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PDE inhibitor
Dipyridamole (Persantine) is a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. - Disulfiram blocks the processing of alcohol in the body by inhibiting acetaldehyde dehydrogenase thus causing an unpleasant reaction when alcohol is consumed.
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
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carbonic anhydrase inhibitor
Dorzolamide HCl is a carbonic anhydrase inhibitor. It is an anti-glaucoma agent and topically applied in the form of eye drops. Dorzolamide HCl is used to lower increased intraocular pressure in open-angle glaucoma and ocular hypertension. -
Adenosine receptor antagonist
Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects. It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor. - Elesclomol induces oxidative stress by provoking a buildup of reactive oxygen species within cancer cells.
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ACE inhibitor
Enalapril is an angiotensin converting enzyme (ACE) inhibitor used in the treatment of hypertension and some types of chronic heart failure. -
RAAS inhibitor
Enalaprilat is the active metabolite of enalapril. It is the first dicarboxylate-containing ACE inhibitor and was developed partly to overcome these limitations of captopril. -
15-PGDH inhibitor
Glycyrrhetinic acid inhibits the enzymes (15-hydroxyprostaglandin dehydrogenase and delta-13-prostaglandin) that metabolize the prostaglandins PGE-2 and PGF-2α to their respective 15-keto-13,14-dihydro metabolites which are inactive. - Ezetimibe is a compound that lowers cholesterol. It acts by decreasing cholesterol absorption in the intestine. Ezetimibe localises at the brush border of the small intestine, where ezetimibe inhibits the absorption of cholesterol from the intestine.
- Nihei W, .et al. , J Lipid Res, 2018, Nov; 59(11): 2181-2187 PMID: 30242108
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xanthine oxidase inhibitor
Febuxostat is a non-purine inhibitor of xanthine oxidase (Ki = 1.2 nM). - Fenofibrate is a drug of the fibrate class. It is mainly used to reduce cholesterol levels in patients at risk of cardiovascular disease.
- Fludarabine or fludarabine phosphate (Fludara) is a chemotherapy drug used in the treatment of hematological malignancies (cancers of blood cells such as leukemias and lymphomas) .Fludarabine inhibits DNA synthesis by interfering with ribonucleotide reductase and DNA polymerase. It is active against both dividing and resting cells.
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STAT inhibitor
Fludarabine or fludarabine phosphate (Fludara) is a chemotherapy drug used in the treatment of hematological malignancies (cancers of blood cells such as leukemias and lymphomas) .Fludarabine inhibits DNA synthesis by interfering with ribonucleotide reductase and DNA polymerase. It is active against both dividing and resting cells.- Irene Dell'Anno, .et al. , Invest New Drugs, 2020, Dec 9 PMID: 33300108
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HMG-CoA reductase inhibitor
Fluvastatin sodium (XU 62320) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. -
CYP2D6 inhibitor
Haloperidol (Haldol) is an antipsychotic and butyrophenone. -
PDE4 inhibitor
Hesperetin, a selective phosphodiesterase (PDE)4 inhibitor, is present in the traditional Chinese medicine, ?€?Chen Pi.?€? Hesperetin is a citrus flavonoid that has been reported to lower plasma cholesterol. Hesperetin reduces the transcription of ACAT-2 mRNA in Hep-G2 cells and reduces ApoB protein synthesis in a dose-dependent manner. It also is a potential therapy for carcinoid cancer. - Hydroxocobalamin is a biologically active form of vitamin B12. It increases the number of red blood cells 2.5-fold over control in a mouse model of anemia when administered at a dose of 2 μg per day for 4 days.
- Rsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
- Isotretinoin was developed to be used as a chemotherapy medication for the treatment of brain cancer, pancreatic cancer and more.
- Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent.
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
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P450 inhibitor
As an antifungal, ketoconazole is structurally similar to imidazole, and interferes with the fungal synthesis of ergosterol, a constituent of fungal cell membranes, as well as certain enzymes. -
Dehydrogenase inhibitor
Leflunomide is a pyrimidine synthesis inhibitor belonging to the DMARD (disease-modifying antirheumatic drug) class of drugs. Leflunomide is used to relieve symptoms caused by rheumatoid arthritis, such as inflammation, swelling, stiffness, and joint pain. -
PDE4 inhibitor
Luteolin is a PDE4 inhibitor, phosphodiesterase inhibitor, and an interleukin 6 inhibitor, affecting xylazine/ketamine-induced anesthesia in mice. Luteolin acts as a monoamine transporter activator, and is one of the few chemicals demonstrated to possess this property. -
Hydroxylase Inhibitor
LX 1606 hippurate is an orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity. -
HnsPLA inhibitor
LY315920 (Varespladib) is an inhibitor of the IIa, V, and X isoforms of secretory phospholipase A2 (sPLA2).- Yap WH, .et al. , Mol Cell Biochem, 2018, Oct;447(1-2):93-101 PMID: 29374817
- Yamato Okita, .et al. , Infect Immun, 2016, Feb; 84(2): 573-579 PMID: 26644377
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PPARγ agonist
5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. - Methoxsalen (8-Methoxypsoralen) is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450).
