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Chromatin/Epigenetic

DNA Methyltransferase

(88)

Epigenetic Reader Domain

HIF/HIF Prolyl-Hydroxylase

(213)

Histone Acetyltransferase

(125)

Histone Demethylase

(196)

Histone Methyltransferase

Methionine Adenosyltransferase (MAT)

Metabolism

Acetyl-CoA Carboxylase

Amino Acids and Derivatives

Angiotensin-converting Enzyme (ACE)

Endogenous Metabolite

Glutathione Peroxidase

(80)

Glyoxalase

(17)

HIF/HIF Prolyl-Hydroxylase

Indoleamine 2,3-Dioxygenase (IDO)

(100)

Isocitrate Dehydrogenase (IDH)

Mitochondrial Metabolism

(221)

N-Acetylglucosaminyltransferase

Procollagen C Proteinase

(1)

Prolyl Endopeptidase (PREP)

Reactive Oxygen Species

Serine/threonin kinase

(91)

Stearoyl-CoA Desaturase (SCD)

HIF/HIF Prolyl-Hydroxylase

HIF prolyl-hydroxylase is an enzyme involved in the HIF (Hypoxia-inducible factor) signalling pathways, and is the target for a set of therapeutic drugs called HIF prolyl-hydroxylase inhibitors. Hypoxia-inducible factor (HIF) is an evolutionarily conserved transcription factor that allows the cell to respond physiologically to low concentrations of oxygen. A class of prolyl hydroxylases which act specifically on HIF has been identified; hydroxylation of HIF allows the protein to be targeted for degradation.

Filter HomeSignaling PathwaysChromatin/Epigenetic-MetabolismHIF/HIF Prolyl-Hydroxylase

Deferoxamine

Desferrioxamine B, Deferoxamine B

T12435870-51-9

Deferoxamine (Desferrioxamine B) is an iron chelator. Deferoxamine can be used to reduce the accumulation and deposition of iron in tissues. Deferoxamine can improve neurological dysfunction by inhibiting ferroptosis and neuroinflammation after traumatic brain injury. It has antioxidant, anti-proliferation and anti-tumor activities, and can induce the production of HIF-1α, apoptosis and autophagy in cancer cells. It can be used to treat acute iron toxicity and COVID-19 related diseases.

Akt Antioxidant Apoptosis Autophagy HIF HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species

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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.

Autophagy HIF HIF/HIF Prolyl-Hydroxylase

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Belzutifan

PT2977, MK-6482

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.

HIF HIF/HIF Prolyl-Hydroxylase

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Deferoxamine Mesylate

DFOM, Desferrioxamine B mesylate

T1637138-14-7

Deferoxamine Mesylate (DFOM) is an iron chelator and ferroptosis inhibitor. Deferoxamine Mesylate binds free iron into a stable complex and reduces iron accumulation. Deferoxamine Mesylate up-regulates HIF-1α levels and induces apoptosis.

Akt Apoptosis Autophagy Beta Amyloid Ferroptosis HIF/HIF Prolyl-Hydroxylase Mitophagy Reactive Oxygen Species

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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).

HIF HIF/HIF Prolyl-Hydroxylase

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Chloramphenicol

Levomycetin, Chloromycetin, Chlornitromycin

T120556-75-7

Chloramphenicol (Chloromycetin) is a broad-spectrum antibiotic that inhibits the biosynthesis of bacterial proteins. Chloramphenicol acts primarily on the 50S subunit of the bacterial 70S ribosome and is active against peptidyltransferases, inhibiting the formation of peptide bonds.

Akt Antibacterial Antibiotic Apoptosis Autophagy HIF/HIF Prolyl-Hydroxylase JNK MMP ribosome VEGFR

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Dendrophenol

Moscatilin

T3S1707108853-14-1

Dendrophenol (Moscatilin) is a natural product isolated from the stem of Dendrobium loddigesii Rolfe, act as a NF-κB inhibitor. Antineoplastic activity.

Apoptosis COX HIF/HIF Prolyl-Hydroxylase JNK NF-κB Wnt/beta-catenin

$106

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Chlorogenic Acid

NSC-407296, Heriguard, 3-O-Caffeoylquinic acid

T2805327-97-9

Chlorogenic acid is a natural phenol found in honeysuckle. Chlorogenic acid has a wide range of biological activities including anti-inflammatory, antioxidant, antitumor, antimicrobial, and neuroprotective.

Antibacterial Endogenous Metabolite HIF/HIF Prolyl-Hydroxylase Influenza Virus Reactive Oxygen Species

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Cucurbitacin B

DATISCACIN, Cuc B, Amarine

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.

