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(82)
Angiogenesis Filter
Angiogenesis Chromatin/EpigeneticAMPK
(138)
Aurora Kinase
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DNA Methyltransferase
(45)
Epigenetic Reader Domain
(364)
HDAC
(267)
HIF
(66)
HIF/HIF Prolyl-Hydroxylase
(82)
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(51)
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(96)
Histone Methyltransferase
(245)
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(4)
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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
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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PX-478
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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Belzutifan
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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Roxadustat
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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Dapagliflozin
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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Oligomycin
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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dmog
T193989464-63-1
DMOG (Dimethyloxalylglycine), an antagonist of the α-ketoglutarate cofactor, is an inhibitor for HIF prolyl hydroxylase.
- $32
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Cucurbitacin B
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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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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Ganetespib
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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TC-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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2-Methoxyestradiol
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.
- $37
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Daprodustat
T3197960539-70-2
Daprodustat (GSK1278863) is a HIF-prolyl hydroxylase inhibitor.
- $33
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Vadadustat
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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Demethyleneberberine
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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Cephaeline
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.
- $148
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HIF-2α-IN-1
T154821799948-06-3
HIF-2α-IN-1 is a potent inhibitor of HIF-2α, with IC50 values below 500 nM.
- $100
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BAY 87-2243
T24881227158-85-1
BAY 87-2243 is a potent and selective inhibitor of hypoxia-inducible factor-1 (HIF-1).
- $30
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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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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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HIF-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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KC7F2
T3169927822-86-4
KC7F2 is a potent HIF-1 pathway inhibitor with potential anti-cancer activity.
- $43
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