Other inhibitors

Acipimox is a niacin derivative used as a hypolipidemic agent.

Thiamet G is a potent, selective O-GlcNAcase inhibitor with Kiof 21 nM, while exhibiting 37,000-fold selectivity over human lysosomal-hexosaminidase.

Ursolic acid(Malol) is a pentacyclic triterpene acid, used in cosmetics, that is also capable of inhibiting various types of cancer cells by inhibiting the STAT3 activation pathway and human fibrosarcoma cells by reducing the expression of matrix metalloproteinase-9 by acting through the glucocorticoid receptor.

Telavancin is a semi-synthetic vancomycin analogue prepared by the addition of a decylaminoethyl moiety to the free amino group of the disaccharide.

GC376 is a 3CLpro inhibitor (3C-like protease inhibitor).

(S)-Reticuline is the (S)-enantiomer of Reticuline. An enantiomer of a tetrahydrobenzylisoquinoline alkaloid. Reticuline is a chemical compound found in a variety of plants including Lindera aggregata, Annona squamosa, and Ocotea fasciculata.

Heparin, also known as unfractionated heparin, a highly sulfated glycosaminoglycan, is widely used as an injectable anticoagulant, and has the highest negative charge density of any known biological molecule.

Bergenin (Cuscutin) is an isocoumarin isolated from various medicinal plants. Shows mild anti-HIV activity, antihepatotoxic activity and antiulcer activity.

ST 2825 is a MyD88 pharmacologic inhibitor.

Treprostinil is a stable analog of prostacyclin that is used clinically for the treatment of PPH.

ANX-510 is a folate-based biomodulator with potential antineoplastic activity. 5,10-methylenetetrahydrofolate (MTHF) stabilizes the covalent binding of the fluorouracil metabolite 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate (FdUMP) to its target enzyme, thymidylate synthase, which results in inhibition of thymidylate synthase, depletion of thymidine triphosphate (TTP), a necessary constituent of DNA, and tumor cell death. Unlike leucovorin, MTHF, as the active form of folate, does not require metabolic activation and may increase the chemotherapeutic effects of fluorouracil with lower toxicity.

EC-17 is a conjugate consisting of fluorescein isothiocyanate (FITC) conjugated with folate with potential antineoplastic activity.

Chlorin E6 is a natural molecule and a promising photosensitizer.

Oxymatrine (Matrine N-oxide) is one of components of the root of Sophora flavescens.

Photochlor is a lipophilic, second-generation, chlorin-based photosensitizer. Upon intravenous administration, HPPH selectively accumulates in the cytoplasm of cancer or pre-cancerous cells.

Arbidol is an antiviral treatment for influenza infection used in Russia and China. Arbidol inhibits membrane fusion. Arbidol prevents contact between the virus and target host cells. Fusion between the viral capsid and the cell membrane of the target cell is inhibited. This prevents viral entry to the target cell, and therefore protects it from infection.

Glycyrrhizic acid is a widely used anti-inflammatory agent isolated from the licorice root.

Nimorazole is a nitroimidazole anti-infective. It is also being investigated for the treatment of head and neck cancer.

Gramine is a naturally occurring indole alkaloid present in several plant species. Gramine may play a defensive role in these plants, since it is toxic to many organisms. It is used mostly in synthetic organic chemistry as a starting material for tryptophan syntheses.

Pirodavir was one of the most promising capsid-binding compounds to show efficacy in human clinical trials for chemoprophylaxis of the common cold.

Chlorogenic acid is an important intermediate in lignin biosynthesis. This compound, long known as an antioxidant, also slows the release of glucose into the bloodstream after a meal.

Daidzein structurally belongs to the group of isoflavones. Daidzein can be converted to its end metabolite S-equol in some humans based on the presence of certain intestinal bacteria. Based on several decades of research, S-equol has potential for significant health benefits.

NB-598 is a potent competitive inhibitor of squalene epoxidase (SE). NB-598 suppresses triglyceride biosynthesis through the farnesol pathway.

Telithromycin is a ketolide antibiotic. It is used to treat community acquired pneumonia of mild to moderate severity. Telithromycin prevents bacteria from growing, by interfering with their protein synthesis. Telithromycin binds to the subunit 50S of the bacterial ribosome, and blocks the progression of the growing polypeptide chain.

Sesamin is a lignan isolated from the bark of Fagara plants and from sesame oil.

TP-434 is a novel, broad-spectrum fluorocycline antibiotic with activity against bacteria expressing major antibiotic resistance mechanisms including tetracycline-specific efflux and ribosomal-protection.

Salinomycin (Procoxacin) is an antibacterial and coccidiostat ionophore therapeutic agent.

Limonin is a limonoid, and a bitter, white, crystalline substance found in citrus and other plants. It is also known as limonoate D-ring-lactone and limonoic acid di-delta-lactone.

Cyclosporin H is a TPA/PMA inhibitor and a selective inhibitor of formyl peptide receptors (Ki = 0.1 uM).

Iopromide is a nonionic, injectable radio-contrast medium.

Methazolastone is a DNA damage inducer.

BAPTA is a selective calcium chelator.

Atopaxar hydrobromide shows potent inhibitory effects on human platelet aggregation induced by thrombin and TRAP with IC values of 0.064 and 0.031 μM respectively.

Natamycin (Pimaricin) is a naturally occurring antifungal agent produced during fermentation by the bacterium Streptomyces natalensis, commonly found in soil.It is used to treat fungal infections.

Doripenem (doripenem monohydrate) is an ultra-broad spectrum injectable antibiotic. It is a beta-lactam and belongs to the subgroup of carbapenems. It is particularly active against Pseudomonas aeruginosa.

SKQ1 is a potent mitochondria-targeted antioxidant. SKQ1 is also an API (active pharmaceutical ingredient) for making eye drop drug called Visomitin. SKQ1 showed activities (1) to prevent amyloid-beta-induced impairment of long-term potentiation in rat hippocampal slices.

Metformin hydrochloride is a biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification.

Oxytetracycline(Terramycin) was the second of the broad-spectrum tetracycline group of antibiotics to be discovered.

D-cycloserine is a partial agonist at the glycine receptor, and has been shown to have cognition-enhancing properties for models of Parkinsons disease in primates.

Exherin is a small, cyclic pentapeptide vascular-targeting agent with potential antineoplastic and antiangiogenic activities.

T-5224 is a selective inhibitor of c-Fos/activator protein-1.

RC-3095 is a bombesin/gastrin-releasing peptide (BN/GRP) antagonist with potential anticancer activity.

Quinidine is a dextrorotatory stereoisomer of quinine with antimalarial and antiarrhythmic properties.

Quarfloxin (CX-3543) is a fluoroquinolone derivative with antineoplastic activity. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template, a critical interaction for rRNA biogenesis that is overexpressed in cancer cells; disruption of this G-quadruplex DNA:protein interaction in aberrant rRNA biogenesis may result in the inhibition of ribosome synthesis and tumor cell apoptosis.

Rhein is a substance in the anthraquinone group found in rhubarb species like Rheum undulatum or Rheum palmatum or in Cassia reticulata.

Ibutamoren mesylate (MK-0677) is an orally active nonpeptide growth hormone (GH) secretagogue.

Kinetin is a kind of cytokinin, a class of plant hormone that promotes cell division.

MPTP hydrochloride induced reduction in the DOPAC HVA/dopamine (DA) ratio and increase in striatal ascorbate (AS) oxidation in rats.

Sapacitabine is an orally bioavailable pyrimidine analogue prodrug with potential antineoplastic activity.

Halofuginone is a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities.