Moroxydine is an antiviral agent. Moroxydine targets DNA and RNA viruses including measles, herpes simplex, varicella zoster, and hepatitis C, and formulations containing moroxydine are used to treat the symptoms of influenza virus strain A.

Benazeprilat, also known as CGS 14831, is an inhibitor of angiotensin converting enzyme (ACE; IC50 = 0.28 nM in plasma from dog) and the active metabolite of the prodrug benazepril.

Terreic Acid is a cell-permeable quinone epoxide that selectively inhibits Bruton’s tyrosine kinase (BTK) catalytic activity (IC50s = 10 and 3 μM for basal and activation levels, respectively). Terreic Acid recapitulated the phenotypic defects of btk mutant mast cells in high-affinity IgE receptor-stimulated wild-type mast cells without affecting the enzymatic activities and expressions of many other signaling molecules, including those of protein kinase C. Terreic acid is a covalent inhibitor of the bacterial cell wall biosynthetic enzyme UDP-N-acetylglucosamine 1-carboxyvinyltransferase (MurA) .

Psoromic Acid is a selective and covalent Rab-prenylation inhibitor targeting autoinhibited RabGGTase. Psoromic acid (PA) potently and selectively inhibits RabGGTase with an IC(50) of 1.3 μM. Mutation of (α)His dramatically enhances the reaction rate, indicating that the activity of RabGGTase is likely regulated in vivo. The covalent binding of PA to the N-terminus of the RabGGTase α subunit seems to potentiate its interaction with the active site and explains the selectivity of PA for RabGGTase. Psoromic acid provides a new starting point for the development of selective RabGGTase inhibitors.

Spirolaxine is a natural product isolated from Sporotrichum laxum ATCC 15155, which has shown a variety of biological activities including promising anti-Helicobacter pylori property.

Ceftazidime is a broad-spectrum β-lactam antibiotic used as an antimicrobial agent. It is used for treating febrile neutropenia in patients with cancer. It is a third-generation cephalosporin. As a class, cephalosporins have activity against Gram-positive and Gram-negative bacteria. The balance of activity tips toward Gram-positive organisms for earlier generations; later generations of cephalosporins have more Gram-negative coverage. Ceftazidime is one of the few in this class with activity against Pseudomonas.

Quinoxaline, also called a benzopyrazine, in organic chemistry, is a heterocyclic compound containing a ring complex made up of a benzene ring and a pyrazine ring. It is a colorless oil that melts just above room temperature. Although quinoxaline itself is mainly of academic interest, quinoxaline derivatives are used as dyes, pharmaceuticals, and antibiotics such as olaquindox, carbadox, echinomycin, levomycin and actinoleutin.

Norepinephrine is an organic chemical in the catecholamine family that functions in the human brain and body as a hormone and neurotransmitter. Norepinephrine directly stimulates adrenergic receptors. Stimulation of alpha-adrenergic receptors causes vasoconstriction of the radial smooth muscle of the iris, arteries, arterioles, veins, urinary bladder, and the sphincter of the gastrointestinal tract. Stimulation of beta-1 adrenergic receptors causes an increase in myocardial contractility, heart rate, automaticity, and atrioventricular (AV) conduction while stimulation of beta-2 adrenergic receptors causes bronchiolar and vascular smooth muscle dilatation.

Quercetin is a plant polyphenol from the flavonoid group, found in many fruits, vegetables, leaves, and grains. It can be used as an ingredient in supplements, beverages, or foods. Quercetin has been reported to inhibit the oxidation of other molecules and hence is classified as an antioxidant. Quercetin contains a polyphenolic chemical substructure that stops oxidation by acting as a scavenger of free radicals that are responsible for oxidative chain reactions. Quercetin also activates or inhibits the activities of a number of proteins.

Ibipinabant, also known as BMS-646256, JD-5001 and SLV-319, is a potent and highly selective CB1 antagonist. It has potent anorectic effects in animals, and was researched for the treatment of obesity, although CB1 antagonists as a class have now fallen out of favour as potential anorectics following the problems seen with rimonabant, and so ibipinabant is now only used for laboratory research, especially structure-activity relationship studies into novel CB1 antagonists.

Cetraxate, also known as DV-1006, is an oral gastrointestinal medication which has a cytoprotective effect.

Lanolin, also known as wool wax or wool grease, is a yellow fat obtained from sheep's wool. It is used as an emollient, cosmetic, and pharmaceutic aid. Lanolin contains a complex combination of esters and polyesters, consisting chiefly of cholesteryl and isocholesteryl esters of the higher fatty acids. Lanolin and its many derivatives are used extensively in both the personal care (e.g., high value cosmetics, facial cosmetics, lip products) and health care sectors such as topical liniments. Lanolin is also found in lubricants, rust-preventive coatings, shoe polish, and other commercial products. Lanolin is a relatively common allergen and is often misunderstood as a wool allergy. However, allergy to a lanolin-containing product is difficult to pinpoint and often other products containing lanolin may be fine for use. Patch testing can be done if a lanolin allergy is suspected.

Echinomycin is a peptide antibiotic. It intercalates into DNA at two specific sites, thereby blocking the binding of hypoxia inducible factor 1 alpha (HIF1alpha).

Oligomycin A, also known as MCH 32, is an inhibitor of ATP synthase. Oligomycin A inhibits ATP synthase by blocking its proton channel (Fo subunit), which is necessary for oxidative phosphorylation of ADP to ATP (energy production). The inhibition of ATP synthesis by oligomycin A will significantly reduce electron flow through the electron transport chain; however, electron flow is not stopped completely due to a process known as proton leak or mitochondrial uncoupling. This process is due to facilitated diffusion of protons into the mitochondrial matrix through an uncoupling protein such as thermogenin, or UCP1.

Amantadine is a drug that has U.S. Food and Drug Administration approval for use both as an antiviral and an anti-parkinsonian drug. Amantadine is a weak antagonist of the NMDA-type glutamate receptor, increases dopamine release, and blocks dopamine reuptake. Amantadine probably does not inhibit MAO enzyme. Moreover, the mechanism of its antiparkinsonian effect is poorly understood.[citation needed] The drug has many effects in the brain, including release of dopamine and norepinephrine from nerve endings. It appears to be a weak NMDA receptor antagonist as well as an anticholinergic, specifically a nicotinic alpha-7 antagonist like the similar pharmaceutical memantine.

Tiapride is a drug that selectively blocks D2 and D3 dopamine receptors in the brain. It is used to treat a variety of neurological and psychiatric disorders including dyskinesia, alcohol withdrawal syndrome, negative symptoms of psychosis, and agitation and aggression in the elderly. Tiapride is a dopamine D2 and D3 receptor antagonist. It is more selective than other neuroleptic drugs such as haloperidol and risperidone, which not only target four of the five known dopamine receptor subtypes (D1-4), but also block serotonin (5-HT2A, 2C), α1- and α2-adrenergic, and histamine H1 receptors.

