Bottle, Glass, Clear, UN2811
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Doxepin (hydrochloride)
Cayman ChemicalA tricyclic antidepressant that inhibits the reuptake of serotonin and norepinephrine and acts as an antagonist at histamine, serotonin, adrenergic, and muscarinic receptors with Ki values in the nanomolar range.
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5-Fluorouracil
Cayman ChemicalA pyrimadine analog that irreversibly inhibits thymidylate synthase, blocking the synthesis of thymidine which is required for DNA synthesis; widely used to treat many gastrointestinal tract adenocarcinomas.
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Valinomycin
Cayman ChemicalA cyclododecadepsipeptide potassium-selective ionophore antibotic; induces apoptosis in several cell tyes, including CHO cells, by stimulating potassium efflux.
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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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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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Nicardipine (hydrochloride)
Cayman ChemicalA dihydropyridine L-type calcium channel antagonist that displays antihypertensive and antianginal activity; selectively inhibits adenosine A3 receptors (Ki = 3.25 µM) and CYP3A4 catalytic activity (IC50 = 0.148 µM); activates TRPA1 channels, producing an increase in Ca2+…
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6-diazo-5-oxo-L-nor-Leucine
Cayman ChemicalA glutamine analog that inhibits glutaminases (Ki = 6 µM) and other glutamine-utilizing enzymes, including cytidine triphosphate synthase.
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(S)-Naproxen
Cayman Chemical(S)-Naproxen is a non-selective COX inhibitor. The IC50 values for human recombinant COX-1 and -2 are 0.6-4.8 µM and 2.0-28.4 µM, respectively.
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Ibotenic Acid
Cayman ChemicalA neuroexcitatory amino acid that functions as a NMDA and metabotropic glutamate receptor agonist; used to induce brain lesions in animal models of cognitive dysfunction.
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Bupivacaine
Cayman ChemicalAn amino-amide anesthetic that binds to the intracellular portion of voltage-gated sodium channels and blocks sodium influx into nerve cells, preventing the generation of an action potential; inhibits the uptake of dopamine in striatal synaptosomes by 47% at 100 µM.
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Cylindrospermopsin
Cayman ChemicalA cyanobacterial toxin that targets protein and glutathione synthesis in hepatocytes (IC50s = 1.3 and 2.4 µM, respectively), inhibits uridine monophosphate synthase complex activity (Ki = 10 µM), and induces DNA damage.
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Genipin
Cayman ChemicalA protein cross-linking agent isolated from G. jasminoides Ellis; inhibits UCP2 activity; 5 µM genipin increases glucose-stimulated insulin secretion in isolated pancreatic islets chronically exposed to high levels of glucose; induces apoptosis in FaO rat hepatoma cells and human…
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Etoricoxib
Cayman ChemicalA dipyridinyl compound that demonstrates high in vitro and ex vivo selectivity for COX-2 over COX-1.
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Prostaglandin E1
Cayman ChemicalPGE1 is the theoretical COX metabolite of DGLA, but it is virtually undetectable in the plasma of normal humans or other animals. Its pharmacology includes vasodilation, hypotension, and anti-platelet activities. The IC50 of PGE1 for the inhibition of ADP-induced human platelet…
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Microcystin-RR
Cayman ChemicalA toxin produced by cyanobacteria that inhibits the catalytic activity of protein phosphatases PP1C, PP1γ, and PP2A with Ki values of 0.15, 0.24, and 0.018 nM, respectively.
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Brefeldin A
Cayman ChemicalA natural fungal metabolite which reversibly interferes with protein trafficking and secretion mediated by the Golgi apparatus and endoplasmic reticulum; directly and reversibly inhibits Sec7 domain-containing GEFs which are necessary for Arf activation associated with vesicular transport (IC50 =…
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Carprofen
Cayman ChemicalAn NSAID commonly used in animals to combat pain and inflammation, particularly as associated with osteoarthritis; inhibits both COX-1 and COX-2 (IC50s = 22.3 and 3.9 µM, respectively) and also FAAH (IC50 = 74 µM).
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Quercetin
Cayman ChemicalA flavonoid compound found in the bark and rinds of many plants and fruits.
