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Chromatin/Epigenetic

DNA Methyltransferase

(45)

Epigenetic Reader Domain

HIF/HIF Prolyl-Hydroxylase

(82)

Histone Acetyltransferase

(51)

Histone Demethylase

(96)

Histone Methyltransferase

Methionine Adenosyltransferase (MAT)

Metabolism

Acetyl-CoA Carboxylase

Amino Acids and Derivatives

Angiotensin-converting Enzyme (ACE)

Endogenous Metabolite

Glutathione Peroxidase

(43)

Glyoxalase

(2)

HIF/HIF Prolyl-Hydroxylase

Indoleamine 2,3-Dioxygenase (IDO)

(36)

Isocitrate Dehydrogenase (IDH)

Mitochondrial Metabolism

(104)

N-Acetylglucosaminyltransferase

Procollagen C Proteinase

(1)

Prolyl Endopeptidase (PREP)

Reactive Oxygen Species

Serine/threonin kinase

(48)

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

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.

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Deferoxamine 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.

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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.

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Chloramphenicol

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.

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DMOG

T193989464-63-1

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

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Minocycline hydrochloride

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.

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Chlorogenic 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.

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IOX2

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).

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Amifostine

T328920537-88-6

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

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AKBA

T5S156967416-61-9

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

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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).

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LW6

T3494934593-90-5

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

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Enarodustat

T152191262132-81-9

Enarodustat (JTZ-951) is an orally active factor inhibitor of prolyl hydroxylase (EC50: 0.22 μM) and has the potential for renal anemia treatment.

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KRH102140

T68511864769-01-7

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

$330

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UNC6934

T95842561494-77-5

UNC6934 is a chemical probe targeting the N-terminal PWWP (PWWP1) domain of NSD2.

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Daprodustat

T3197960539-70-2

Daprodustat (GSK1278863) is a HIF-prolyl hydroxylase inhibitor.

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Glucosamine

T04293416-24-8

Glucosamine (Chitosamine) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids. Supplemental glucosamine may help to rebuild cartilage and treat arthritis.

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JNJ-42041935

T31801193383-09-3

JNJ-42041935 (HIF-PHD Inhibitor II) is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes.

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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.

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Molidustat

T26521154028-82-6

Molidustat (BAY 85-3934)(BAY-85-3934), an inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase (PH), stimulates erythropoietin (EPO) production and the formation of red blood cells.

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Deoxyshikonin

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.

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