Azeliragon 2HCl (also known as TTP488 2HCl and PF-04494700 2HCl) is a potent and orally bioactive RAGE (Receptor for Advanced Glycation End products) inhibitor that has the potential for the treatment of mild-to-moderate Alzheimer's disease and cerebral amyloid angiopathy. RAGE is a pattern recognition receptor that affects the movement of amyloid (a biomarker for Alzheimer's disease) into the brain. In preclinical studies, azeliragon decreased brain amyloid in mice and improved their performance on behavior tests. Azeliragon has been shown to be involved in adaptive immune responses. It is currently in Phase 3 clinical trial.

Methylisothiazolinone, also known as MIT, or MI, (sometimes erroneously called methylisothiazoline), is a powerful synthetic biocide and preservative within the group of isothiazolinones, which is used in numerous personal care products and a wide range of industrial applications.

Methylisothiazolinone, also known as MIT, or MI, (sometimes erroneously called methylisothiazoline), is a powerful synthetic biocide and preservative within the group of isothiazolinones, which is used in numerous personal care products and a wide range of industrial applications.

Tylosin, also known as Tylosin A, is an antibiotic and a bacteriostatic feed additive used in veterinary medicine. It has a broad spectrum of activity against Gram-positive organisms and a limited range of Gram-negative organisms. It is found naturally as a fermentation product of Streptomyces fradiae. It is a macrolide antibiotic. Tylosin is used in veterinary medicine to treat bacterial infections in a wide range of species and has a high margin of safety. It has also been used as a growth promotant in some species, and as a treatment for colitis in companion animals.

Pinostrobin is a flavonoid with diverse biological activities, including antioxidant, anti-inflammatory, and anticancer properties. Pinostrobin is a dietary bioflavonoid discovered more than 6 decades ago in the heart-wood of pine (Pinus strobus). Pinostrobin has depicted many pharmacological activities including anti-viral, anti-oxidant, anti-leukaemic, anti-inflammatory and anti-aromatase activities. It is an inhibitor of sodium channel and Ca(2+) signalling pathways and also inhibits intestinal smooth muscle contractions.

Albofungin, also known as Antibiotic P42-1, Antibiotic P42-C, is a xanthone isolated from A. tumemacerans with diverse biological activities.

Disopyramide is an antiarrhythmic medication used in the treatment of ventricular tachycardia. It is a sodium channel blocker and therefore classified as a Class 1a anti-arrhythmic agent. Disopyramide has a negative inotropic effect on the ventricular myocardium, significantly decreasing the contractility. Disopyramide also has an anticholinergic effect on the heart which accounts for many adverse side effects. Disopyramide is available in both oral and intravenous forms, and has a low degree of toxicity.

Pirlindole is a reversible inhibitor of monoamine oxidase A (RIMA) which was developed and is used in Russia as an antidepressant. It is structurally and pharmacologically related to metralindole. Pirlindole is approved in some European and non-European countries for the treatment of depression. Pirlindole has an absolute bioavailability of between 20 and 30% due to an extensive first-pass effect. Orally, the Tmax varies between 2.5 and 6 h in the rat and 0.8 and 2 h in the dog.

Tetrindole was a drug candidate that functions by reversibly inhibiting monoamine oxidase A; it was first synthesized in Moscow in the early 1990s. Tetrindole is similar in its chemical structure to pirlindole (Pyrazidol), and metralindole.

Tropodithietic acid is a broad spectrum tropolone antibiotic with activity against both Gram-negative and Gram-positive bacteria.

Trilaurin is a triacylglycerol found in dietary fats. Trilaurin can be used in cosmetic products as an thickening agent. Trilaurin can be also used to make nanopartice drug formulation.

Tetryzoline, also known as tetrahydrozoline, is a derivative of imidazoline, is found in over-the-counter eye drops and nasal sprays. Other derivatives include naphazoline, oxymetazoline, and xylometazoline. Tetrahydrozoline is an alpha agonist and its main mechanism of action is the constriction of conjunctival blood vessels. This serves to relieve the redness of the eye caused by minor ocular irritants. To treat allergic conjunctivitis, tetryzoline can be combined in a solution with antazoline.

Equilenin is an equine estrogen found in the urine of pregnant mares. Equilenin is also a naturally fluorescent steroid, has high binding affinity for human sex steroid-binding protein (SBP). At 4 degrees C the equilibrium association constant is approximately 6 X 10(7) M-1.

Mabuterol is a selective β2 adrenoreceptor agonist. Mabuterol has a specific effect on beta 2-adrenoceptors with no beta 1-stimulation. Mabuterol inhibited the positive inotropic effect of isoprenaline at 10(-7) g/ml and decreased the maximum driving frequency at 3 X 10(-6) g/ml. Mabuterol was 3 times more potent in relaxing the isolated rat uterus, but 700 times less potent than isoprenaline in relaxing the rabbit jejunum. Mabuterol (p.o.) depressed the intestinal propulsion and was equipotent to isoprenaline and 2.5 times less potent than salbutamol.

Neomycin is an aminoglycoside antibiotic found in many topical medications such as creams, ointments, and eyedrops. The discovery of neomycin dates back to 1949. It was discovered in the lab of Selman Waksman. Neomycin belongs to aminoglycoside class of antibiotics that contain two or more aminosugars connected by glycosidic bonds.

Prefolic A, also known as 5-Methyltetrahydrofolate, is a biologically active form of folic acid that functions, in conjunction with vitamin B12, as a methyl-group donor involved in the conversion of homocysteine to methionine.

Artemotil, also known as Arteether, is a fast acting blood schizonticide specifically indicated for the treatment of chloroquine-resistant Plasmodium falciparum malaria and cerebral malaria cases. It is a semi-synthetic derivative of artemisinin, a natural product of the Chinese plant Artemisia annua. It is currently only used as a second line drug in severe cases of malaria.

Aspercolorin is a fungal metabolite produced by Aspergillus.

Sancycline, also known as GS-2147, is a semi-synthetic tetracycline antibiotic that is more active than tetracycline against 339 strains of anaerobic bacteria (average MIC90s = 1 and 32 μg/ml, respectively).

Clomazone, also known as Dimethazone, is an agricultural herbicide, and has been the active ingredient of products named "Command" and "Commence". The molecule consists of a 2-chlorobenzyl group bound to a N-O heterocycle called Isoxazole. Clomazone suppresses the biosynthesis of chlorophyll and other plant pigments.

Terrain, also known as NSC 291308, is a fungal metabolite with diverse biological activities. Terrein reduces age-related inflammation induced by oxidative stress through Nrf2/ERK1/2/HO-1 signalling in aged HDF cells. (+)-terrein suppresses interleukin-6/soluble interleukin-6 receptor induced-secretion of vascular endothelial growth factor in human gingival fibroblasts.

Bicyclol, also known as SY 801, is a hepatoprotective agent. Bicyclol upregulates transcription factor Nrf2, HO-1 expression and protects rat brains against focal ischemia. Bicyclol induces cell cycle arrest and autophagy in HepG2 human hepatocellular carcinoma cells through the PI3K/AKT and Ras/Raf/MEK/ERK pathways. Bicyclol attenuates tetracycline-induced fatty liver associated with inhibition of hepatic ER stress and apoptosis in mice. Bicyclol promotes toll-like 2 receptor recruiting inosine 5'-monophosphate dehydrogenase II to exert its anti-inflammatory effect.

Synephrine, or, more specifically, p-synephrine, is an alkaloid, occurring naturally in some plants and animals, and also in approved drugs products as its m-substituted analog known as neo-synephrine. p-Synephrine and m-synephrine are known for their longer acting adrenergic effects compared to norepinephrine. This substance is present at very low concentrations in common foodstuffs such as orange juice and other orange (Citrus species) products, both of the "sweet" and "bitter" variety.

Aegeline is a main alkaloid isolated from Aegle marmelos Correa collected in Yogyakarta Indonesia. Aegeline inhibited the histamine release from RBL-2H3 cells induced by DNP(24)-BSA. Aegeline showed strong inhibition when RBL-2H3 cells induced by Ca(2+) stimulants such as thapsigargin and ionomycin. Tthe inhibitory effects of aegeline on the histamine release from mast cells depended on the type of mast cell and also involved some mechanisms related to intracellular Ca(2+) signaling events via the same target of the action of thapsigargin or downstream process of intracellular Ca(2+) signaling in mast cells.

Cyclopenin, also known as NSC 114538 and NSC 604989, is an inhibitor of acetylcholinesterase (AChE; IC50 = 2.04 μM for human recombinant AChE).

Antazoline is a 1st generation antihistamine with also anticholinergic properties used to relieve nasal congestion and in eye drops, usually in combination with naphazoline, to relieve the symptoms of allergic conjunctivitis. Antazoline is an ethylenediamine derivative with histamine H1 antagonistic and sedative properties. Antazoline antagonizes histamine H1 receptor and prevents the typical allergic symptoms caused by histamine activities on capillaries, skin, mucous membranes, and gastrointestinal and bronchial smooth muscles.

Pipamperone is a typical antipsychotic of the butyrophenone family used in the treatment of schizophrenia. Pipamperone acts as an antagonist of the 5-HT2A, 5-HT2B, 5-HT2C D2, D3, D4, α1-adrenergic, and α2-adrenergic receptors. It shows much higher affinity for the 5-HT2A and D4 receptors over the D2 receptor (15-fold in the case of the D4 receptor, and even higher in the case of the 5-HT2A receptor), being regarded as "highly selective" for the former two sites at low doses. Pipamperone has low and likely insignificant affinity for the H1 and mACh receptors, as well as for other serotonin and dopamine receptors.

Pipamperone is a typical antipsychotic of the butyrophenone family used in the treatment of schizophrenia. Pipamperone acts as an antagonist of the 5-HT2A, 5-HT2B, 5-HT2C D2, D3, D4, α1-adrenergic, and α2-adrenergic receptors. It shows much higher affinity for the 5-HT2A and D4 receptors over the D2 receptor (15-fold in the case of the D4 receptor, and even higher in the case of the 5-HT2A receptor), being regarded as "highly selective" for the former two sites at low doses. Pipamperone has low and likely insignificant affinity for the H1 and mACh receptors, as well as for other serotonin and dopamine receptors.

Thioridazine is a piperidine typical antipsychotic drug belonging to the phenothiazine drug group and was previously widely used in the treatment of schizophrenia and psychosis. The branded product was withdrawn worldwide in 2005 because it caused severe cardiac arrhythmias. However, generic versions are still available in the US.

Sarecycline, also known as WC-3035 and P005672, is a novel, tetracycline-derived, narrow-spectrum antibiotic being developed for use as an oral once daily antibiotic treatment for patients suffering from moderate to severe acne vulgaris. Sarecycline was designed by Paratek as a narrow-spectrum antibiotic with anti-inflammatory activity and the potential for a favorable tolerability profile.

Vasopressin, also named antidiuretic hormone (ADH), arginine vasopressin (AVP) or argipressin, is a hormone synthesized as a peptide prohormone in neurons in the hypothalamus, and is converted to AVP. It then travels down the axon of that cell, which terminates in the posterior pituitary, and is released from vesicles into the circulation in response to extracellular fluid hypertonicity (hyperosmolality). AVP has two primary functions. First, it increases the amount of solute-free water reabsorbed back into the circulation from the filtrate in the kidney tubules of the nephrons. Second, AVP constricts arterioles, which increases peripheral vascular resistance and raises arterial blood pressure.

Sultamicillin, also known as CP-49952 and VD 1827, is an oral form of the antibiotic combination (codrug or mutual prodrug) ampicillin/sulbactam. It contains esterified ampicillin and sulbactam and is marketed under a number of trade names,Unasyn from Pfizer. After absorption, sultamicillin releases ampicillin and sulbactam into the system, so all the antibacterial efficacy of sultamicillin is due to ampicillin and sulbactam. Ampicillin exerts antibacterial activity against sensitive organisms by inhibiting biosynthesis of cell wall mucopeptide where as sulbactam irreversibly inhibits most important beta-lactamases that occur in resistant strains.

Ribostamycin sulfate, also known as Landamycine, is an aminoglycoside-aminocyclitol antibiotic isolated from a streptomycete, Streptomyces ribosidificus, originally identified in a soil sample from Tsu City of Mie Prefecture in Japan. It is made up of 3 ring subunits: 2-deoxystreptamine (DOS), neosamine C, and ribose. Ribostamycin, along with other aminoglycosides with the DOS subunit, is an important broad-spectrum antibiotic with important use against human immunodeficiency virus and is considered a critically important antimicrobial by the World Health Organization., Resistance against aminoglycoside antibiotics, such as ribostamycin, is a growing concern. The resistant bacteria contain enzymes that modify the structure through phosphorylation, adenylation, and acetylation and prevent the antibiotic from being able to interact with the bacterial ribosomal RNAs.

Fludrocortisone Acetate the acetate form of the synthetic corticosteroid fludrocortisone, which is a mineralocorticoid receptor agonist. Fludrocortisone has been used in the treatment of cerebral salt wasting syndrome.

Bifenazate is a very selective acaricide that controls the spider mite, Tetranychus urticae. Bifenazate is the first example of a carbazate acaricide.

Alagebrium Chloride, also known as ALT711, was a drug candidate developed by Alteon, Inc. It was the first drug candidate to be clinically tested for the purpose of breaking the crosslinks caused by advanced glycation endproducts (AGEs), thereby reversing one of the main mechanisms of aging. Through this effect Alagebrium is designed to reverse the stiffening of blood vessel walls that contributes to hypertension and cardiovascular disease, as well as many other forms of degradation associated with protein crosslinking. Alagebrium has proven effective in reducing systolic blood pressure and providing therapeutic benefit for patients with diastolic

Citromycetin, also known as Frequentic Acid and NSC 53584, a fungal metabolite originally isolated from Australian P. frequentans with antibiotic activity against the Gram-positive bacteria S. aureus and the Gram-negative bacteria V. cholerae and S. flexneri.

Frequentin is an antibiotic originally isolated from P. frequentans that is active against bacteria (MICs = 300 and 200 μg/ml for S. aureus and B. subtilis, respectively) and fungi

Epicoccamide is a marine fungal metabolite originally isolated from E. purpurascens.

Fucoxanthin, also known as α-Carotene, is a carotenoid that occurs naturally in certain algae. It is found as an accessory pigment in the chloroplasts of brown algae and most other heterokonts, giving them a brown or olive-green color. Fucoxanthin absorbs light primarily in the blue-green to yellow-green part of the visible spectrum, peaking at around 510-525 nm by various estimates and absorbing significantly in the range of 450 to 540 nm.

Arazasetron is an antiemetic which acts as a 5-HT3 receptor antagonist, pKi = 9.27. It is used in the management of nausea and vomiting induced by cancer chemotherapy (such as cisplatin chemotherapy). Azasetron hydrochloride is given in a usual dose of 10 mg once daily by mouth or intravenously. It is approved for marketing in Japan, and marketed exclusively by Torii Pharmaceutical Co., Ltd. under the trade names "Serotone I.V. Injection 10 mg" and "Serotone Tablets 10 mg".

Sphingosine is formed primarily from the breakdown of ceramide. Sphingosine inhibits protein kinase C and phosphatidic acid phosphohydrolase. D-sphingosine, a lipid possessing the same hydrophobic base as ceramide but without a carbohydrate residue, efficiently blocked this glycolipid antigen presentation both in vitro and in spinal cords of EAE mice, and significantly decreased IL-17 and ameliorated the pathological symptoms.

Meloside A, also known as NSC-287464 and Isovitexin 2''-O-galactoside is found in cereals and cereal products.

Kansuiphorin C, also known as KPC is a natural product with a number of bioactivity. KPC could ameliorate malignant ascites by modulating gut microbiota mainly containing the increase of Lactobacillus and the decrease of Helicobacter and related carbohydrate and amino acid metabolism, providing a basis for their promising clinical usage.

Isocanadine is an isomer of canadine. Canadine, also known as tetrahydroberberine and xanthopuccine, is a benzylisoquinoline alkaloid (BIA), of the protoberberine structural subgroup, and is present in many plants from the family Papaveraceae, such as Corydalis yanhusuo and C. turtschaninovii.

Ziprazidone is approved for the treatment of schizophrenia, and acute mania and mixed states associated with bipolar disorder. Its intramuscular injection form is approved for acute agitation in schizophrenic patients for whom treatment with just ziprasidone is appropriate. The mechanism of action of ziprasidone, as with other drugs having efficacy in schizophrenia, is unknown. However, it has been proposed that this drug's efficacy in schizophrenia is mediated through a combination of dopamine type 2 (D2) and serotonin type 2 (5HT2) antagonism. As with other drugs having efficacy in bipolar disorder, the mechanism of action of ziprasidone in bipolar disorder is unknown.

Triacetyl-ganciclovir is related to ganciclovir, which may be used for toxicity studies and other analytical studies during commercial production of Ganciclovir.

Dexamethasone phosphate is a synthetic adrenal corticosteroid with potent anti-inflammatory properties. In addition to binding to specific nuclear steroid receptors.

Morin is a yellow chemical compound that can be isolated from Maclura pomifera (Osage orange), Maclura tinctoria (old fustic) and from leaves of Psidium guajava (common guava). In a preclinical in vitro study, morin was found to be a weak inhibitor of fatty acid synthase with an IC50 of 2.33 μM. Morin was also found to inhibit amyloid formation by islet amyloid polypeptide (or amylin) and disaggregate amyloid fibers. Morin can be used to test for the presence of aluminium or tin in a solution, since it forms characteristically fluorescent coordination complexes with them.

Chlorotoluron is a pheylurea herbicide that has been used to control growth of broad-leaved weeds in winter wheat, rye, barley, and triticale crops.

Gabaculine is a naturally occurring, conformationally constrained analog of GABA and an irreversible inhibitor of GABA transaminase (GABA-T; Ki = 2.9 μM). Gabaculine alters plastid development and differentially affects abundance of plastid-encoded DPOR and nuclear-encoded GluTR and FLU-like proteins in spruce cotyledons.

Desmetramadol is a central analgesic drug candidate. Desmetramadol inhibits 5-hydroxytryptamine type 2C receptors expressed in Xenopus Oocytes.

GR-203040 is a selective NK1 receptor antagonist. GR203040 inhibits cyclophosphamide-induced damage in the rat and ferret bladder. GR203040 is a novel anti-emetic agent, and the broad spectrum of anti-emetic activity, together with activity observed in three species, suggests that this compound is worthy of clinical investigation.

Norbormide, also known as Raticate, Shoxin, is a toxic compound used as a rodenticide. It has several mechanisms of action, acting as a vasoconstrictor and calcium channel blocker, but is selectively toxic to rats and has relatively low toxicity to other species, due to a species specific action of opening the permeability transition pores in rat mitochondria.

Alpha-Chloralose is an avicide, and a rodenticide used to kill mice in temperatures below 15 °C. It is also widely used in neuroscience and veterinary medicine as an anesthetic and sedative.

Remogliflozin, also known as Remogliflozin A and GSK189074, is a potent inhibitor of sodium-glucose transporter 2 (SGLT2; Kis = 12.4 and 26 nM for human and rat SGLT2, respectively).

Grazoprevir, also known as MK5172, is a drug approved for the treatment of hepatitis C. Grazoprevir is a second generation hepatitis C virus protease inhibitor acting at the NS3/4a protease targets. It has good activity against a range of HCV genotype variants, including some that are resistant to most currently used antiviral medications.

Perastine is a biochemical.

Sodium aurothiomalate (INN, known in the United States as gold sodium thiomalate) is a gold compound that is used for its immunosuppressive anti-rheumatic effects. Along with an orally-administered gold salt, auranofin, it is one of only two gold compounds currently employed in modern medicine

Pritelivir, also known as AIC-316 and BAY 57-1293, is a potent helicase primase inhibitor. BAY 57-1293 inhibits replication of herpes simplex virus (HSV) type 1 and type 2 in the nanomolar range in vitro by abrogating the enzymatic activity of the viral primase-helicase complex. In various rodent models of HSV infection the antiviral activity of BAY 57-1293 in vivo was found to be superior compared to all compounds currently used to treat HSV infections. The compound shows profound antiviral activity in murine and rat lethal challenge models of disseminated herpes, in a murine zosteriform spread model of cutaneous disease, and in a murine ocular herpes model. It is active in parenteral, oral, and topical formulations.

Cenicriviroc, also known as TAK-652 and TBR-652, is an experimental drug candidate for the treatment of HIV infection. It is being developed by Takeda Pharmaceutical and Tobira Therapeutics. Cenicriviroc is an inhibitor of CCR2 and CCR5 receptors, allowi

Chlorcyclizine is a first-generation antihistamine of the phenylpiperazine class marketed in the United States and certain other countries. It is used primarily to treat allergy symptoms such as rhinitis, urticaria, and pruritus, and may also be used as an antiemetic. In addition to its antihistamine effects, chlorcyclizine also has some anticholinergic, antiserotonergic, and local anesthetic properties. It also has been studied as a potential treatment for hepatitis C.

Lycoramine is a natural alkaloid isolated from Lycoris chinensis.

