Biologically Active Small Molecules, 100 mg, Cayman Chemical
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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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L-Mimosine
Cayman ChemicalA non-protein amino acid that chelates iron and copper; inhibits certain enzymes that contain iron or copper, including arginase (IC50 = 3.7 µM).
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Aztreonam
Cayman ChemicalA monobactam antibiotic that is effective against Gram-negative bacteria but inactive against Gram-positive bacteria.
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10-HDA
Cayman ChemicalAn unsaturated fatty acid found in royal jelly produced from honeybees; demonstrates longevity-promoting effects in C. elegans, down regulates matrix metalloproteinases (MMPs) in rheumatoid arthritis, inhibits VEGF-induced angiogenesis in HUVECs, facilitates differentiation of neurons from neural…
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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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Docosahexaenoic Acid
Cayman ChemicalAn essential fatty acid and the most abundant ω-3 fatty acid in neural tissues, especially in the retina and brain; constitutes as much as 40% of the total PUFA pool in retinal and neuronal membranes; dietary supplementation via fish oil inhibits the progression of atherosclerosis and delays…
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Asiatic Acid
Cayman ChemicalA natural triterpene which stimulates wound healing; induces cell cycle arrest and apoptosis in breast cancer cells (IC50 = 5.9 µM for MCF-7 cells); blocks angiogenesis in glioblastomas; down regulates BACE1 while increasing ADAM10 maturation in primary rat cortical neurons; protects against…
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Fluvoxamine (maleate)
Cayman ChemicalA selective serotonin reuptake inhibitor (Ki = 6.2 nM in rat hypothalamus) with comparatively little effect on noradrenaline reuptake (Ki = 1,100 nM); potentiates the pharmacological effects of serotonin and its precursor, 5-hydroxy tryptophan, in the CNS resulting in antidepressant effects.
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Concanavalin A
Cayman ChemicalA plant lectin that selectively cross-links cell-surface glycoproteins and affects the initiation of cell agglutination, mitogenesis, and apoptosis; widely used in affinity chromatography purifications of various glycoproteins and cellular structures; also used to induce liver injury in…
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1,2-Diphytanoyl-sn-glycero-3-PE
Cayman ChemicalA phospholipid containing the tetramethylated long-chain (16:0) diphytanic acid inserted at the sn-1 and sn-2 positions.
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HET0016
Cayman Chemical20-HETE is a major biologically active CYP450 metabolite of arachidonic acid in the kidney and liver. It regulates renal vascular and tubular functions as well as vascular tone in the cerebral circulation. HET0016 is an inhibitor of 20-HETE formation in human renal microsomes with an…
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Gaboxadol (hydrochloride)
Cayman ChemicalA GABAA receptor agonist whose potency varies depending on the receptor subunit composition (partial agonist at α1β2γ2 (ED50 = 143 µM), full agonist at α5 (ED50 = 28-129 µM), and super agonist at α4β3δ (ED50 = 6 µM)); acts as an antagonist…
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Leupeptin (hemisulfate)
Cayman ChemicalA reversible inhibitor of cysteine, serine, and threonine proteases; inhibits cathepsin B (Ki = 6 nM), calpain (Ki = 10 nM), trypsin (Ki = 35 nM), plasmin (Ki = 3.4 μM), and kallikrein (Ki = 19 μM), and has no effect against chymotrypsin, elastase, renin, or pepsin.
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5'-Deoxy-5'-methylthioadenosine
Cayman ChemicalAn intermediate in the generation of adenine and methionine that is produced by the decarboxylation of SAM; a potent agonist of adenosine receptors (Kis = 0.15, 1.13, 13.9, and 0.68 μM for A1, A2A, A2B, and A3, respectively); inhibits several enzymes at higher concentrations.
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Monoacylglycerol Lipase Inhibitor 21
Cayman ChemicalSelectively and reversibly blocks MAGL activity (IC50s = 0.18 and 59 µM for MAGL and FAAH in mouse brain, respectively); does not inhibit ABHD6, ABHD12, CB1, or CB2 receptors (Kis > 10 µM); used to ameliorate disease progression in a mouse model of multiple sclerosis.