Apoptosis Autophagy COX Endogenous Metabolite HIF HIF/HIF Prolyl-Hydroxylase Integrin PTEN ROS Kinase STAT

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Roxadustat

FG-4592, ASP1517

T2515808118-40-3

Roxadustat (FG-4592) is an orally bioavailable, hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI), with potential anti-anemic activity.

Ferroptosis HIF HIF/HIF Prolyl-Hydroxylase

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Amifostine

WR2721, Gammaphos, Ethyol

T328920537-88-6

Amifostine (Ethyol) anhydrous is a cytoprotective agent, acts as a free radical scavenging activity.

HIF/HIF Prolyl-Hydroxylase MDM-2/p53

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DMOG

Dimethyloxalylglycine, Dimethyloxaloylglycine, Dimethyloxallyl Glycine

T193989464-63-1

DMOG (Dimethyloxalylglycine), an antagonist of the α-ketoglutarate cofactor, is an inhibitor for HIF prolyl hydroxylase.

Autophagy HIF HIF/HIF Prolyl-Hydroxylase

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Astragaloside II

Astrasieversianin VIII

T392484676-89-1

Astragaloside II (Astrasieversianin VIII) is an effective MDR reversal agent and may be a potential adjunctive agent for hepatic cancer chemotherapy. Astragaloside II also induces osteogenic activities, differentiation, proliferation, and mineralization, through the bone morphogenetic protein-2/MAPK and Smad1/5/8 pathways.

Autophagy HIF/HIF Prolyl-Hydroxylase Interleukin NF-κB TGF-beta/Smad

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Minocycline hydrochloride

Minocycline HCl

T110113614-98-7

Minocycline hydrochloride (Minocycline HCl) is a tetracycline antibiotic with excellent absorption and tissue penetration that is used for several bacterial infections as well as treatment of acne. Minocycline hydrochloride can cause both an acute hepatitis-like syndrome occurring within 1 to 3 months of starting therapy or a more insidious chronic hepatitis with autoimmune features typically after long-term treatment.

Antibacterial Antibiotic Apoptosis Calcium Channel HIF/HIF Prolyl-Hydroxylase MDM-2/p53 Potassium Channel

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IOX2

JICL38, IOX 2

T1823931398-72-0

IOX2 (IOX 2) is a selective inhibitor of the Hypoxia Inducible Factor (HIF) Prolyl-Hydroxylases (PHD); active in cells with the IC50 value of 21 nM for PHD2/ELGN-1 and no inhibition at FIH (20uM).

HIF/HIF Prolyl-Hydroxylase

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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).

HIF HIF/HIF Prolyl-Hydroxylase

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AKBA

Acetyl-11-keto-β-boswellic acid, 3-O-Acetyl-11-keto-β-boswellic acid, 3-O-Acetyl-11-keto-beta-boswellic acid

T5S156967416-61-9

AKBA (3-O-Acetyl-11-keto-beta-boswellic acid), a natural component from frankincense, is a novel activator of Nrf2.

Endogenous Metabolite HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species

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LW6

LW8, HIF-1α inhibitor, CAY10585

T3494934593-90-5

LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor.

Apoptosis Dehydrogenase HIF HIF/HIF Prolyl-Hydroxylase

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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.

HIF HIF/HIF Prolyl-Hydroxylase

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KRH102140

KRH 102140

T68511864769-01-7

KRH102140 is a PHD2 activator that reduces angiogenesis by inhibiting HIF-1alpha, used in cardiovascular disease research.

HIF/HIF Prolyl-Hydroxylase

$330

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1,4-DPCA ethyl ester

T3679686443-19-8

1,4-DPCA ethyl ester is a form of 1,4-DPCA modified to ethyl ester, which has potential anticancer activity based on growth inhibition assays with the mlh1 rad18 yeast strain.

HIF/HIF Prolyl-Hydroxylase Others

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Deoxyshikonin

Arnebin 7

T5S234743043-74-9

1. Deoxyshikonin (Arnebin 7) may be a new drug candidate for wound healing and treatment of lymphatic diseases. 2. Deoxyshikonin enhances the ability of human dermal lymphatic microvascular endothelial cells (HMVEC-dLy) to undergo time-dependent in vitro cord formation. 3. Deoxyshikonin and dodecyl gallate show significantly synergic antimicrobial activity with penicillin in vivo and in vitro, and can effectively reduce nasopharyngeal and lung colonization caused by different penicillin-resistant pneumococcal serotypes.

Antibacterial Apoptosis HIF/HIF Prolyl-Hydroxylase PI3K

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