Light green SF yellowish (C.I. 42095) is a dye that is used for the preparation of a staining solution which is is widely used as a counterstain. for e.g. trichrome Masson-Goldner staining in histological sections or for Papanicolaou’s polychromatic staining in cytology of samples human origin

Estradiol cypionate, also known as Depoestradiol, is an estrogen medication which is used in hormone therapy for menopausal symptoms and low estrogen levels in women, in hormone therapy for transgender women, and in hormonal birth control for women. Estradiol cypionate was first described as well as introduced for medical use in 1952. Along with estradiol valerate, it is one of the most commonly used esters of estradiol.

Clobetasone is a corticosteroid used in dermatology, for treating such skin inflammation as seen in eczema, psoriasis and other forms of dermatitis, and ophthalmology. Topical clobetasone butyrate has shown minimal suppression of the Hypothalamic-pituitary-adrenal axis. It is available as clobetasone butyrate under the brand names Eumosone or Eumovate both manufactured by GlaxoSmithKline.

Gramicidin is a combination of six different antimicrobial polypeptides (from Bacillus aneurinolyticus (Bacillus brevis)).

Bimatoprost acid is a metabolically stable analog of PGF2α and is a potent agonist for the FP receptor. It binds to the FP receptor on ovine luteal cells with a relative potency of 756% compared to that of PGF2α.

Parbendazole is an anthelmintic drug. Parbendazole is a potent inhibitor of microtubule assembly, destabilizes tubulin and exhibits a broad-spectrum anthelmintic activity.

Dirithromycin is a macrolide glycopeptide antibiotic. Dirithromycin is a more lipid-soluble prodrug derivative of 9S-erythromycyclamine prepared by condensation of the latter with 2-(2-methoxyethoxy)acetaldehyde. The 9N, 11O-oxazine ring thus formed is a hemi-aminal that is unstable under both acidic and alkaline aqueous conditions and undergoes spontaneous hydrolysis to form erythromycyclamine.

Pseudopelletierine is the main alkaloid derived from the root-bark of the pomegranate tree (Punica granatum), along with at least three other alkaloids: pelletierine, isopelletierine, and methylpelleteirine (C9H17ON), which yield 1.8, 0.52, 0.01, and 0.20 grams per kilogram of raw bark.

Betamethasone acetate, also known as Betamethasone 21-acetate, is a synthetic glucocorticoid corticosteroid and a corticosteroid ester. It is the 21-acetate ester of betamethasone.

Salvinorin A is a potent, non-nitrogenous κ opioid selective receptor agonist. Salvinorin A is isolated from Salvia divinorum. Salvinorin A preserves cerebral pial artery autoregulation after forebrain ischemia via the PI3K/AKT/cGMP pathway. Salvinorin A ameliorates cerebral vasospasm through activation of endothelial nitric oxide synthase in a rat model of subarachnoid hemorrhage.

Triclopyr, also known as 3,5,6-Trichloro-2-pyridinyloxyacetic acid, is a systemic foliar herbicide and fungicide. Triclopyr is used to control broadleaf weeds while leaving grasses and conifers unaffected or to control rust diseases on crops.

Fluphenazine is a antipsychotic medication. It is used in the treatment of chronic psychoses such as schizophrenia. Fluphenazine exerts its actions by blocking postsynaptic dopamine D2 receptors in the limbic, cortical system and basal ganglia. This prevents the actions of dopamine, thereby reducing the hallucinations and delusions that are associated with schizophrenia. It is given by mouth, injection into a muscle, or just under the skin.

Hibifolin is a flavonol glycoside that prevents beta-amyloid-induced neurotoxicity in vitro. Hibifolin prevents beta-amyloid-induced neurotoxicity in cultured cortical neurons. Hibifolin is a potential inhibitor of adenosine deaminase.

Nicotinamide Mononucleotide, also known as ("NMN" and "β-NMN") is a nucleotide derived from ribose and nicotinamide Like nicotinamide riboside, NMN is a derivative of niacin, and humans have enzymes that can use NMN to generate nicotinamide adenine dinuc

Tafenoquine-d3 is a trideuerium-labeled Tafenoquine derivative. Tafenoquine, also known as WR-238605, is an oral active antimalaria drug that is being investigated as a potential treatment for malaria, as well as for malaria prevention. Tafenoquine Shows Activity against Trypanosoma brucei. Tafenoquine targets leishmania respiratory complex III and induces apoptosis. Tafenoquine has a long half-life of approximately 14 days and is generally safe and well tolerated, Malaria remains an important cause of global morbidity and mortality. As antimalarial drug resistance escalates, new safe and effective medications are necessary to prevent and treat malarial infection.

Dihydrolipoic acid, also know as DHLA, is a dithiol-containing carboxylic acid that is the reduced form of α-lipoic acid . It acts as a general antioxidant that is highly reactive against a variety of reactive oxygen species, including hydroxyl radicals, peroxynitirite, hydrogen peroxide, and hypochlorite, at concentrations ranging from 0.01-0.5 mM.

Matrixyl, also known as Palmitoyl pentapeptide-4 (palmitoyl pentapeptide-3 before 2006) is a matrikine used in anti-wrinkle cosmetics. It was launched in 2000 as an active ingredient for the personal care industry under the trade name Matrixyl by the French cosmetic active ingredient manufacturer Sederma SAS.

Argireline, also known as Acetyl Hexapeptide-3, is a newer ingredient in skincare, ideal for maturing skin and diminishing the appearance of wrinkles. Argireline is the brand name of Acetyl Hexapeptide-8, a molecule formed principally of 6 amino acids (which in a row are called a peptide). It is synthetically produced in a lab, but there are no indications of any degree of toxicity and it is one of our favorite compounds for maturing skin.

Elexacaftor, also known as VX-445 and WHO 11180, is a next-generation cystic fibrosis transmembrane conductance regulator (CFTR) corrector designed to restore Phe508del CFTR protein function in patients with cystic fibrosis when administered with tezacaftor and ivacaftor (VX-445–tezacaftor–ivacaftor).

Hesperidin Methyl Chalcone is a derivative of the flavonoid hesperidin and is found in citrus fruits like oranges and grapefruit and is often used to reduce dark circles under the eyes.

Brassinazole is an inhibitor of brassinosteroid biosynthesis that has been developed in order to probe the myriad functions of brassinosteroids.

Arbutin is a glycoside; a glycosylated hydroquinone extracted from the bearberry plant in the genus Arctostaphylos among many other medicinal plants, primarily in the family Ericaceae. Applied topically, it inhibits tyrosinase and thus prevents the formation of melanin. Arbutin is therefore used as a skin-lightening agent. Very tiny amounts of arbutin are found in wheat, pear skins, and some other foods. It is also found in Bergenia crassifolia. Arbutin was also produced by an in vitro culture of Schisandra chinensis. α-Arbutin Protects Against Parkinson's Disease-Associated Mitochondrial Dysfunction In Vitro and In Vivo.

Picrocrocin is a monoterpene glycoside precursor of safranal. Picrocrocin is found in the spice saffron, which comes from the crocus flower. Picrocrocin is a degradation product of the carotenoid zeaxanthin. Picrocrocin exhibits growth inhibitory effects against SKMEL- 2 human malignant melanoma cells by targeting JAK/ STAT5 signaling pathway, cell cycle arrest and mitochondrial mediated apoptosis.

