m-Nifedipine is an impurity of Nifedipine (BAY-a-1040). Nifedipine is a potent calcium channel blocker and drug of choice for cardiac insufficiencies.

Diisohexyl phthalate is a class of dialkyl phthalate esters and a plasticizer.

RP 48497, an impurity of Eszopiclone, is a photodegradation product of Eszopiclone. Eszopiclone is a non-benzodiazepine sedative-hypnotic used in the treatment of insomnia.

8pyDTZ is a pyridyl diphenylterazine (DTZ) analog and an ATP-independent pyridyl substrate of LumiLuc luciferase. 8pyDTZ exhibit spectrally shifted emission and improved water solubility. 8pyDTZ has excellent biocompatibility and superior in vivo sensitivity. 8pyDTZ can be used for in vivo luminescence imaging.

NMP-ACA is an impurity of Cefepime. Cefepime is a broad-spectrum cephalosporin with enhanced coverage against Gram-positive and Gram-negative bacteria.

Desfluoro-atorvastatin is an impurity of Atorvastatin. Atorvastatin is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, has the ability to effectively decrease blood lipids.

(3R,5S)-Atorvastatin sodium is an impurity of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively.

O-Methyl Atorvastatin (hemicalcium) is an impurity of Atorvastatin. Atorvastatin is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, has the ability to effectively decrease blood lipids.

Atorvastatin methyl ester (Compound 2a) is a methyl esterified derivative of Atorvastatin. Atorvastatin methyl ester inhibits the 9-cis-RA-induced Gal4 reporter activity more strongly than Atorvastatin.

Atorvastatin 3-Deoxyhept-2E-Enoic Acid ((2E)-2,3-Dehydroxy Atorvastatin) is an impurity of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor and has the ability to effectively decrease blood lipids.

Atorvastatin ethyl ester is a derivative of Atorvastatin and displays strong inhibition of the 9-cis-RA-induced Gal4 reporter activity.

Atorvastatin acetonide is an impurity of Atorvastatin, and extracted from patent WO2011131605A1, Compound 4. Atorvastatin is an orally active HMG-CoA reductase inhibitor and has the ability to effectively decrease blood lipids.

Atorvastatin acetonide tert-butyl ester is a useful pharmaceutical intermediate in the preparation of Atorvastatin salts. Atorvastatin is an orally active HMG-CoA reductase inhibitor and has the ability to effectively decrease blood lipids.

3-Oxo Atorvastatin is an impurity of 3-Oxo Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor and has the ability to effectively decrease blood lipids.

(3S,5S)-Pitavastatin cacium is the 3-epimer of Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor.

(3S,5R)-Pitavastatin cacium is the enantiomer of Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor.

(Z)-Pitavastatin calcium is the Z-Isomer of Pitavastatin hemicacium. Pitavastatin calcium is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin calcium inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells.

(R)-Linezolid is an impurity of Linezolid (PNU-100766). Linezolid, the first member of the class of oxazolidinone synthetic antibiotic, acts by inhibiting the initiation of bacterial protein synthesis.

Decarboxy Moxifloxacin (compound 8) is a decarboxylated compound of Moxifloxacin. Moxifloxacin is an orally active 8-methoxyquinolone antimicrobial for use in acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia.

Anhydrosimvastatin (Impurity C) is an impurity of Simvastatin. Simvastatin is a competitive inhibitor of HMG-CoA reductase.

4-Acetylsimvastatin is an acetylated simvastatin. Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.

(3R,5R)-Rosuvastatin Lactone is an isomer of Rosuvastatin Lactone.

ABZ-amine (Amino albendazole) is an impurity of Albendazole. Albendazole is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.

TLX agonist 1 (ccrp2) is an orphan nuclear receptor tailless (TLX, NR2E1) modulator (EC50=1μM; Kd= 650 nM). TLX agonist 1 potentiates TLX transcriptional repressive activity.

Raloxifene Bismethyl Ether is a metabolite of Raloxifene and an estrogen receptor inactive compound on which both hydroxyl groups are absent.

Raloxifene Bismethyl Ether hydrochloride is a metabolite of Raloxifene and an estrogen receptor inactive compound on which both hydroxyl groups are absent.

LY88074 Trimethyl ether (Example 1) is useful for the inhibition of the various estrogen deficient conditions, which are associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia.

LY88074 (Compound 88074) is a Raloxifene analog lacking the basic side chain. Raloxifene is a selective estrogen receptor modulator, and reduces fracture risk at least in part by improving the mechanical properties of bone in a cell- and estrogen receptor-independent manner.

4'-tert-Butyldimethylsilyl-6-hydroxy Raloxifene (Compound 4) is a reaction product of Raloxifene with tertbutyldimethylsilyl chloride. 4'-tert-Butyldimethylsilyl-6-hydroxy Raloxifene is used to synthesize Raloxifene 6-glucuronide.

Raloxifene 6,4'-Bis-β-D-glucuronide (compound IV) is a metabolite of Raloxifene. Raloxifene is a selective estrogen receptor antagonist for the prevention of osteoporosis.

7-[4-(2-Piperidinyl)ethoxy]benzoyl Raloxifene is a liver receptor homolog-1 (LRH-1) antagonist with an IC50 of 3.1 μM.

Methyl Raloxifene 4'-(2,3,4-Tri-O-acetyl-β-D-glycopyranuronate) is an analogue of Raloxifene 4'-glucuronide.

LY88074 Methyl ether (Example 2) is useful for the inhibition of the various estrogen deficient conditions, which are associated with estrogendeprivation syndrome including osteoporosis and hyperlipidemia.

LY88074 analog 1 is a benzothiophene compound with nitrogen-containing non-basic side chains, Compound 26, extracted from patent EP0747380A1. LY88074 analog 1 is an agent for alleviating the symptoms of post-menopausal symptoms, such as osteoporosis, cardiovascular related pathological conditions, and estrogen-dependent cancer. LY88074 analog 1 can be used alone or in combination with estrogen or progestin.

Raloxifene dimethyl ester hydrochloride is an analog of Raloxifene, extracted from patent US5464845A, compound 28.

GNF-2-PEG-acid, an analogue of GNF-2, is usually used as a labeled chemical or fluorescent probe.

ABL-001-Amide-PEG3-acid, an analogue of ABL-001, is usually used as a labeled chemical or fluorescent probe.

Ponatinib Acid, an analogue of Ponatinib, is usually used as a labeled chemical or fluorescent probe.

Nilotinib Acid, an analogue of Nilotinib, is usually used as a labeled chemical or fluorescent probe.

Imatinib Acid, an analogue of Imatinib, is usually used as a labeled chemical or fluorescent probe.

Alkyne-probe 1 is usually used as a Alkyne-labeled chemical or fluorescent probe.

