Biologically Active Small Molecules, 500 mg
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Floxuridine
Cayman ChemicalA prodrug that is rapidly catabolized in vivo to 5-fluorouracil when administered by rapid injection; inhibits thymidylate synthase (EC50 = 0.6 nM), interfering with DNA synthesis; used to treat various cancers, particularly metastases to the liver.
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Tamoxifen
Cayman ChemicalA selective estrogen receptor (ER) modulator; an ER antagonist in breast tissue, effective in treating early breast cancer; an ER agonist in bone and blood vessels and a partial ER agonist in uterine tissues.
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Ketoconazole
Cayman ChemicalAn orally active broad spectrum antifungal agent that blocks ergosterol biosynthesis by inhibiting the fungal CYP isoform CYP51; potently inhibits the mammalian analog CYP51A1 (IC50 = 63.5 nM), as well as a variety of other CYP isoforms.
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Puromycin (hydrochloride)
Cayman ChemicalAn aminonucleoside antibiotic that blocks protein synthesis in both prokaryotes and eukaryotes by causing premature termination of nascent polypeptide chains; used in assays for peptide-bond formation and elongation and also often used as selective agent in cell culture systems.
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N-Octyl-ß-D-thioglucopyranoside
Cayman ChemicalA low molecular weight nonionic detergent that is commonly used for cell lysis and non-denaturing protein solubilization.
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Omeprazole
Cayman ChemicalA selective and irreversible inhibitor of the gastric H+/K+ ATPase pump (IC50 = 1.1 μM).
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Sulforhodamine 101
Cayman ChemicalA nonfixable red fluorescent dye (excitation max: 586 nm; emission max: 605 nm) that can be used as a specific marker for astrocytes and an activity-dependent probe for monitoring regulated exocytosis.
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a-D-Galactose-1-phosphate (potassium salt)
Cayman ChemicalAn intermediate in the interconversion of glucose and galactose.
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Nifuroxazide
Cayman ChemicalA broad-spectrum nitrofuran antibiotic used against urinary tract infections and as therapy for acute diarrhea of bacterial origin; inhibits the survival and migration of cancer cells, suppressing tumor growth and metastasis in vivo, at least in part by inhibiting STAT3 (IC50 = 10 µM).
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3-chloro-5-hydroxy BA
Cayman ChemicalAn agonist of GPR81 (EC50 = 16 µM) that is inactive against the related GPR109a (HCAR2) receptor; stimulates lipolysis (increased serum free fatty acids) in mice fed high fat chow for 10 weeks; blocks basal ghrelin secretion by primary gastric mucosal cells.
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Corticosterone
Cayman ChemicalA steroid hormone produced in the cortex of the adrenal glands that binds to both glucocorticoid and mineralocorticoid receptors; also is the precursor to aldosterone synthesis.
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CAY10512
Cayman ChemicalCAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.
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Chlorogenic Acid
Cayman ChemicalChlorogenic acid is a phenolic natural product isolated from the leaves and fruits of dicotyledonous plants, including the coffee bean. Structurally, chlorogenic acid is the ester of caffeic acid with the 3-hydroxyl group of quinic acid. Chlorogenic acid is an important factor in plant metabolism.…
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Dihomo-y-Linolenic Acid ethyl ester
Cayman ChemicalDGLA is a metabolite produced by chain elongation of the essential fatty acid γ-linolenic acid. Ethyl DGLA is an esterified version of the free acid which is less water soluble, but more ammenable for the formulation of DGLA-containing diets and dietary supplements. DGLA has been advanced as…
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Amiodarone (hydrochloride)
Cayman ChemicalA class III antiarrhythmic agent; inhibits KCNH2 with an IC50 value of 1 µM; also inhibits CYP2C8 and CYP3A4 in vitro at low micromolar concentrations.