Methylthialazole Tetrazolium, also known as MTT or Tetrazolium Bromide, is a cell-permeable and positively charged tetrazolium dye that is used to detect reductive metabolism in cells.1 It is taken up by cells through the plasma membrane and then reduced to formazan by intracellular NAD(P)H-oxidoreductases. It is frequently used in colorimetric assays to measure cell proliferation, cytotoxicity, and apoptosis.

(R)-Carisbamate is the R-isomer of Carisbamate . Carisbamate (YKP 509, proposed trade name Comfyde) is an experimental anticonvulsant drug that was under development by Johnson & Johnson Pharmaceutical Research and Development but never marketed.

Terphenyllin is a naturally abundant p-terphenyl metabolite isolated from the coral derived fungus Aspergillus candidus, has signi?cant α-glucosidase inhibitory activity.

Iristectorigenin A is an natural isoflavones, showing antioxidant activity.

Afamelanotide, also known as CUV1647, is a Melanocortin receptor agonist. Afamelanotide is a synthetic peptide and analogue of α-melanocyte stimulating hormone used to prevent skin damage from the sun in people with erythropoietic protoporphyria .It is under development in other skin disorders in several jurisdictions. It causes skin to turn darker by causing the skin to make more melanin.

Lasmiditan, also known as COL-144 and LY573144, is a novel, centrally acting, highly selective 5-HT(1F) receptor agonist (K1=2.21 μM) without vasoconstrictor activity that seemed effective when given as an intravenous infusion in a proof-of-concept migraine study. Lasmiditan showed efficacy in its primary endpoint, with a 2-hour placebo-subtracted headache response of 28.8%, though with frequent reports of dizziness, paresthesias, and vertigo.

Meropenem is an ultra-broad spectrum injectable antibiotic used to treat a wide variety of infections, including meningitis and pneumonia. It is a beta-lactam and belongs to the subgroup of carbapenem, similar to imipenem and ertapenem. Meropenem was originally developed by Sumitomo Pharmaceuticals. It is marketed outside Japan by AstraZeneca with the brand names Merrem and Meronem. Other brand names include Zwipen (India, Marketed by Nucleus) Mepem (Taiwan) Meropen (Japan, Korea) and Neopenem (NEOMED India) . It gained FDA approval in July 1996. It penetrates well into many tissues and body fluids including the cerebrospinal fluid, bile, heart valves, lung, and peritoneal fluid.

Niraparib, also know as MK-4827, is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. MK4827 inhibits PARP activity, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. The PARP family of proteins detect and repair single strand DNA breaks by the base-excision repair (BER) pathway.

Panobinostat, also known as NVP LBH-589 or LBH-589, is a cinnamic hydroxamic acid analogue with potential antineoplastic activity. Panobinostat selectively inhibits histone deacetylase (HDAC), inducing hyperacetylation of core histone proteins, which may result in modulation of cell cycle protein expression, cell cycle arrest in the G2/M phase and apoptosis. In addition, this agent appears to modulate the expression of angiogenesis-related genes, such as hypoxia-inducible factor-1alpha (HIF-1a) and vascular endothelial growth factor (VEGF), thus impairing endothelial cell chemotaxis and invasion.

Siponimod, also known as BAF-312, is a a potent and orally selective S1P Receptor Modulator with EC50 value of 0.39nM for S1P1 receptors and 0.98nM for S1P5 receptors, respectively. Development of sphingosine-1-phosphate receptor 1 (S1P1) modulators to dampen inflammation and its sequelae is becoming increasingly promising for treating medical conditions characterized by significant immunopathology.

Stiripentol (marketed as Diacomit by Laboratoires Biocodex) is an anticonvulsant drug used in the treatment of epilepsy. It is approved for the treatment of Dravet syndrome, an epilepsy syndrome. Stiripentol increases GABAergic activity. At clinically relevant concentrations, it enhances central GABA neurotransmission through a barbiturate-like effect, since it increases the duration of opening of GABA-A receptor channels in hippocampal slices.

Danshenxinkun A is a natural diterpenoid isolated from the roots of Salvia miltiorrhiza Bge.

Segetalin B is natural product isolated from Seeds of Vaccaria Segetalis. Segetalin B demonstrated to have an estrogen-like activity.

Nafamostat, also known as FUT-175, is a serine protease inhibitor and an anticoagulant. Nafamostat promotes endothelium-dependent vasorelaxation via the Akt-eNOS dependent pathway. Nafamostat Attenuates Ischemia-Reperfusion-Induced Renal Injury. Nafamostat Attenuates Ischemia-Reperfusion-Induced Renal Injury. Nafamostat protects against acute cerebral ischemia via blood-brain barrier protection. Nafamostat Inhibits TNF-α-Induced Vascular Endothelial Cell Dysfunction by Inhibiting Reactive Oxygen Species Production. Researchers have identified the drug as a potential therapy for COVID-19,[ with clinical trials in Japan possibly set to begin in March 2020.

Fatostatin A is a Cell permeable inhibitor of SREBP activation. Fatostatin Inhibits Cancer Cell Proliferation by Affecting Mitotic Microtubule Spindle Assembly and Cell Division. Fatostatin suppresses growth and enhances apoptosis by blocking SREBP-regulated metabolic pathways in endometrial carcinoma.

Caerulein is a specific decapeptide obtained from the skin of Hila caerulea, an Australian amphibian. Caerulein is similar in action and composition to CHOLECYSTOKININ. It stimulates gastric, biliary, and pancreatic secretion; and certain smooth muscle. It is used in paralytic ileus and as diagnostic aid in pancreatic malfunction.

Eyeseryl, also known as Acetyl Tetrapeptide-5, humectant or hydroscopic moisturizer which helps reduce eye puffiness, improve skin elasticity as well as overall smoothness.

Ziram, also known as Zinc dimethyldithiocarbamate, is a coordination complex of zinc with dimethyldithiocarbamate. It is a pale yellow solid that is used as a fungicide, the vulcanization of rubber, and other industrial applications.

Polaprezinc is an orally bioavailable chelate composed of zinc and L-carnosine, with potential gastroprotective, anti-oxidant, anti-ulcer and anti-inflammatory activities. Upon administration, polaprezinc increases the expression of various anti-oxidant enzymes, such as superoxide dismutase 1 (SOD-1), SOD-2, heme oxygenase-1 (HO-1), glutathione S-transferase (GST), glutathione peroxidase (GSH-px), peroxidredoxin-1 (PRDX1; PRXI) and PRXD5 (PRXV) in the gastric mucosa, which protect cells against reactive oxygen species (ROS).

N-Benzyloxycarbonylglycine

Propham is a biochemical.

Vinyltrimethoxysilane

Y 27152 is a biochemical.

Niraxostat is a biochemical.

Yakkasterone is a major metabolite of cholesterol formed during exposure of lung epithelial cells to ozone.

Carbofuran is one of the most toxic carbamate pesticides.

Molinate is a biochemical.