TAMRA-probe 1 is a commonly used fluorescent probe for labeling.

Biotin-probe 1 is a non-radiolabeled probe. Biotin-labeled probes can be applied to in situ hybridization.

SMS1-IN-1, compound SAPA 1j, is a novel and the most potent sphingomyelin synthase 1 (SMS1) inhibitor with an IC50 value of 2.1 μM. SMS1-IN-1 has the potential for the treatment of atherosclerosis.

Glycosidase-IN-1 (Compound 9) is a glycosidase inhibitor synthesized from D-mannose. Glycosidase-IN-1 be used to synthesize some immunosuppressive agents and β-glucosidase inhibitors. Glycosidase-IN-1 has hypoglycemic activity.

β-glycosidase-IN-1 (Compound 33) is a piperidine derivative and a β-glycosidase inhibitor. β-glycosidase-IN-1 has hypoglycemic activity.

Glycosidase-IN-2 (Compound 20) is an azasugar class of glycosidase inhibitor. Glycosidase-IN-2 has hypoglycemic activity.

Nitrosobiotin is prepared from biotin.

Norbiotinamine is an alternative to biotin. Norbiotinamine can be coupled with a carboxylic group of amino acids to give inverse peptides, having the amide linkage oriented in the opposite direction.

Norbiotinamine hydrochloride is an alternative to biotin. Norbiotinamine can be coupled with a carboxylic group of amino acids to give inverse peptides, having the amide linkage oriented in the opposite direction.

Dicaprylyl carbonate, a solid, plant-derived fat, is a dry emollient. Dicaprylyl carbonate has excellent dermatological compatibility and a comprehensive performance profile, such as solubilizing and dispersing ability for sun-care filters.

BN201 promotes neuronal differentiation, the differentiation of precursor cells to mature oligodendrocytes (EC50 of 6.3 μM) in vitro, and the myelination of new axons (EC50 of 16.6 μM). BN201 is able to cross the blood-brain barrier by active transport and activate pathways (IGF-1 pathway) associated with the response to stress and neuron survival. BN201 has potently neuroprotective effects.

OSMI-2 (Compound 1b) is a cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-2 increases detained intron splicing in cells.

OSMI-3 (Compound 2b) is a potent, long-lasting, and cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-3 increases detained intron splicing in cells.

1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) is a highly selective soluble epoxide hydrolase (sEH) inhibitor. 1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) increases epoxyeicosatrienoic acids (EETs) levels and lowers blood pressure in angiotensin II (Ang II) hypertension.

Arachidonyl alcohol is a long-chain primary fatty alcohol. Arachidonyl alcohol is used as a substrate for the production of several ether lipids possessing beneficial functions.

(R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed. Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor.

(R)-Thalidomide ((R)-(+)-Thalidomide) is the R-enantiomer of Thalidomide. (R)-Thalidomide has sedative properties.

β-D-Glucose Pentaacetate (Penta-O-acetyl-β-D-glucopyranose) is used in biochemical reaction.

4-Acetamidophenyl acetate is an impurity of Acetaminophen (paracetamol). Acetaminophen, an analgesic drug, is a selective COX-2 inhibitor (IC50=25.8 μM), and is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.

trans-Doxercalciferol is an isomer of Doxercalciferol. Doxercalciferol is a Vitamin D2 analog, acts as an activator of Vitamin D receptor, and prevent renal disease.

L-Xylose (L-(-)-Xylose) is the levo-isomer of Xylose. Xylose is classified as a monosaccharide of the aldopentose type.

L-Ornithine L-aspartate is a stable salt of two natural nonessential L-amino acids: ornithine and aspartic acid. L-Ornithine L-aspartate lowers blood ammonia concentration and to eliminate symptoms of hepatic encephalopathy associated with liver cirrhosis.

Fibrin, isolated from bovine blood, is an insoluble protein produced in response to bleeding. Fibrin is the major component of the blood clot and is used for coagulation.

Amoxapine is a tetracyclic antidepressant of the dibenzoxazepine family, though it is often classified as a secondary amine tricyclic antidepressant.

Hydrastinine is a major alkaloid constituent in goldenseal (Hydrastis canadensis). Hydrastinine can be used as a haemostatic agent.

Mebrofenin (SQ 26962) is a type of iminodiacetic acid (IDA). Mebrofenin is available as a ready to use the kit for radio-labeling with Tc-99m. Tc-99m Mebrofenin, a diagnostic agent, is used for hepatobiliary imaging. Tc-99m Mebrofenin is the radiopharmaceutical of choice for the evaluation of hepatic function.

Metrizoic acid (Metrizoate) is an ionic contrast medium. Metrizoic acid (Metrizoate) shows high osmolality and has a risk of inducing allergic reactions.

Perflubron(1-Bromoheptadecafluorooctane;Heptadecafluorooctyl bromide; Perfluorooctyl bromide) is a contrast medium for magnetic resonance imaging and sonography. Perflubron (1-Bromoheptadecafluorooctane;Heptadecafluorooctyl bromide; Perfluorooctyl bromide) can be emulsified with egg phospholipids (EYP) and shows exceptionally fast excretion characteristics.

Spermidine trihydrochloride maintains cell membrane stability, increases antioxidant enzymes activities, improving photosystem II (PSII), and relevant gene expression. Spermidine trihydrochloride significantly decreases the H2O2 and O2.- contents.

Tolonidine is a derivative of imidazoline. Tolonidine is orally active and has been shown to possess hypotensive and antihypertensive properties.

Mildronate (Meldonium) functions as a cardioprotective drug by cpmpetetively inhibiting BBOX1 and OCTN2. Mildronate (Meldonium) exhibits IC50 values of 34-62 μM for human recombinant BBOX and an EC50 of 21 μM for human OCTN2. Mildronate (Meldonium) treatment-induced redirection of long-chain FA metabolism from mitochondria to peroxisomes.

(R)-(+)-Atenolol is the less active enantiomer of the (R,S)-atenolol. (R,S)-atenolol is a β-adrenergic receptor antagonist.

Phosphatidylcholine is the main phospholipid component in eukaryotic biofilms. Phosphatidylcholine exists in commensal or pathogenic bacteria associated with eukaryotes in prokaryotes. Phosphorylcholine exhibits a surprising range of immunomodulatory properties.

Br-Mmc (4-Bromomethyl-7-methoxycoumarin) is often used as fluorescent label for the determination of compounds possessing a carboxylic group. Br-Mmc is used for the determination fatty acids by TLC or HPLC.

Orcinol (3,5-Dihydroxytoluene) is an organic compound used as biological dye and indicator for proteomics research.

NIR-H2O2 is a cell-permeable near-infrared (NIR) fluorescent turn-on sensor. NIR-H2O2 has both absorption and emission in the NIR region. NIR-H2O2 responds to H2O2 with a large turn-on NIR fluorescence signal upon excitation in the NIR region. NIR-H2O2 is capable of imaging endogenously produced H2O2 in living cells and mice.