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PDE3 inhibitor
Milrinone(Primacor) is a a potent and selective phosphodiesterase 3 inhibitor with an IC50 of 0.42 μM for the inhibition of FIII PDE -
IMPDH inhibitor
Mycophenolate mofetil is a reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH) in purine biosynthesis (specifically guanine synthesis) which is necessary for the growth of T cells and B cells. - Naringenin is a flavanone, a type of flavonoid, that is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, anti-inflammatory, carbohydrate metabolism promoter, and immune system modulator.
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dopamine beta-hydroxylase inhibitor
Nepicastat is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine. -
DHFR inhibitor
NSC 131463 is a dihydrofolate reductase potent inhibitor with an IC50 of 1 nM. -
HSP90 Inhibitor
AUY922 (NVP-AUY922) is highly potent and oral inhibitor of Hsp90 with IC50=21 nM in Hsp90 FP binding assay and inhibits proliferation of various human cancer cell lines in vitro, with GI50 average 9 nM.- Haruka Wakasa, .et al. , J Mammary Gland Biol Neoplasia, 2022, Jun;27(2):155-170 PMID: 35581442
- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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HSP90 Inhibitor
NVP-BEP800 is a novel, fully synthetic, orally bioavailable inhibitor that binds to the NH2-terminal ATP-binding pocket of Hsp90.- Hiroki Murano, .et al. , Plant Biotechnol Rep, 2017, 11:107-113
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ATPase inhibitor
Oligomycin A is a mitochondrial ATPase inhibitor. Oligomycin A inhibits ATP5 (mitochondrial ATPases, F1F0) bound to the cell membrane.- Makoto Kawatani, .et al. , ACS Chem Biol, 2021, 16, 8, 1576-1586
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FASN inhibitor
Orlistat is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice. Orlistat is also an inhibitor of fatty acid synthase (FASN), is used orally for long-term research of obesity. Anti-atherosclerotic effect.
- M Sugihara, .et al. , J Cell Biol, 2019, pii: jcb.201712120 PMID: 30705059
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TXAS inhibitor
Ozagrel is a potent and selective thromboxane A2 synthetase inhibitor with an IC50 of 4 nM. -
DHFR inhibitor
Pemetrexed disodium is chemically similar to folic acid and is in the class of chemotherapy drugs called folate antimetabolites. It works by inhibiting three enzymes used in purine and pyrimidine synthesis?€?thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase.- Adi Jacob Berger, .et al. , Nat Cancer, 2021, 2, 1055-1070 PMID: 35121883
- Perindopril Butylamine Salt is an angiotensin-converting enzyme (ACE) inhibitor.
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PDE inhibitor
Pimobendan (Vetmedin) is a calcium sensitizer with positive inotropic and vasodilator effects. It is also a selective inhibitor of phosphodiesterase III (PDE3). -
HMG-CoA reductase inhibitor
Pitavastatin Calcium is a competitive inhibitor of the enzyme HMGCR (HMG-CoA reductase) results in a reduction in LDL cholesterol synthesis.- Weizhen Chen, .et al. , Biomaterials, 2021, 280:121260 PMID: 34823885
- Karis Tutuska, .et al. , Cell Death Dis, 2020, Apr; 11(4): 274 PMID: 32332697
- D Jarmuzek, .et al. , J Photochem Photobiol A Chem, 2019, November
- Marwan Ibrahim Abdullah, .et al. , Sci Rep, 2017, 7: 8090 PMID: 28808351
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PLA inhibitor
Polydatin protects cerebral cells from ischemic damages via improvement of microcirculation and inhibition of platelet aggregation. In addition, polydatin inhibits ICAM-1 expression in endothelial cells stimulated by lipopolysaccharide; it also attenuates adhesion between white blood cells and endothelial cells.- Darshika Pathiraja, .et al. , Food Chem, 2023, May 1;407:135145 PMID: 36521391
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CYP3A4 inhibitor
Posaconazole is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14?? demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours. - Prednisolone is a glucocorticoid with the general properties of the corticosteroids.
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MAO-B inhibitor
Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C. -
MAO-B inhibitor
Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.