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Brevetoxin B
Cayman ChemicalA neurotoxin that binds to voltage-gated sodium channels (IC50 = 15 nM) on neurons at the neuromuscular junction, causing the channel to open irreversibly at potentials more negative than normal, discharging action potentials repetitively; ichthyotoxic at nanomolar concentrations.
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Pargyline (hydrochloride)
Cayman ChemicalPargyline is an irreversible inhibitor of monoamine oxidase (MAO) that is used clinically to treat moderate hypertension. At 10 mg/kg iv, pargyline induces a moderate decrease of systolic blood pressure in unanaesthetized hypertensive rats but not normotensive WKR or Sprague-Daley rats. The…
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Indomethacin
Cayman ChemicalA non-selective COX inhibitor with IC50 values for ovine COX-1 and -2 of 0.1 and 6 µM, respectively; IC50 values for human recombinant COX-1 and -2 are 1.67 and 24.6 µM, respectively.
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Endothall
Cayman ChemicalAn herbicide that is used to control a wide range of terrestrial and aquatic plants.
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Beraprost (sodium salt)
Cayman ChemicalBeraprost is an analog of prostacyclin in which the unstable enol-ether has been replaced by a benzofuran ether function. This modification increases the plasma half-life from 30 seconds to several hours, and permits the compound to be taken orally. Doses of 20-100 µg in humans, given 1 to 3…
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Xylazine
Cayman ChemicalAn agonist of α2 adrenergic receptors (Ki = 194 nM); used for sedation, anesthesia, and analgesia in non-human mammals.
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17ß-hydroxy Wortmannin
Cayman ChemicalAn analog of wortmannin; irreversibly binds PI3K; inhibits recombinant PI3K and mTOR (IC50 = 2.7 and 193 nM, respectively) and prevents the growth of LNCap cells (IC50 = 1.46 μM).
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6-Thioguanine
Cayman ChemicalA thio analog of the purine base guanine that incorporates into DNA during replication, inducing double-strand breaks that destabilize its structure and result in cytotoxicity; used as a chemotherapeutic for acute leukemia and other types of cancer, including BRCA2-mutated tumors.
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1-hydroxy Vitamin D3
Cayman ChemicalA synthetic prodrug which is converted to the vitamin D receptor agonist 1,25-dihydroxy vitamin D3 in vivo; suppresses the synthesis and secretion of parathyroid hormone in secondary hyperparathyroidism; supports bone growth; provides renal and cardiovascular protection during chronic kidney disease.
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Pentylenetetrazole
Cayman ChemicalA central nervous system modulator that is used to experimentally induce seizures in animals; used extensively to screen for compounds that block the production of nonconvulsive (absence or myoclonic) seizures.
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Luotonin A
Cayman ChemicalAn alkaloid that inhibits the growth of mouse leukemia P388 cells (IC50 = 1.8 μg/ml); binds to and stabilizes the topoisomerase I-DNA binary complex, leading to DNA breakage and cell death (IC50 = 5.07-12.6 μM); selectively inhibits CYP1A1 and CYP1A2 (IC50 = ~6 μM for…
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XAV939
Cayman ChemicalA small molecule inhibitor of tankyrase 1 and 2 (IC50 = 11 and 4 nM, respectively); increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin; inhibits colony formation of APC-deficient colorectal cancer cells at 0.33 µM.
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Myriocin
Cayman ChemicalMyriocin is an amino fatty acid antibiotic derived from certain thermophylic fungi, in this case Mycelia sterilia. It is a potent immunosuppressant having 10- to 100-fold more activity than cyclosporin A. Myriocin is a potent inhibitor of serine palmitoyltransferase (Ki = 0.28 nM), the enzyme that…
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Riluzole (hydrochloride)
Cayman ChemicalA benzothiazole derivative with anti-excitotoxic effects that acts by blocking the presynaptic release of glutamate, indirectly antagonizing glutamate receptors, and inactivating neuronal voltage-gated Na+ channels (ED50 = 2.3 μM); suppresses glutamate-induced seizures in rats (ED50 =…