NIR-Thiol dinitrobenzenesulfonate has both absorption and emission in the NIR region. NIR-Thiol dinitrobenzenesulfonate responds to thiol with a large turn-on NIR fluorescence signal upon excitation in the NIR region. NIR-Thiol dinitrobenzenesulfonate is capable of imaging endogenously produced thiol in living cells and mice.

NIR dye-1 (Compound 1h) is a near-infrared (NIR) fluorescent dye. NIR dye-1 has absorption and emission in the NIR region, while retaining an optically tunable hydroxyl group.

Vilazodone carboxylic acid is a vilazodone metabolite observed in both urine (major) and plasma (minor).

Phthalic acid is the final common metabolite of phthalic acid esters (PAEs). Phthalic acid can be used for the synthesis of synthetic agents, such as isophthalic acid (IPA), and terephthalic acid (TPA). Phthalic acid has applications in the preparation of phthalate ester plasticizers.

(R)-Apremilast ((R)-CC-10004) is a enantiomer of Apremilast.

Argireline acetate (Acetyl hexapeptide-3 acetate) is a non-toxic, skin-permeable, antiwrinkle peptide. Argireline acetate significantly inhibits Ca2+ dependent neurotransmitter release (acetylcholine) at the neuromuscular junction. Argireline acetate has antiwrinkle and anti-aging activity.

Sincalide ammonium (Cholecystokinin octapeptide ammonium) is a rapid-acting amino acid polypeptide hormone analogue of cholecystokinin (CCK) for intravenous use in postevacuation cholecystography. Sincalide ammonium is an agent that promotes gallbladder contraction by injection and helps diagnose gallbladder and pancreas disorders. The hepatobiliary physiologic effect of Sincalide ammonium is to increase bile secretion, cause the gallbladder to contract and relax the sphincter of Oddi, resulting in bile drainage into the duodenum.

Xenopsin TFA, a neurotensin-like octapeptide from Xenopus laevis skin. Xenopsin TFA is an inhibitor of Tetragastrin stimulated gastric acid secretion.

Fibronectin Adhesion-promoting Peptide (Heparin Binding Peptide) is one of the heparin-binding amino acid sequences found in the carboxy-terminal heparin-binding domain of fibronectin. It promotes assembly of mesenchymal stem cell (MSC) spheroids into larger aggregates. Fibronectin Adhesion-promoting Peptide directly promotes the adhesion, spreading, and migration of endothelial cells by reacting with heparin binding domains of cells.

Hexa-D-arginine TFA (Furin Inhibitor II TFA) is a stable furin inhibitor with Ki values 106 nM, 580 nM and 13.2 μM for furin, PACE4 and prohormone convertase-1 (PC1), respectively. Hexa-D-arginine TFA blocks Pseudomonas exotoxin A and anthrax toxins toxicity in vitro and in vivo.

Amylin, amide, human TFA, a 37-amino acid polypeptide, is a pancreatic hormone cosecreted with insulin that exerts unique roles in metabolism and glucose homeostasis. Amylin, amide, human TFA inhibits glucagon secretion, delays gastric emptying, and acts as a satiety agent.

Neuromedin U, rat TFA is a 23-amino acid brain-gut peptide. Neuromedin U (NMU), through its cognate receptor NMUR2 in the central nervous system, regulates several important physiological functions, including energy balance, stress response, and nociception.

PKG inhibitor peptide TFA is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a Ki of 86 μM.

Secretin (28-54), human TFA is a 27-amino acid residue C-terminally amidated peptide, which acts on human secretin receptors.

Fibrinopeptide B, human TFA (FPB,human TFA), human is a 14-aa peptide, released from the amino-terminus of β-chains of fibrinogen by thrombin.

Secretin, porcine TFA (Porcine secretin TFA) is a 27-amino acid peptide, acting on pancreatic acinar cells and ductal epithelial cells stimulating the production of bicarbonate rich fluid.

Fibrinopeptide A, human TFA is a 16-residue short polypeptide cleaved from fibrinogen by thrombin. Fibrinopeptide A, human locates at the NH2-termini of the Aα chain.

BNP-45 (rat) TFA is a circulating form of rat brain natriuretic peptide isolated from rat heart with potent hypotensive and natriuretic potency.

HPV16 E7 (86-93) TFA is a human leukocyte antigen (HLA)-A2.1 restricted HPV16 E7-derived peptide. HPV16 E7 (86-93) TFA is immunogenic in cervical carcinomas.

β-Casomorphin (1-5), bovine (TFA) is a peptide of bovine β-Casomorphin.

Caerulein, desulfated TFA is the desulfurated form of Caerulein. Caerulein is a decapeptide having the same five carboxyl-terminal amino acids as gastrin and cholecystokinin (CCK).

SEB Domain 144-153 TFA is Staphylococcal Enterotoxin B domain amino acid residue 144-153. SEB Domain 144-153 inhibits transcytosis of multiple staphylococcal enterotoxins, SEA, SEE, and TSST-1. Staphylococcal enterotoxin B (SEB) is a toxin produced by Staphylococcus aureus.

Lanreotide acetate (BIM 23014 acetate) is a somatostatin analogue with antineoplastic activity. Lanreotide acetate is used for treatment for carcinoid syndrome.

GIP (1-30) amide (Human) is a glucose-dependent insulinotropic polypeptide fragment. Glucose-dependent insulinotropic polypeptide (GIP) is an incretin hormone that stimulates insulin secretion and reduces postprandial glycaemic excursions. GIP (1-30) amide (Human) dose-dependently promotes insulin secretion over the range 10-9-10-6 M.

GIP (1-30) amide (Human) TFA is a glucose-dependent insulinotropic polypeptide fragment. Glucose-dependent insulinotropic polypeptide (GIP) is an incretin hormone that stimulates insulin secretion and reduces postprandial glycaemic excursions. GIP (1-30) amide (Human) TFA dose-dependently promotes insulin secretion over the range 10-9-10-6 M.

CCP peptide is a synthetic cyclic citrullinated peptide (CCP) and used as the substrate for detecting anti-CCP antibodies serologically. CCP peptide functions as a target for autoantibodies with a very high specificity for rheumatoid arthritis (RA).

CCP peptide TFA is a synthetic cyclic citrullinated peptide (CCP) and used as the substrate for detecting anti-CCP antibodies serologically. CCP peptide TFA functions as a target for autoantibodies with a very high specificity for rheumatoid arthritis (RA).

KISS1-305, the Metastin/Kisspeptin analog, is a prototype peptide and a chemical probe. KISS1-305 has suboptimal KISS1R agonistic activity, and resists plasma protease degradation.