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Hydroxy Dimetridazole
Cayman ChemicalA metabolite of dimetridazole, the nitroimidazole-based antibacterial and anticoccidial agent suspected to be carcinogenic and mutagenic to humans.
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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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EA4
Cayman ChemicalA quinone derivative that inhibits red blood cell PLA2 with a Ki value of 130 µM.
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GYY 4137
Cayman ChemicalA water-soluble, slow-releasing H2S donor which demonstrates vasodilator and anti-hypertensive activity in hypertensive rats when given intravenously; also protects against endotoxic shock in rats, inhibiting pro-inflammatory signaling.
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Flumazenil
Cayman ChemicalAn imidazobenzodiazepine derivative that competitively inhibits benzodiazepine binding to GABAA receptors (IC50 = 2 nM); used to reverse sedation induced by benzodiazepine drugs and is effective in the treatment of benzodiazepine overdose or withdrawal.
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2,4-DPD
Cayman ChemicalA cell permeable, competitive inhibitor of HIF-PH with effective concentrations in the low µM range.
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Ursolic Acid
Cayman ChemicalA natural triterpenoid carboxylic acid that is known to have antioxidative, antimicrobial, anti-inflammatory, and anticancer activities; inhibits Na+/K+-ATPase activity (IC50 = 24.7 μM) and blocks NF-κB activation in various human cancer cells lines (10-100 μM), inhibiting cell…
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Celecoxib
Cayman ChemicalAn anti-inflammatory compound from the diaryl heterocycle class that selectively inhibits COX-2 (IC50s = 22.9 and 0.05 μM for COX-1 and COX-2, respectively; displays chemopreventive activity in multiple tumor types via proapoptotic effects independent of its capacity to block COX-2.
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Mn(III)TBAP
Cayman ChemicalMn(III)TBAP is a cell-permeable SOD mimic. At a concentration of 30 µM, it decreases the doubling time of SOD-null E. coli. by 2-fold.
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L-Leucine 4-methoxy-ß-naphthylamide (hydrochloride)
Cayman ChemicalA cell-permeable substrate for aminopeptidase M and leucine aminopeptidase that was developed for intracellular analysis of protease activities.
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DL-Cystathionine
Cayman ChemicalAn intermediate in the synthesis of cysteine that is produced from homocysteine and serine by the action of cystathionine-β-synthase; excess cystathionine in the urine is a hallmark of cystathioninuria.
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17-Octadecynoic Acid
Cayman ChemicalA suicide inhibitor of LTB4 20-hydroxylase and renal CYP450 ω-hydroxylase.
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CFDA-SE
Cayman ChemicalA stable, cell-permeable dye employed to assay cell proliferation as it is partitioned with high fidelity between daughter cells for up to eight generational divisions.
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Spermine NONOate
Cayman ChemicalSpermine NONOate is a NO donor. It spontaneously dissociates in a pH-dependent, first-order process with a half-life of 39 minutes and 230 minutes at 37°C and 22-25°C, respectively, (pH 7.4) to liberate 2 moles of NO per mole of parent compound.
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Pirfenidone
Cayman ChemicalAn orally active small molecule drug with antioxidant, anti-inflammatory, and anti-fibrotic effects; reduces inflammatory cytokine production, suppresses TGF-β expression, and lowers markers of oxidative stress; has effectiveness in IPF and other conditions with a significant fibrotic component.
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Vildagliptin
Cayman ChemicalAn inhibitor of DPP-4 (IC50 = 3.5-34 nM); also inhibits DPP-8 and DPP-9 (Ki = 810 and 95 nM, respectively) but not DPP-2 or FAPα; blocks the degradation of several circulating peptides, including incretins; reduces fasting and postprandial glucose levels and decreases inflammatory…
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Ezetimibe
Cayman ChemicalA selective cholesterol transport inhibitor that targets the NPC1L1 (KDs = 12,000, 540, 40, and 220 nM for its glucuronide in mouse, rat, rhesus monkey, and human, respectively); blocks intestinal cholesterol absorption in various animal models (IC50s = 0.0005-0.05 mg/kg).