is a novel and highly potent HIF-1α inhibitor with anticancer and antitumor activity that inhibits the expression of HIF-1α and VEGF in a dose-dependent manner and inhibits cell migration.
- $82
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Oltipraz
T015364224-21-1
Oltipraz (RP 35972) is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties. Oltipraz induces phase II detoxification enzymes, such as glutathione S transferase (GST) and NAD(P)H: quinone oxidoreductase 1 (NQO1). The induction of detoxification enzymes enhances the detoxification of certain cancer-causing agents, thereby enhancing their elimination and preventing carcinogen-induced DNA damages. Although the exact mechanism through which the anti-angiogenesis effect remains to be fully elucidated, oltipraz maybe able to modulate the expression of a number of angiogenic factors, thereby blocking the sustained and focal neovascularization in multiple tumor cell types.
- $31
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IDF-11774 Cited
T55371429054-28-3
IDF-11774 is a HIF-1 inhibitor.It reduces hif-1α HRE luciferase activity (IC50 = 3.65 μM).
- $55
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CitedBAY 87-2243 Cited
T24881227158-85-1
BAY 87-2243 is a potent and selective inhibitor of hypoxia-inducible factor-1 (HIF-1).
- $38
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CitedVadadustat
T46511000025-07-9
Vadadustat is a novel, titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor in development for the treatment of anemia.
- $42
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HIF-IN-1
T604132393928-76-0
HIF-IN-1 is a potent inhibitor of hypoxia-inducible factor (HIF-1), which is associated with tumor and cancer cell proliferation and inhibits HIF-1α protein aggregation.
- $69
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Acriflavine Hydrochloride
T198328063-24-9
Acriflavine Hydrochloride (Acriflavine HCl) is a HIF-1α inhibitor. It acts by targeting HIF-1α-mediated pathways and decreasing the level of PGK1, VEGF, and HIF-1α in vitro and in vivo.
- $41
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Pantoprazole sodium
T6929138786-67-1
Pantoprazole sodium (Pantecta) is the sodium salt form of a substituted benzimidazole with proton pump inhibitor activity. Pantoprazole sodium is a lipophilic, weak base that crosses the parietal cell membrane and enters the acidic parietal cell canaliculus where it becomes protonated, producing the active metabolite sulfenamide, which forms an irreversible covalent bond with two sites of the H+ K+-ATPase enzyme located on the gastric parietal cell, thereby inhibiting both basal and stimulated gastric acid production.
- $50
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HIF-1 inhibitor-4
T67767333357-56-5
HIF-1 inhibitor-4 (HIF-1 inhibitor-4) is a HIF-1 inhibitor with IC50 of 560 nM. HIF-1 inhibitor-4 reduces the HIF-1α protein level without affecting its mRNA level.
- $41
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AKB-6899
T297971007377-55-0In house
AKB-6899 is an inhibitor of prolyl hydroxylase domain 3 (PHD3) and increases the soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages. AKB-6899 leads to stabilization of HIF-2α which induces sVEGFR-1 production from tumor-associated macrophages and decreases tumor growth.
- $68
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HIF-2α agonist 2
T678312750141-15-0In house
HIF-2α agonist 2 is an HIF-2α agonist with an EC50 value of 1.68 μM for HIF-2α. HIF-2α agonist 2 can promote the stability of the ARNT A B ring in the 3z structure of HIF-2a-ARNT complex without cytotoxicity to 786-o-Reha-Luc cells. HIF-2α agonist 2 can be used in the study of oxygen metabolism and is closely related to the occurrence of cancer.
- $51
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VH-298 Cited
TQ01212097381-85-4
VH-298 is a potent inhibitor of VHL that stabilizes HIF-α and elicits a hypoxic response via a different mechanism, that is the blockade of the VHL:HIF-α protein-protein interaction downstream of HIF-α hydroxylation by PHD enzymes.
- $39
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CitedM1002
T61822823830-85-9In house
M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist that enhances the affinity of HIF-2alpha and ARNT for transcriptional activation. It alters the Tyr2 conformation of the HIF-2alpha PAS-B structural domain and acts synergistically with inhibitors of the prolyl hydroxylase structural domain (PHD).
- $44
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FM19G11
T36711329932-55-0
FM19G11 is an inhibitor of hypoxia inducible factor (HIF) α-subunit (IC50 = 80 nM in hypoxia induced luciferase assay).
- $43
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SYP-5
T130501384268-04-5
SYP-5 is a novel inhibitor of HIF-1, suppresses tumor cells invasion and angiogenesis.
- $30
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Naphthofluorescein
T3695361419-02-1
Naphthofluorescein （Naphthafluorescein） is a Mint3 inhibitor with potential antitumor and anti-inflammatory activities, inhibits the interaction between HIF-1 and Mint3, inhibits Mint3-dependent HIF-1 activity, and inhibits glycolytic activity in cancer cells and macrophages without showing significant in vitro cytotoxicity or in vivo side effects. Naphthofluorescein is also a fluorescent pH-sensitive probe for functional Cherenkov imaging.
- $44
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Adaptaquin
T22022385786-48-1
Adaptaquin is an inhibitor of the hypoxia-inducing factor prolyl hydroxylase (HIF-PH) [1] [2].
- $29
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HIF1-IN-3
T9890333314-79-7
HIF1-IN-3 (Benzenepropanamide, N-[(8-hydroxy-7-quinolinyl)(4-methoxyphenyl)methyl]-) is an effective inhibitor of HIF-1 (EC50 = 0.9 μM) and can be used in anticancer studies.
- $38
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ZINC13466751
T13398117953-17-0
ZINC13466751 is a potent HIF-1α/von Hippel-Lindau interaction inhibitor(IC50 of 2.0 µM).
- $41
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HIF-2α-IN-2
T115611672666-82-8
HIF-2α-IN-2 is a hypoxia-inducible factor (HIF-2α) inhibitor with an IC50 of 16 nM in scintillation proximity assay (SPA).
- $65
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2,4-DPD
T769241438-38-4
2,4-DPD is competitive inhibitor of the oxygen-sensing enzyme HIF-α prolyl hydroxylase (HIF-PH)
- $40
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THS-044
T1392562054-67-5
THS-044 (N-[2-Nitro-4-(Trifluoromethyl)phenyl]morpholin-4-Amine) binding stabilizes the HIF2α PAS-B folded state with a kd of 2 μM and regulates HIF2 activity in endogenous and clinical settings.
- $73
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GN44028
T153961421448-26-1
GN44028 (N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-1,4-dihydroindeno[1,2-c]pyrazol-3-amine) is a hypoxia-inducible factor inhibitor of (HIF)-1 (IC50: 14 nM). GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity. However, It can not be suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization.
- $64
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HIF-2α-IN-3
T11562313964-19-1
HIF-2α-IN-3 is a HIF-2α alteration inhibitor with anti-tumor properties and may be used in the study of cardiovascular disease.
- $117
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Acetylarenobufagin
T10233184673-79-8
Acetylarenobufagin is a steroidal hypoxia-inducible factor-1 (HIF-1) modulator.
- $105
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Daprodustat
T3197960539-70-2
Daprodustat (GSK1278863) is a HIF-prolyl hydroxylase inhibitor.
- $49
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