TAT-amide is a cell penetrating peptide. Cell-penetrating peptides (CPPs) are short amino acid sequences able to enter different cells.

TAT-amide TFA is a cell penetrating peptide. Cell-penetrating peptides (CPPs) are short amino acid sequences able to enter different cells.

AtPep3 is a hormone-like peptide. AtPep3 can enhance salinity tolerance of plants and inhibits the salt-induced bleaching of chlorophyll in seedlings.

AtPep3 TFA is a hormone-like peptide. AtPep3 TFA can enhance salinity tolerance of plants and inhibits the salt-induced bleaching of chlorophyll in seedlings.

CGGRGD, a RGD derivative with cysteine as its N-terminal, CGGRGD is synthesized via solid-phase peptide synthesis technique and the surface of PCL fibers is aminolysised by amino 2-cyanobenzothiazole followed by the addition of 2-cyanobenzothiazole (CBT).

CGGRGD TFA, a RGD derivative with cysteine as its N-terminal, CGGRGD TFA is synthesized via solid-phase peptide synthesis technique and the surface of PCL fibers is aminolysised by amino 2-cyanobenzothiazole followed by the addition of 2-cyanobenzothiazole (CBT).

3-Hydroxy-4-methoxyacetophenone(Acetoisovanillone; Isoacetovanillone) is an active compound isolated from P. spinosa. Isoacetovanillone possesses anti-inflammatory activity and prevented injuries due to administration of acetic acid in the colon.

Nonadecanoic acid is a 19-carbon long saturated fatty acid. Nonadecanoic acid is the major constituent of the substance secreted by Rhinotermes marginalis to defence.

Methyl nonadecanoate may be used as an internal standard to determine fatty acid methyl ester (FAME) content of biodiesel.

Indole-3-carboxaldehyde (3-Formylindole), a cabbage extract, is the product of the oxidative degradation of indole-3-acetic acid (IAA) by crude enzyme preparations from etiolated pea seedlings. Indole-3-carboxaldehyde (3-Formylindole) is a biochemical used to prepare analogs of the indole phytoalexin cyclobrassinin.

2-Chloroadenosine, a stable adenosine analogue, protects against long term development of ischaemic cell loss in the rat hippocampus. 2-Chloroadenosine is an apparent competitive inhibitor of uridine influx (apparent Ki=33 μM) and high-affinity nitrobenzylthioinosine binding (apparent Ki=0.18 mM). 2-Chloroadenosine is a transported permeant for the nucleoside transporter in human erythrocytes.

Vanillin acetate is easily synthesized from vanillin by treatment with acetic anhydride.

2'-O-Methyladenosine, a methylated adenine residue is found in urine of normals as well as in urine of adenosine deaminase (ADA) deficient patients. 2'-O-Methyladenosine exhibits unique hypotensive activities .

Triethyl citrate is an ester of citric acid. Triethyl citrate can be used as a plasticizer for cellulosic plastic-based nanocomposites.

Pyridoxal 5'-phosphate hydrate, the active form of vitamin B6, is an essential cofactor for multiple enzymes, including aromatic l-amino acid decarboxylase that catalyzes the final stage in the production of the neurotransmitters dopamine and serotonin. Pyridoxal 5'-phosphate hydrate is the most important coenzyme variant in the process of vitamin B6 intracellular phosphorylation and is interconvertible with other variants, including pyridoxine 5′‐phosphate (PNP) and pyridoxamine 5′‐phosphate (PMP).

N-Acetyl-L-methionine, a human metabolite, is nutritionally and metabolically equivalent to L-methionine. L-methionine is an indispensable amino acid required for normal growth and development.

Vanillyl butyl ether is a major contributor to the characteristic flavor and fragrance of vanilla. Vanillyl butyl ether is one of the eco-friendly and nontoxic substances. Vanillyl butyl ether has been proposed as a mild warming agent providing a warming sensation and enhancing the blood circulation.

Neryl acetate is a chemical compound isolated from citrus oils.

Disodium succinate is the disodium salt of Succinic acid. Succinic acid is an intermediate product of the tricarboxylic acid cycle, as well as one of fermentation products of anaerobic metabolism.

Paracetamol (4-acetamidophenol). 2-Acetamidophenol is a promising analgesic and an anti-arthritic agent.

Glycyl-l-leucine is a dipeptide that can be a common substrate for glycyl-leucine dipeptidase.

Terpinen-4-ol (4-Carvomenthenol), a naturally occurring monoterpene, is the main bioactive component of tea-tree oil. Terpinen-4-ol suppresses inflammatory mediator production by activated human monocytes. Terpinen-4-ol significantly enhances the effect of several chemotherapeutic and biological agents.

Cyclosporin D, a metabolite of Cyclosporin A, is a weak immunosuppressant. Cyclosporin D is used as internal standard for quantification of Cyclosporin A. Cyclosporin A is a potent immunosuppressant drug, suppress T cell activation by inhibiting calcineurin and the calcineurin-dependent transcription factors nuclear factor of activated T cells (NFAc).

Glufosinate ammonium, a phosphinic acid analogue of glutamic acid, is an herbicide which is converted by plant cells into PT (L-phosphinothricin). Glufosinate ammonium exerts neurotoxic activity.

Glufosinate, a phosphinic acid analogue of glutamic acid, is a herbicide which is converted by plant cells into PT (L-phosphinothricin). Glufosinate exerts neurotoxic activity.

Tricarballylic acid, a conjugate acid of a tricarballylate, is a competitive inhibitor of the enzyme aconitate hydratase (aconitase; EC 4.2.1.3) with a Ki value of 0.52 mM.

4-Nitrophenyl α-D-galactopyranoside (PNP-alpha-D-Gal) is an artificial substrate of 4-nitrophenyl (pNP) glycopyranoside for detecting α-galactosidase activity. The amount of released pNP is significantly increased when 4-Nitrophenyl α-D-galactopyranoside is used as substrates.

OR-1855, an active metabolite of Levosimendan, has effect on human myometrial contractility. Levosimendan is a calcium sensitiser used in the management of acutely decompensated congestive heart failure.

(S)-Tenofovir ((S)-GS 1278) is the less active S-enantiomer of Tenofovir. Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV).

4-Hydroxyacetophenone (P-hydroxyacetophenone) is a key hepatoprotective and choleretic compound in Artemisia capillaris and A. morrisonensis, also has an anti-hepatitis B virus effect and anti-inflammatory effect.

Tropinone, an alkaloid, acts as a synthetic intermediate to Atropine.

Prochloraz is a broad-spectrum contact imidazol fungicide used against several diseases in wheat, barley and oleaginous plants but also for treatment of flower production. It is a fungicide known to have multiple effects on the endocrine system of vertebrates.