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Dihomo-y-Linolenic Acid
Cayman ChemicalAn elongation product of γ-linolenic acid (18:3), rapidly metabolized by fatty acid desaturases to produce arachidonic acid (20:4); metabolized through the cyclooxygenase pathway to produce 1-series prostaglandins; can reduce atopic dermatitis and atherosclerosis when added to the diet of mice.
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a-Truxillic Acid
Cayman ChemicalCan be formed by the dimerization of two molecules of α-trans-cinnamic acid; significantly blocks inflammatory pain while having little effect on neurogenic pain, as indicated by the formalin test in mice.
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Bromocriptine (mesylate)
Cayman ChemicalA potent dopamine receptor agonist that binds the D2 receptor with highest affinity (Ki = 2.5 nM); avidly binds the serotonin receptors 5-HT1A and 5-HT1D (Ki = 12.9 and 10.7 nM, respectively), as well as α and β adrenoreceptors.
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X-Gal
Cayman ChemicalA cell-permeable, chromogenic substrate for β-galactosidase used in histochemical and molecular biology applications, including detection of lacZ activity in cells and tissues.
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Polymyxin B (sulfate)
Cayman ChemicalA mixture of at least four closely related components, polymyxin B1 to B4, with polymyxin B1 and B2 being the two major components; demonstrates rapid in vitro bactericidal activity against major multidrug-resistant Gram-negative bacteria, including P. aeruginosa, A. baumannii, and K. pneumonia.
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2-phenyl-3-methyl-Quinoxaline
Cayman ChemicalA synthetic intermediate useful for pharmaceutical synthesis.
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Glutathione ethyl ester
Cayman ChemicalA cell permeable derivative of GSH that undergoes hydrolysis by intracellular esterases to release GSH; used to protect cells against damage from radiation, oxidants, and various toxic compounds including heavy metals.
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Rosiglitazone (maleate)
Cayman ChemicalA potent and selective PPARγ ligand, binding to the PPARγ ligand-binding domain with a Kd value of 43 nM.
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Ceftazidime (hydrate)
Cayman ChemicalA broad-spectrum β-lactam antibiotic used for parenteral administration.
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1,2-Dimyristoyl-sn-glycero-3-phosphate (sodium salt)
Cayman ChemicalA phospholipid containing the long-chain (14:0) myristic acid inserted at the sn-1 and sn-2 positions.
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DPPH
Cayman ChemicalA cell-permeable, stable free radical that is commonly used to evaluate the ability of compounds to act as free radical scavengers or hydrogen donors and to measure the antioxidant activity of tissue extracts; followed by color change from purple (absorbance at 515-528 nm) to yellow.
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N-Palmitoyl Glycine
Cayman ChemicalAn 18-carbon saturated fatty acid that is structurally similar to the phospholipid-derived N-acyl ethanolamines; inhibits heat-induced firing of nociceptive neurons in rat dorsal horn; induces transient calcium influx in native dorsal root ganglion (DRG) cells and in the PTX-sensitive, DRG-like…
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Lucigenin
Cayman ChemicalA dual purpose probe; a chemiluminescent probe that detects superoxide production by enzymatic and cellular sources; a fluorescent chloride-sensitive indicator, with fluorescence being quenched by chloride (excitation: 455 nm; emission: 505 nm).
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Cilostazol
LKT LabsCilostazol is a quinolone inhibitor of phosphodiesterase 3B (PDE 3B) that exhibits vasodilatory, antiplatelet, anti-inflammatory, anti-diabetic, antidepressant, anxiolytic, and pro-angiogenic activities. Cilostazol is clinically used to treat intermittent claudication associated with peripheral…
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cis-trismethoxy Resveratrol
Cayman ChemicalA potent anti-mitotic drug that is 100-fold more active than resveratrol at inhibiting the growth of human colon cancer Caco-2 cells; inhibits tubulin polymerization in a dose-dependent manner (IC50 = 4 μM) and enzymes involved in the synthesis of the polyamines, putrescine, and spermidine.