Yatein is a natural product isolated from from Cleistanthus boivinianu or Chamaecyparis obtusa. Yatein suppresses herpes simplex virus type 1 replication in HeLa cells by interruption the immediate-early gene expression. The mechanisms of antiviral action of yatein seem to be mediated, by inhibiting HSV-1 α gene expression, including expression of the ICP0 and ICP4 genes, and by arresting HSV-1 DNA synthesis and structural protein expression in HeLa cells. Yatein showed antiproliferative activity against the HCT-116 human colon carcinoma cell line, with an IC50 > 10 uM.

Yau 17 is a biochemical.

L 709049 is a biochemical.

Josamycin is a macrolide antibiotic.

Midecamycin is a naturally occurring 16-membered macrolide that fits under the category of acetoxy-substituted macrolide antibiotics. In this molecule, an acetoxy group is substituted on the position 9 of the 16-member ring and on position 4 of the terminal sugar.

Oxazole yellow is a fluorescent cyanine dye that binds to DNA and is used to detect apoptotic cells. Oxazole yellow does not enter live cells. However, during apoptosis the cytoplasmic membrane becomes slightly permeable, allowing entry of the dye. Oxazole yellow is often used along with propidium iodide (catalog no. P4170), a DNA dead cell stain that does not enter either live or apoptotic cells. The λEx/λEm of Oxazole yellow is 491/509.

Alizarine Yellow R is a yellow colored azo dye made by the diazo coupling reaction.

Calcon is a biochemical indicator of calcium.

B355252 is a neuroprotective agent that potentiates nerve growth factor (NGF)-induced neurite outgrowth and protects against cell death caused by glutamate-evoked oxidative stress.

DMH4 is a potent VEGF inhibitor and an angiogenesis inhbitor.

GW2974 Potent and selective dual inhibitor of EGFR.

NP603 is a cell-permeable inhibitor of PDGFRβ, FGFR1 and VEGFR2 that binds to ATP pocket. NP603 is a very weak inhibitor of EGFR

PD173952 is a Src family kinase inhibitor.

PF-06250112 is a potent inhibitor of Bruton′s tyrosine kinase

PF-06439015 is a potent and selective inihibitor that overcomes clinical ALK (receptor tyrosine kinase anaplastic lymphoma kinase) mutations resistant to Crizotinib.

Roslin 2 is a p53 reactivator that disrupts the FAK and p53 interaction, and reactivates transcriptional activity of p53 with p21, Mdm-2 and Bax transcriptional targets. Roslin 2 decreases viability and clonogenicity of cancer cells, and inhibits tumor growth.

SKI 5C is a selective Sphingosine Kinase 1 (SPHK1) inhibitor.

Tyrphostin 51 is a potent inhibitor of EGFR (EGF receptor) kinase activity

Tyrphostin AG 1112 is a Bcr-Abl kinase blocker that can activate the terminal differentiation of K562 cells and the purging of Ph+ cells.

Tyrphostin AG 825 is shown to be a potent inhibitor of EGFR (epidermal growth factor receptor) and Neu (HER-2) kinases.

Rescinnamine is an angiotensin-converting enzyme inhibitor used as an antihypertensive drug. It is a vinca alkaloid obtained from Rauwolfia serpentina and other species of Rauwolfia.

Tazobactam sodium is a biochemical.

Methylmethionine sulfonium chloride is a biochemical.

Methoprene is a juvenile hormone (JH) analog which acts as a growth regulator when used as an insecticide. It is an amber-colored liquid with a faint fruity odor which is essentially nontoxic to humans when ingested or inhaled. It is used in drinking water cisterns to control mosquitoes which spread dengue fever and malaria.

Aurodox is a polyketide antibiotic active against Gram-positive bacteria. It is effective against S. pyogenes infection in mice with a 50% curative dose (CD50) value of 71 mg/kg. Aurodox inhibits bacterial protein synthesis by binding to bacterial elongation factor Tu (EF-Tu) and inhibiting its release from the ribosome.

Ranitidine-S-oxide is a metabolite of Ranitidine. Ranitidine, sold under the trade name Zantac among others, is a medication which decreases stomach acid production. It is commonly used in treatment of peptic ulcer disease, gastroesophageal reflux disease, and Zollinger–Ellison syndrome.

Xanthinol niacinate is a combination of xanthinol and niacin which acts as a vasodilator. Studies show that Xanthinol niacinate can modulate tumors during their reoxygenation. Xanthinol niacinate also displays anti-platelet and thrombolytic activity. In addition, this compound can reduce whole blood viscosity, as a result of its anti-platelet activity and decrease cholesterol and fibrinogen.

Dixanthogen is an ectoparasiticide.

Xantphos is an organophosphorus compound derived from the heterocycle xanthene.

Rhodamine 110 is a biochemical.

Rhodamine 123 is a chemical compound and a dye.

Fenazaquin is a chemical compound from the group of quinazoline derivatives and alkylaryl ethers

Cyhalofop-butyl is a biochemical.

Tetrasulis a chemical compound from the group of thioethers and diphenyls .

Flutianil is a chemical compound from the group of thiazolidines .

Penicillin V potassium is a broad-spectrum penicillin antibiotic used orally in the treatment of mild to moderate infections by susceptible gram-positive organisms.

Pyrinuron is a chemical compound formerly used as a rodenticide. Pyrinuron is an inhibitor of NAMPT and NMNAT2.

Bromopride is a dopamine antagonist with prokinetic properties widely used as an antiemetic

Prenylamine is a calcium channel blocker of the amphetamine chemical class which was used as a vasodilator in the treatment of angina pectoris.

Valencene is a sesquiterpene that is an aroma component of citrus fruit and citrus-derived odorants.

Isocaproaldehyde is a biochemical.

Vamidothion sulfoxide is a biochemical.

Mexacarbate is a carbamate pesticide developed by Alexander Shulgin.

Chlorpyrifos-methyl acts on the nervous system of insects by inhibiting acetylcholinesterase.

MCPA-thioethyl is a biochemical.

Vapiprost hydrochloride is a biochemicla.

Clopyralid is a selective herbicide used for control of broadleaf weeds.

Clothiapine, also known as Entumine, is an atypical antipsychotic of the dibenzothiazepine chemical class. It was first introduced in a few European countries (namely, Belgium, Italy, Spain and Switzerland), Argentina, Taiwan and Israel in 1970.

Crimidine is a convulsant poison used as a rodenticide. Crimidine was originally known by its product name, Castrix. It was originally produced in the 1940s by the conglomerate, IG Farben.

Alclofenac may be used to treat patients with chronic rheumatic diseases. Research shows that alclofenac has a pronounced effect upon the acute-phase protein response and the extent to which L-tryptophan is bound to plasma protein.

Butachlor is a chloroacetanalide herbicide. Butachlor is commonly used for weed control in rice as well as cotton, maize, wheat and other crops.

Zinc Pyrithione is a dimer of two pyrithione molecules bound by zinc. It is commonly found as an ingredient of commercial anti-dandruff shampoos. This products acts as an antifungal and antibacterial.

Vedaprofen is a nonsteroidal anti-inflammatory drug (NSAID) used in veterinary medicine for the treatment of pain and inflammation due to musculoskeletal disorders in dogs and horses and for the treatment of pain due to horse colic

Mefluidide is a biochemical.