Amino-PEG8-alcohol is a PEG derivative containing an amino group with a hydroxyl group. The amino group is reactive with carboxylic acids, activated NHS esters, carbonyls (ketone, aldehyde) etc. The hydroxyl group enables further derivatization or replacement with other reactive functional groups. PEG Linkers may be useful in the development of antibody drug conjugates and drug delivery methods.

L-Butyrine is a member of the class of compounds known as L-alpha-amino acids. L-alpha-Amino acids are alpha amino acids which have the L-configuration of the alpha-carbon atom. L-alpha-aminobutyric acid is soluble (in water) and is a moderately acidic compound (based on its pKa). L-alpha-Aminobutyric acid is a non-proteogenic amino acid that can be found in the human kidney, in liver tissues, and in most biofluids or excreta (e.g. feces, breast milk, urine, and blood). Within the cell, L-alpha-aminobutyric acid is primarily located in the cytoplasm. alpha-Aminobutyric acid is biosynthesized by transaminating oxobutyrate, a metabolite in isoleucine biosynthesis. As a non-proteogenic amino acid, alpha-aminobutyric acid can be used by nonribosomal peptide synthases. One example of a nonribosomal peptide containing alpha-aminobutyric acid is ophthalmic acid, which was first isolated from calf lens. alpha-Aminobutyric acid is a non-essential amino acid that is primarily derived from the catabolism of methionine, threonine, and serine. High protein diets can result in significantly higher alpha-aminobutyrate levels in plasma (PMID: 26227325 ). alpha-Aminobutyric acid is elevated in the plasma of children with Reye's syndrome, tyrosinemia, homocystinuria, nonketotic hyperglycinemia, and ornithine transcarbamylase deficiency (PMID: 420125 ). alpha-Aminobutyric acid is one of the three isomers of aminobutyric acid. The two other are the neurotransmitter gamma-aminobutyric acid (GABA) and beta-aminobutyric acid (BABA) which is known for inducing plant disease resistance.

Isopropyl myristate is the ester of isopropyl alcohol and myristic acid.

Ditridecyl phthalate is a phthalate ester. Phthalate esters are esters of phthalic acid and are mainly used as plasticizers, primarily used to soften polyvinyl chloride. They are found in a number of products, including glues, building materials, personal care products, detergents and surfactants, packaging, children's toys, paints, pharmaceuticals, food products, and textiles. Phthalates are hazardous due to their ability to act as endocrine disruptors.

Diisononyl phthalate (DINP) is a phthalate used as a plasticizer. DINP is typically a mixture of chemical compounds consisting of various isononyl esters of phthalic acid.

Leucic acid, L- is a metabolite of the branched-chain amino acid leucine. It is commonly sold as a purported muscle building supplement. It also has fungicidal properties. HICA was shown to increase protein synthesis and muscle mass in rats who were recovering from a period of induced atrophy.

Asulam is a wild oat herbicide used in prairie regions for control of wild oats in cereal grains such as wheat.

Abarelix is a synthetic decapeptide and antagonist of naturally occurring gonadotropin-releasing hormone (GnRH). Abarelix directly and competitively binds to and blocks the gonadotropin releasing hormone receptor in the anterior pituitary gland, thereby inhibiting the secretion and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone. As a result, this may relieve symptoms associated with prostate hypertrophy or prostate cancer, since testosterone is required to sustain prostate growth.

Aclarubicin is an oligosaccharide anthracycline antineoplastic antibiotic isolated from the bacterium Streptomyces galilaeus. Aclarubicin intercalates into DNA and interacts with topoisomerases I and II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. Aclarubicin is antagonistic to other agents that inhibit topoisomerase II, such as etoposide, teniposide and amsacrine. This agent is less cardiotoxic than doxorubicin and daunorubicin.

Alitretinoin, or 9-cis-retinoic acid, is a form of vitamin A. Alitretinoin is an orally- and topically-active naturally-occurring retinoic acid with antineoplastic, chemopreventive, teratogenic, and embryotoxic activities. Alitretinoin binds to and activates nuclear retinoic acid receptors (RAR) and retinoid X receptors (RXR); these activated receptors act as transcription factors, regulating gene expression that results in the inhibition of cell proliferation, induction of cell differentiation, and apoptosis of both normal cells and tumor cells.

Amsacrine is an aminoacridine derivative with potential antineoplastic activity. Although its mechanism of action is incompletely defined, amsacrine may intercalate into DNA and inhibit topoisomerase II, resulting in DNA double-strand breaks, arrest of the S/G2 phase of the cell cycle, and cell death. This agent's cytotoxicity is maximal during the S phase of the cell cycle when topoisomerase levels are greatest. In addition, amsacrine may induce transcription of tumor promoter p53 protein and block p53 ubiquitination and proteasomal degradation, resulting in p53-dependent tumor cell apoptosis.

Bicalutamide is a synthetic, nonsteroidal antiandrogen. Bicalutamide competitively binds to cytosolic androgen receptors in target tissues, thereby inhibiting the receptor binding of androgens. This agent does not bind to most mutated forms of androgen receptors.

Carmofur (INN) or HCFU (1-hexylcarbamoyl-5-fluorouracil) is a pyrimidine analogue used as an antineoplastic agent. It is a derivative of fluorouracil.

Degarelix, also known as FE-200486 and ASP-3550, is a long-acting, synthetic peptide with gonadotrophin-releasing hormone (GnRH) antagonistic properties. Degarelix targets and blocks GnRH receptors located on the surfaces of gonadotroph cells in the anterior pituitary, thereby reducing secretion of luteinizing hormone (LH) by pituitary gonadotroph cells and so decreasing testosterone production by interstitial (Leydig) cells in the testes. Degarelix acetate was approved in 2008.

Estramustine phosphate sodium is a synthetic molecule that combines estradiol and nornitrogen mustard through a carbamate link. Estramustine and its major metabolite estramustine bind to microtubule-associated proteins (MAPs) and tubulin, thereby inhibiting microtubule dynamics and leading to anaphase arrest in a dose-dependent fashion. This agent also exhibits anti-androgenic effects. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Floxuridine is a fluorinated pyrimidine monophosphate analogue of 5-fluoro-2'-deoxyuridine-5'-phosphate (FUDR-MP) with antineoplastic activity. As an antimetabolite, floxuridine inhibits thymidylate synthetase, resulting in disruption of DNA synthesis and cytotoxicity. This agent is also metabolized to fluorouracil and other metabolites that can be incorporated into RNA and inhibit the utilization of preformed uracil in RNA synthesis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Flutamide, also known as SCH13521, is a toluidine derivative and nonsteroidal antiandrogen that is structurally related to bicalutamide and nilutamide. Flutamide and its more potent active metabolite 2-hydroxyflutamide competitively block dihydrotestosterone binding at androgen receptors, forming inactive complexes which cannot translocate into the cell nucleus. Formation of inactive receptors inhibits androgen-dependent DNA and protein synthesis, resulting in tumor cell growth arrest or transient tumor regression. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Formylmelphalan was approved in China for treating cancer. Formylmelphalan is an alkylating agents, which could cross-link DNA.

