Prolyl-4-hydroxylase Inhibitor 11, a novel proline 4-hydroxylase inhibitor, shows protective effects against oxidative stress and Cu(II) toxicity in Chlorella vulgaris.

Collagen proline hydroxylase inhibitor-1 exhibits antifibroproliferative activity.

Cholesterol 24-hydroxylase-IN-1 is an orally active, selective, and potent inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1) that crosses the blood-brain barrier.Cholesterol 24-hydroxylase-IN-1 may be useful in the study of epilepsy-like neurological disorders. Cholesterol 24-hydroxylase-IN-1 is used to study epilepsy-like neurological diseases.

Collagen proline hydroxylase inhibitor is an inhibitor collagen proline hydroxylase and useful for antifibrotic proliferative agents.

Cholesterol 24-hydroxylase-IN-2 is a potent inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1), exhibiting an IC50 value of 5.4 nM, and has potential applications in mammalian imaging of this enzyme [1].

Prolyl Hydroxylase inhibitor 1 is an orally active inhibitor of hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) (IC50 of 62.23 nM).

Lysyl Hydroxylase 2-IN-1 (compound 12) is a selective inhibitor of lysyl hydroxylase 2 (LH2) with an IC50 of approximately 300 nM and demonstrates specificity for LH2 over LH1 and LH3 [1].

Lysyl Hydroxylase 2-IN-2 (compound 13) is a potent inhibitor of Lysyl Hydroxylase 2 (LH2), exhibiting an IC50 of approximately 500 nM. It effectively inhibits cell migration in 344SQ WT cells without affecting the migration of LH2 knockout cells [1].

Cytochrome P450 2C9 is a cytochrome P-450 subtype that possesses specificity for acidic xenobiotics. It oxidizes a wide range of important clinical drugs under the categories of nonsteroidal anti-inflammatory agents, anticoagulants, hypoglycemic agents, a

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.

Syrosingopine has selective depleting effect on brain amines is potentiated by combined treatment with disulfiram or fusaric acid, a dopamine beta-hydroxylase inhibitor.

Osilodrostat (LCI699) (LCI699) is an effective inhibitor of human 11β-hydroxylase (IC50: 2.5 nM) and aldosterone synthase (IC50: 0.7 nM).

1. Hypericin (Cyclosan) has antineoplastic activity. 2. Hypericin has antibiotic and antiviral activities. 3. Hypericin has antidepressive activity through inhibiting monoamine oxidase enzyme. 4. Hypericin inhibits RANKL-mediated osteoclastogenesis via affecting ERK signalling in vitro and suppresses wear particle-induced osteolysis in vivo.

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.

Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) effectively inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation, and anti-tumor effects. Hydroxycitric acid tripotassium hydrate(Potassium citrate monohydrate) (Potassium citrate monohydrate) is the major active ingredient of Garcinia cambogia and a derivative of citric acid. Hydroxycitric acid tripotassium hydrate(Potassium citrate monohydrate) competitively inhibits ATP citrate lyase with weight loss benefits.

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.

Carbidine (Carbidin) is a derivative of gamma-carboline, an atypical antipsychotic drug. It reduces the inhibitory effect of DA on the 3H-DA release from synaptosomes of the nucleus accumbens septi and on the activity of tyrosine hydroxylase in vivo and in vitro.

α-Hydroxyglutaric Acid Lithium, converted from glutamate in microorganisms and animals, is an inhibitor of α-ketoglutarate-dependent dioxygenase and 5-methylcytosine hydroxylase, and has an inhibitory effect on ATP synthase and mTOR signaling.

4-Methylhistamine hydrochloride has been shown to inhibit the activity of copper-dependent enzymes such as tyrosinase and dopamine beta-hydroxylase and has also been shown to modulate the expression of genes involved in cell cycle regulation and apoptosis.

Bupicomide is a dopamine beta hydroxylase inhibitor with antihypertensive and vasodilatory activity that reduces 14C-norepinephrine biosynthesis of 14C-dopamine and can be used to study hypertension.

Guanoclor (VATENSOL) (INN), also known as guanochlor, is a sympatholytic drug. It is known to bind to non-adrenergic sites in pig kidney membranes.

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.

1,4-DPCA is an inhibitor of prolyl-hydroxylase with an IC50 of 2.4 µM for collagen hydroxylation in human foreskin fibroblasts and 60 μM for factor inhibiting HIF (FIH).

M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist that enhances the affinity of HIF-2alpha and ARNT for transcriptional activation.M1002 alters the Tyr2 conformation of the HIF-281alpha PAS-B structural domain and acts synergistically with inhibitors of the prolyl hydroxylase structural domain (PHD).