FIIN-1 is Potent, irreversible FGFR inhibitor, acts at the ATP binding site. Also irreversibly inhibits Flt-1, Flt-4 and VEGFR-2.

OM137 is an inhibitor of Aurora kinases. which is growth inhibitory to cultured cells when applied at high concentration and potentiates the growth inhibitory effects of subnanomolar concentrations of paclitaxel.

YC-137 is a BCL-2 inhibitor, which selectively induces apoptosis of Bcl-2-overexpressing cells and disrupts its interaction with Bid BH3, thereby blocking the anti-apoptotic activity of Bcl-2.

PD166326 is one of the most potent members of the pyridopyrimidine class of protein tyrosine kinase inhibitors. In mice with the CML-like disease, PD166326 rapidly inhibited Bcr/Abl kinase activity after a single oral dose and demonstrated marked antileukemic activity in vivo. In vivo, PD166326 was also superior to imatinib mesylate in inhibiting the constitutive tyrosine phosphorylation of numerous leukemia-cell proteins, including the src family member Lyn. PD166326 also prolonged the survival of mice with imatinib mesylate-resistant CML induced by the Bcr/Abl mutants P210/H396P and P210/M351T.

PD180970 is a novel Bcr-Abl inhbiitor. PD180970 inhibited in vivo tyrosine phosphorylation of p210Bcr-Abl (IC50 = 170 nM) and the p210BcrAbl substrates Gab2 and CrkL (IC50 = 80 nM) in human K562 chronic myelogenous leukemic cells. In vitro, PD180970 potently inhibited autophosphorylation of p210Bcr-Abl (IC50 = 5 nM) and the kinase activity of purified recombinant Abl tyrosine kinase (IC50 = 2.2 nM). Incubation of K562 cells with PD180970 resulted in cell death. PD180970 is among the most potent inhibitors of the p210Bcr-Abl tyrosine kinase, which is present in almost all cases of human chronic myelogenous leukemia. PD180970 is a promising candidate as a novel therapeutic agent for Bcr-Abl-positive leukemia.

GTP-14564 is a specific kinase inhibitor for ITD-FLT3. GTP-14564 inhibited the growth of interleukin-3-independent Ba/F3 expressing ITD-FLT3 at 1 microM, whereas a 30-fold higher concentration of GTP-14564 was required to inhibit FLT3 ligand-dependent growth of Ba/F3 expressing wild type FLT3 (wt-FLT3).

KU59403 is a potent and selective ATM (Ataxia telangiectasia mutated) inhibitor with with potential anticancer activity. KU59403 was not cytotoxic to human cancer cell lines (SW620, LoVo, HCT116, and MDA-MB-231) per se but significantly increased the cytotoxicity of topoisomerase I and II poisons: camptothecin, etoposide, and doxorubicin. KU59403 significantly enhanced the antitumor activity of topoisomerase poisons in mice bearing human colon cancer xenografts (SW620 and HCT116) at doses that were nontoxic alone and well-tolerated in combination

CAY10505 is a phosphatidylinositol 3-kinase-γ inhibitor , was found to significantly improve acetylcholine-induced endothelium dependent relaxation, serum nitrate and (or) nitrite level, glutathione level, and the vascular endothelial lining in hypertensive rats. CAY10505 , may improve hypertension-associated vascular endothelial dysfunction. Inhibition of PI3Kγ might be a useful approach in the therapeutics of vascular endothelium dysfunction.

PD0407824, also known as PD407824 is a potent selective, small molecular CHK1 inhibitor with potential anticancer activity.

NU6140 is a cyclin-dependent kinase 2 (cdk2) inhibitor; induces cell-cycle arrest at the G2-M phase.

NU1085 is a potent poly(ADP-ribose) polymerase (PARP) inhibitors have been developed that potentiate the cytotoxicity of ionizing radiation and anticancer drugs. The biological effects of NU1085 [Ki = 6 nM], in combination with temozolomide (TM) or topotecan (TP) have been studied in 12 human tumor cell lines (lung, colon, ovary, and breast cancer). Cells were treated with increasing concentrations of TM or TP +/- NU1085 (10 microM) for 72 h.

Methylthioadenosine, also known as MTA and 5'- Methylthioadenosine, is a naturally occurring sulfur-containing nucleoside present in all mammalian tissues. In vitro experiments showed that MTA treatment inhibited melanoma cell proliferation and viability in a dose dependent manner, where BRAF mutant melanoma cell lines appear to be more sensitive. Importantly, MTA was effective inhibiting in vivo tumor growth. The molecular analysis of tumor samples and in vitro experiments indicated that MTA induces cytostatic rather than pro-apoptotic effects inhibiting the phosphorylation of Akt and S6 ribosomal protein and inducing the down-regulation of cyclin D1. ( BMC Cancer . 2010 Jun 8;10:265.)

Purpurogallin is a red, crystalline compound, and the aglycon of several glycosides from nutgalls and oak barks. It can inhibit hydroxyestradiol methylation by catechol-O-methyltransferase. It potently and specifically inhibits PLK, TLR1/TLR2 activation pathway. Purpurogallin showed antiplatelet and antithrombotic activities; anti?inflammatory effects; antitumor activity, anti-oxidation activities; hepatoprotecting effects; antibacterial activity toward gram-positive bacteria.

Thiocolchicine is a potent tubulin polymerization and microtubule assembly inhibitor, a axonal cytoskeleton modulator and apoptosis inducer. Structurally, thiocolchicine is a colchicine analog in which the C-10 methoxy is replaced with a thiomethyl moiety. Thiocolchicine was shown to bind with high affinity to the colchicine site on tubulin (Ka = 1.07 +/- 0.14 x 10(6) M-1). Thiocolchicine-dimers were shown to be potent topoisomerase I inhibitors.

ATN-163 is a five amino acid peptide. ATN-163 is a scramble peptide of ATN-161. ATN-161 (Ac-PHSCN-NH2), a five-amino acid peptide with documented anti-angiogenic activity.

Gemcitabine monophosphate disodium salt, also called GemMP, is a monophosphate derivative of Gemcitabine. Gemcitabine (Gem) is a deoxycytidine analog that is effective against pancreatic cancer and other malignancies following conversion to the 5'-O-mono-, di- and tri-phosphate forms. GemMP decreased tumor cell growth at concentrations ranging from 1 to 50 nM. GemMP is a potent cytotoxic agent that serves to induce apoptosis in association with increased Fas expression in cultured thyroid cancer cell lines. (Anticancer Res. 2000 Sep-Oct;20(5A):2915-22).

9-hydroxyellipticine, also known as IGIG 929 and LS133324, is a potent cytotoxic and antitumor agent. Structurally, 9-hydroxyellipticine is a 9-hydroxy derivative of ellipticine. The hydroxy group in 9-hydroxyellipticines increases the apparent affinity for DNA, stabilisation of toposiomerase II-DNA cleavable complex, oxidation to reactive quinone-imine intermediates, phosphorylation of p53 suppressor proteins and cytotoxicity relative to the parent ellipticines.