Fotemustine is a chloroethylating nitrosourea with antineoplastic activity. Fotemustine alkylates guanine by forming chloroethyl adducts at the 6 position of guanine, resulting in N1-guanine and N3-cytosine cross linkages, inhibition of DNA synthesis, cell cycle arrest, and finally apoptosis. This agent is lipophilic and crosses the blood-brain barrier. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Glyfosfin is an alkylatin agent and a DNA cross-linking agent with anticancer activity. Glyfosfin was approved for treating cancer in China, which belongs to alkylating agents. Glyfosfin was approved in China.

Goserelin is a synthetic decapeptide analog of luteinizing hormone-releasing hormone (LHRH) with antineoplastic activity. Goserelin binds to and activates pituitary gonadotropin releasing hormone (GnRH) receptors. Prolonged administration of goserelin inh

Heptaplatin (Sunpla) is a new platinum derivative with anticancer activity against various cancer cell lines, including cisplatin-resistant cancer cell lines. Heptaplatin has been reported to have a response rate of 17% as a single agent, and tolerable toxicity in the treatment of advanced gastric cancer.

Histrelin acetate is a nonapeptide analog of gonadotropin-releasing hormone (GnRH) with added potency. When present in the bloodstream, it acts on particular cells of the pituitary gland called gonadotropes. Histrelin stimulates these cells to release luteinizing hormone and follicle-stimulating hormone. Thus it is considered a gonadotropin-releasing hormone agonist or GnRH agonist. Histrelin is marketed by Endo Pharmaceuticals under the brand names Vantas and Supprelin LA. Histrelin is used to treat hormone-sensitive cancers of the prostate in men and uterine fibroids in women. In addition, histrelin has been proven to be highly effective in treating central precocious puberty in children. It is available as a daily intramuscular injection. Histrelin is also available in a 12-month subcutaneous implant (Vantas) for the palliative treatment of advanced prostate cancer (since 2005 in the US, and since Jan 2010 in the UK. A 12-month subcutaneous implant (Supprelin LA) for central precocious puberty (CPP) was approved on May 3, 2007 by the U.S. Food and Drug Administration. (See http://en.wikipedia.org/wiki/Histrelin.)

Lanreotide is a a synthetic cyclic octapeptide analogue of somatostatin. Lanreotide inhibits the secretion of growth hormone (GH) by binding to pituitary somatostatin receptors, and may inhibit the release of various other hormones, including thyroid stimulating hormone (TSH) and the gastroenteropancreatic hormones insulin, glucagon and gastrin. This agent also decreases circulating total and free insulin-like growth factor 1 (IGF-I). Lanreotide exhibits a high binding affinity for somatostatin receptor 2 (SSTR-2) and a lesser binding affinity for SSTR-5. However, compared to octreotide, this agent is less potent in inhibiting the release of growth hormone from the pituitary gland. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

Leucovorin calcium is a n active metabolite of folic acid (also called folinic acid and citrovorum factor), which does not require metabolism by dihydrofolate reductase, the molecular target of folate antagonist-type chemotherapeutic drugs. Leucovorin calcium counteracts the toxic effects of these medications, 'rescuing' the patient while permitting the antitumor activity of the folate antagonist. This agent also potentiates the effects of fluorouracil and its derivatives by stabilizing the binding of the drug's metabolite to its target enzyme, thus prolonging drug activity.

Mechlorethamine, an antineoplastic nitrogen mustard also known as HN2 hydrochloride, is a nitrogen analog of sulfur mustard. It is a light yellow brown, crystalline, hygroscopic powder that is very soluble in water and also soluble in alcohol. (Source: http://www.rxlist.com/mustargen-drug.htm).

Megestrol acetate is the acetate ester of megestrol, a synthetic derivative of the naturally occurring female sex hormone progesterone, with progestogenic, antiestrogenic, and antineoplastic activities. Mimicking the action of progesterone, megestrol binds to and activates nuclear progesterone receptors (PRs) in the reproductive system and pituitary; ligand-receptor complexes are translocated to the nucleus where they bind to progesterone response elements (PREs) located on target genes.

Mercaptopurine is a thiopurine-derivative antimetabolite with antineoplastic and immunosuppressive activities. Produced through the metabolism of mercaptopurine by hypoxanthine-guanine phosphoribosyltransferase (HGPRT), mercaptopurine metabolites 6-thioguanosine-5'-phosphate (6-thioGMP) and 6-thioinosine (T-IMP) inhibit nucleotide interconversions and de novo purine synthesis, thereby blocking the formation of purine nucleotides and inhibiting DNA synthesis.

Methylene blue is a synthetic basic dye. Methylene blue stains to negatively charged cell components like nucleic acids; when administered in the lymphatic bed of a tumor during oncologic surgery, methylene blue may stain lymph nodes draining from the tumor, thereby aiding in the visual localization of tumor sentinel lymph nodes. When administered intravenously in low doses, this agent may convert methemoglobin to hemoglobin.

Mitobronitol (1,6-dibromo-1,6-dideoxy-D-mannitol) is a brominated analog of mannitol. It is an anticancer drug that is classified as an alkylating agent. (Source: http://en.wikipedia.org/wiki/Mitobronitol)

Nafarelin is a gonadotropin-releasing hormone agonist (GnRH agonist) which acts as an analog of GnRH. Nafarelin increases the release of FSH and LH by the anterior pituitary, which in turn leads to an increase of estrogen/progesterone. When administered, Nafarelin has the purpose of causing increase estrogen that will negatively feed back upon hypothalamus to decrease GnRH ( negative feedback loop ) Through negative feedback, Nafarelin causes a decrease in pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH). Nafarelin may be used in the treatment of estrogen-dependent conditions (such as endometriosis or uterine fibroids), to treat central precocious puberty, and to control ovarian stimulation in IVF. It is normally delivered via a nasal spray. Nafarelin acetate is marketed by Searle (now part of Pfizer) under the brand name Synarel.

NIMUSTINE is a antineoplastic agent especially effective against malignant brain tumors. The resistance which brain tumor cells acquire to the initial effectiveness of this drug can be partially overcome by the simultaneous use of membrane-modifying agents such as reserpine, calcium antagonists such as nicardipine or verapamil, or the calmodulin inhibitor, trifluoperazine. The drug has also been used in combination with other antineoplastic agents or with radiotherapy for the treatment of various neoplasms. (Source: http://pubchem.ncbi.nlm.nih.gov/compound/nimustine#section=Top)

This medication is used alone or with other medications to prevent nausea and vomiting caused by cancer drug treatment (chemotherapy) and radiation therapy. It is also used to prevent and treat nausea and vomiting after surgery. It works by blocking one of the body's natural substances (serotonin) that causes vomiting.