Diethyl-pythiDC is an collagen prolyl 4-hydroxylase inhibitor.

PT-2385 is a selective HIF-2α inhibitor (Kd<50 nM).

p-Ethynylphenylalanine (4-Ethynyl-L-phenylalanine), a tryptophan hydroxylase (TPH) inhibitor, is competitive, effective, selective, and reversible, with a Ki of 32.6 μM.

Rhapontigenin (Protigenin) is a mechanism-based, selective inactivator of cytochrome P450 1A1 (IC50: 400 nM), an aryl hydrocarbon hydroxylase which activates polycyclic aromatic hydrocarbons that act as procarcinogens. Rhapontigenin is a natural analog of resveratrol with antioxidant and anti-cancer activity. At higher concentrations, rhapontigenin inhibits the proliferation of HL-60R and HepG2 cancer cell lines (IC50: 48 μM).

Galeterone (VN 124) is an orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both 17alpha-hydroxylase and 17, 20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens.

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.

Abiraterone (CB-7598) (CB-7598) is an effective steroidal cytochrome P450 17alpha-hydroxylase-17, 20-lyase (CYP17) inhibitor (IC50: 4 nM).

IDF-11774 is a HIF-1 inhibitor.It reduces hif-1α HRE luciferase activity (IC50 = 3.65 μM).

BAY 87-2243 is a potent and selective inhibitor of hypoxia-inducible factor-1 (HIF-1).

Abiraterone Acetate (CB7630) is an androstene derivative that inhibits STEROID 17-ALPHA-HYDROXYLASE and is used as an ANTINEOPLASTIC AGENT in the treatment of metastatic castration-resistant PROSTATE CANCER.

Chlorogenic acid, as a major phenolic compound in honeysuckle, possesses potential antioxidant, antibacterial, anti-inflammatory, and anticancer activities. It can be utilized in research related to the treatment of advanced cancer and impaired glucose tolerance.

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

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

KC7F2 is a potent HIF-1 pathway inhibitor with potential anti-cancer activity.

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.

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

Chloramphenicol (Chloromycetin), a broad-spectrum antibiotic, blocks bacterial protein synthesis.

Ketoconazole (R-41400), a CYP3A4 inhibitor, is an imidazole anti-fungal agent.

1. Oroxylin A (Baicalein 6-methyl ether) has various anti-tumor effects including apoptosis, cell cycle arrest, drug-resistant reversion. 2. Oroxylin A possesses abilities of inhibiting the ATRA-induced IL-6 production via modulation of LAP/LIP/CHOP in leukemia cell lines, which could providing a therapeutic strategy for RAS. 3. Oroxylin A inhibits UCP2s triggers the MPTP opening, and promotes the apoptosis in CaCo-2 cells; uncoupling protein 2 plays a key role in mitochondrial apoptotic pathway. 4. Oroxylin A inhibits N1ICD translocating to the nucleus and binding to epithelial-mesenchymal transition-related transcription factor Snail, thus suppressing the invasion and migration of MCF-7 cells. 5. Oroxylin A improves the sensitivity of K562/ADM cells by increasing apoptosis in leukemic cells and decreasing the expression of CXCR4 and PI3K/Akt/NF-κB pathway, and probably served as a most promising agent for CML treatment.

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

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.

4-Chloro-L-phenylalanine (L-PCPA) is an inhibitor of 5-HT biosynthesis.4-Chloro-L-phenylalanine is also a non-specific antagonist of tryptophan hydroxylase (TPH1 and TPH2).

3-Chlorophenylboronic acid, a phenylboronic acid derivative, is an important intermediate in the synthesis of prolyl hydroxylase inhibitors, and can be used to synthesize a variety of compounds.The IC50 of 3-Chlorophenylboronic acid for lysophospholipase LYPLA2 was 0.418 µM.

Calcifediol-D6 is the deuterated form of Calcifediol, which is a prehormone that is produced in the liver by hydroxylation of vitamin D3 by the enzyme cholecalciferol 25-hydroxylase.

2,4-Dihydroxypyrimidine-5-carboxylic acid (Isoorotic acid) has been obtained from 5-formyluracil by the action of enzyme, thymine 7-hydroxylase. 2,4-Dihydroxypyrimidine-5-carboxylic acid has been used to synthesize N1-alkylated uracil derivatives.

Adaptaquin is an inhibitor of the hypoxia-inducing factor prolyl hydroxylase (HIF-PH) [1] [2].