Pipobroman (trade names Vercite, Vercyte) is an anti-cancer drug that probably acts as an alkylating agent. It is marketed by Abbott Laboratories. Pipobroman (PB) has well documented clinical activity in polycythemia vera (PV) and essential thrombocythemia (ET).

Triptorelin, a decapeptide (pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2), is a gonadotropin-releasing hormone agonist (GnRH agonist) used as the acetate or pamoate salts. By causing constant stimulation of the pituitary, it decreases pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH). Like other GnRH agonists, triptorelin may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, precocious puberty, estrogen-dependent conditions (such as endometriosis or uterine fibroids), and in assisted reproduction. It is also used as therapy for gender identity disorder.

Ponatinib, also known as AP24534 is an oral drug for the treatment of chronic myeloid leukemia (CML) and Philadelphia chromosome–positive (Ph+) acute lymphoblastic leukemia (ALL). It is a multi-targeted tyrosine-kinase inhibitor. Some forms of CML, those that have the T315I mutation, are resistant to current therapies such as imatinib. Ponatinib has been designed to be effective against these types of tumors. Ponatinib was approved in 2012.

Carubicin HCl is an anthracycline antineoplastic antibiotic isolated from the bacterium Actinomadura carminata. Carubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis.

Amikacin is an antibiotic used for a number of bacterial infections. This includes joint infections, intraabdominal infections, meningitis, pneumonia, sepsis, and urinary tract infections. It is also used for the treatment of multidrug-resistant tuberculosis. It is used either by injection into a vein or muscle. Amikacin is in the aminoglycoside family of medications. It works by blocking the function of the bacteria's 30S ribosomal subunit, making it unable to make protein.

Misonidazole is a radiosensitizer used in radiation therapy to cause normally resistant hypoxic tumor cells to become sensitive to the treatment.

Doxorubicin free base, also called doxorubicin, is an anthracycline antibiotic with antineoplastic activity. Approved API for cancer therapeutic use is doxorubicin HCl. Doxorubicin, isolated from the bacterium Streptomyces peucetius var. caesius, is the h

Mitoxantrone is an anthraquinone that intercalates in DNA and inhibits topoisomerase II (IC50 = 5.3 μM), thus inhibiting cell proliferation. It also inhibits HIV-1 integrase (IC50 = 3.8 μM). Mitoxantrone is exported from cells in an ATP- and glutathione-dependent manner by multidrug resistance protein-1.4 Formulations containing mitoxantrone have been used in the treatment of cancer and multiple sclerosis.

Miriplatin (MPT) is a novel platinum complex used in TACE that shows promise for the treatment of hepatocellular carcinoma (HCC). Miriplatin is a lipophilic platinum complex that can be easily suspended in Lipiodol and gradually releases active platinum compounds in tumor tissue. Miriplatin is less severe toxicity profile compared to other platinum anticancer agents.

Idoxuridine is an anti-herpesvirus antiviral and anticancer drug. It is a nucleoside analogue, a modified form of deoxyuridine, similar enough to be incorporated into viral DNA replication, but the iodine atom added to the uracil component blocks base pairing. It is used only topically due to cardiotoxicity. It was synthesized by William Prusoff in the late 1950s. Initially developed as an anticancer drug, idoxuridine became the first antiviral agent in 1962.

Ceritinib, also known as LDK-378, is a selective inhibitor of ALK1, a target found in metastatic non-small cell lung cancer (NSCLC). In Phase I trials, LDK378 showed a marked clinical response in 78 patients with anaplastic lymphoma kinase positive (ALK+) metastatic non-small cell lung cancer (NSCLC) who had progressed during or after crizotinib therapy or had not been previously treated with crizotinib. LDK378 blocks the ALK protein and stops it sending growth signals to cancer cells, which may stop them growing. Ceritinib was approved in April 2014.

Triptorelin is a gonadotropin-releasing hormone agonist (GnRH agonist) used as the acetate or pamoate salts. By causing constant stimulation of the pituitary, it decreases pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH). Like other GnRH agonists, triptorelin may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, precocious puberty, estrogen-dependent conditions (such as endometriosis or uterine fibroids), and in assisted reproduction. It is also used as therapy in cases of gender dysphoria.

Abiraterone acetate is an FDA approved drug, and is an orally active acetate ester of the steroidal compound abiraterone with antiandrogen activity. Abiraterone acetate was approved by the U.S. Food and Drug Administration (FDA) in April 2011. Abiraterone inhibits the enzymatic activity of steroid 17alpha-monooxygenase (17alpha-hydrolase/C17,20 lyase complex), a member of the cytochrome p450 family that catalyzes the 17alpha-hydroxylation of steroid intermediates involved in testosterone synthesis. Administration of this agent may suppress testosterone production by both the testes and the adrenals to castrate-range levels. FDA Approval this drug in May 2011.

Alanosine, also known as L-alanosine, is an amino acid analogue and antibiotic derived from the bacterium Streptomyces alanosinicus with antimetabolite and potential antineoplastic activities. L-alanosine inhibits adenylosuccinate synthetase, which converts inosine monophospate (IMP) into adenylosuccinate, an intermediate in purine metabolism. L-alanosine-induced disruption of de novo purine biosynthesis is potentiated by methylthioadenosine phosphorylase (MTAP) deficiency. The clinical use of this agent may be limited by its toxicity profile. MTAP is a key enzyme in the adenine and methionine salvage pathways.

Apricoxib, also known as Benzenesulfonamide 42(4ethoxyphenyl)4methyl1Hpyrrol1yl, is an orally bioavailable nonsteroidal anti-inflammatory agent (NSAID) with potential antiangiogenic and antineoplastic activities. Apricoxib binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), thereby inhibiting the conversion of arachidonic acid into prostaglandins. Apricoxib-mediated inhibition of COX-2 may induce tumor cell apoptosis and inhibit tumor cell proliferation and tumor angiogenesis. COX-related metabolic pathways may represent crucial regulators of cellular proliferation and angiogenesis.

Sardomozide HCl, also known as SAM486A or CGP48664, is a second-generation polyamine synthesis inhibitor, which inhibits the activity of the polyamine biosynthetic enzyme S-adenosylmethionine decarboxylase (SAMDC). SAM486 is more potent and specific than the first-generation SAMDC inhibitor methylglyoxal (bis) guanylhydrazone (MGBG). Preclinical testing confirmed promising antiproliferative activity. The in vitro tests showed that p53 wild-type NB cells were highly sensitive to SAM486A treatment. Most notably, SAM486A treatment resulted in the rapid accumulation of proapoptotic proteins p53 and Mdm2.

Becatecarin, also known as BMY-27557, XL119 and BMS-181176, is a synthetic diethylaminoethyl analogue of the indolocarbazole glycoside antineoplastic antibiotic rebeccamycin. Becatecarin intercalates into DNA and stabilizes the DNA-topoisomerase I complex, thereby interfering with the topoisomerase I-catalyzed DNA breakage-reunion reaction and initiating DNA cleavage and apoptosis.

Crolibulin, also known as EPC2407 and crinobulin, is a small molecule tubulin polymerization inhibitor with potential antineoplastic activity. Microtubulin inhibitor EPC2407 binds to the colchicine-binding site on beta-tubulin and inhibits the polymerization of tubulin into microtubules, which may result in cell cycle arrest, the induction of apoptosis, and the inhibition of tumor cell proliferation. As a vascular disruption agent (VDA), this agent also disrupts tumor neovascularization, which may result in a reduction in tumor blood flow and tumor hypoxia and ischemic necrosis.

CVT-6883, also known as GS6201 is a selective A2B adenosine antagonist, represents a novel potential approach to treating cardiopulmonary diseases. A pre-clinical study showed that CVT-6883 significantly reduced elevated markers of inflammation, fibrosis and pulmonary injury in in vivo preclinical models.

Darinaparsin, also know as ZIO-101 and SP-02, is a small-molecule organic arsenical with potential antineoplastic activity. Although the exact mechanism of action is unclear, darinaparsin, a highly toxic metabolic intermediate of inorganic arsenicals (iAs) that occurs in vivo, appears to generate volatile cytotoxic arsenic compounds when glutathione (GSH) concentrations are low. The arsenic compounds generated from darinaparsin disrupt mitochondrial bioenergetics, producing reactive oxygen species (ROS) and inducing ROS-mediated tumor cell apoptosis; in addition, this agent or its byproducts may initiate cell death by interrupting the G2/M phase of the cell cycle and may exhibit antiangiogenic effects.

Efaproxiral, also known as RSR13, is an analogue of the cholesterol drug bezafibrate developed for the treatment of depression, traumatic brain injury, ischemia, stroke, myocardial infarction, diabetes, hypoxia, sickle cell disease, hypercholesterolemia and as a radio sensitiser. One use for efaproxiral is to increase the efficacy of certain chemotherapy drugs which have reduced efficacy against hypoxic tumours, and can thus be made more effective by increased offloading of oxygen into the tumour tissues

Eniluracil, also known as GW776 and GW776C85, is an orally active and irreversible inhibitor of dihydropyrimidine dehydrogenase. Eniluracil inhibits dihydropyrimidine dehydrogenase, the rate-limiting enzyme that catabolizes and inactivates 5-fluorouracil (5-FU) in the liver. Co-administration of ethynyluracil permits the oral administration of 5-FU. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Exherin, also known as ADH-1, is a small, cyclic pentapeptide vascular-targeting agent with potential antineoplastic and antiangiogenic activities. ADH-1 selectively and competitively binds to and blocks N-cadherin, which may result in disruption of tumor vasculature, inhibition of tumor cell growth, and the induction of tumor cell and endothelial cell apoptosis. N-cadherin, a cell- surface transmembrane glycoprotein of the cadherin superfamily of proteins involved in calcium-mediated cell-cell adhesion and signaling mechanisms; may be upregulated in some aggressive tumors and the endothelial cells and pericytes of some tumor blood vessels. Note: The old CAT# for this product was 201350A

GS-9219 is a prodrug of the acyclic nucleoside phosphonate analogue 9-(2-phosphonylmethoxyethyl)guanine (PMEG) with potential antineoplastic activity. Formulated to selectively accumulate in lymphocytes, nucleotide analogue GS 9219 is converted to its active metabolite, PMEG diphosphate (PMEGpp), via enzymatic hydrolysis, deamination, and phosphorylation; subsequently, PMEGpp is incorporated into nascent DNA chains by DNA polymerases, which may result in the termination of DNA synthesis, S-phase cell cycle arrest, and the induction of apoptosis in susceptible lymphoma cell populations.

Hypothemycin is a resorcylic acid lactone polyketide that has fungicidal, kinase inhibitory, and anticancer properties. Hypothemycin inhibits MEK and other protein kinases containing a conserved cysteine residue in the ATP-binding domain. Hypothemycin inhibits proliferation of cancer cell lines dependent on activating mutations.

Symadex, also known as imidazoacridone; XLS-002 and C-1311, is a member of the novel imidazoacridinone family of anticancer agents. Imidazoacridone has shown activity in experimental tumour models both in vitro and in nude mice. C-1311 at the EC(99) dose delayed progression of cells through the S phase which was followed by G2 arrest. C-1311 does not induce rapid apoptosis in HT-29 cells, instead drug exposure leads to prolonged G2 arrest followed by G2 to M transit and cell death during mitosis in the process of mitotic catastrophe.

Iincyclinide, also known as CMT-3 and COL-3, is a MMP inhibitor and a chemically-modified tetracycline with potential antineoplastic activity. Incyclinide inhibits matrix metalloproteinases (MMPs), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis. This agent also causes mitochondrial depolarization in tumor cells and induces both cellular apoptosis and tissue necrosis.

Indibulin is a synthetic small molecule with antimitotic and potential antineoplastic activities. Indibulin binds to a site on tubulin that is different from taxane- or Vinca alkaloid-binding sites, destabilizing tubulin polymerization and inducing tumor cell cycle arrest and apoptosis. This agent has been shown to be active against multidrug-resistant (MDR) and taxane- resistant tumor cell lines. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Aldoxorubicin, also known as INNO-206 and Doxo-EMCH, is the 6-maleimidocaproyl hydrazone derivative prodrug of the anthracycline antibiotic doxorubicin with antineoplastic activity. INNO-206 binds selectively to the cysteine-34 position of albumin via its maleimide moiety. Doxorubicin is released from the albumin carrier after cleavage of the acid-sensitive hydrazone linker within the acidic environment of tumors and, once located intracellularly, intercalates DNA, inhibits DNA synthesis, and induces apoptosis. Albumin tends to accumulate in solid tumors as a result of high metabolic turnover, rapid angiogenesis, hyervasculature, and impaired lymphatic drainage. Because of passive accumulation within tumors, this agent may improve the therapeutic effects of doxorubicin while minimizing systemic toxicity.

INSM-18, also known as nordihydroguaiaretic acid, NDGA and masoprocol, is a naturally occurring antioxidant dicatechol originally derived from the creosote bush Larrea divaricatta with antipromoter, anti-inflammatory, and antineoplastic activities. NDGA directly inhibits activation of two receptor tyrosine kinases (RTKs), the insulin-like growth factor receptor (IGF-1R) and the c-erbB2/HER2/neu receptor, resulting in decreased proliferation of susceptible tumor cell populations.