UN2811, NEW! Life Science
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GNF-5
Cayman ChemicalA selective allosteric inhibitor of Bcr-Abl (IC50s = 4.52, 0.38, and 0.93 µM against Bcr-Abl mutants G250E, E255V, and M351T, respectively); displays additive inhibitory activity against T315I Bcr-Abl mutants both in in vitro assays and in a recalcitrant T315I Bcr-Abl mutant mouse…
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Diclofenac-d4
Cayman ChemicalIntended for use as an internal standard for the quantification of diclofenac by GC- or LC-MS.
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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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Carmustine
Cayman ChemicalA nitrogen mustard β-chloro-nitrosourea compound used as an alkylating agent to form interstrand crosslinks in DNA, which leads to cancer cell cytotoxity and apoptosis; also reported to inhibit glutathione reductase, thioredoxin reductase, and lipoamide dehydrogenase.
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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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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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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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Salinomycin (sodium salt)
Cayman ChemicalAn antibacterial and coccidiostat compound that shows selective toxicity for HMLER breast cancer stem cells (IC50 = ~24 μM); 8 μM treatment of 4T1 and MCF-7-Ras breast cancer cell lines decreases cancer stem cell growth ~2-fold and ~3-fold, respectively; 5 mg/kg inhibits mammary…
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Paxilline
Cayman ChemicalAn indole diterpene which potently and reversibly inhibits large conductance Ca2+-activated K+ (BKCa) channels, as shown in patch clamp (Ki = 1.9 nM) and whole smooth muscle cell studies (Ki = 35.7 nM).
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Rotenone
Cayman ChemicalA classical inhibitor of complex I of the mitochondrial electron transport chain, inhibiting NADH/DB oxidoreductase and NADH oxidase with IC50 values of 28.8 and 5.1 nM, respectively; used in animal models of Parkinson’s disease.
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Colcemid
Cayman ChemicalA colchicine derivative that inhibits tubulin polymerization (IC50 = 2.1 μM) with low toxicity; suppresses microtubule dynamicity, inhibits cell migration, blocks microtubule assembly, and arrests cells in metaphase; used to synchronize cells and for karyotyping in cytogenetic studies.
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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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1,24-dihydroxy Vitamin D3
Cayman ChemicalAn analog of 1,24-dihydroxy vitamin D3 which, when used in a 4 μg/g ointment, suppresses psoriasis; inhibits the growth of both normal and psoriatic human keratinocytes (IC50 ~ 10 nM) via the vitamin D receptor; suppresses the production of RANTES and IL-8 by human dermal fibroblasts.
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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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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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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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Actinomycin D
Cayman ChemicalA cyclic polypeptide-containing anticancer antibiotic that binds to DNA and blocks transcription by interfering with RNA synthesis; ~10 nM promotes cell death in a variety of tumors.
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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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GSK2193874
Cayman ChemicalA potent, selective antagonist of TRPV4 channels, blocking the influx of calcium induced by the TRPV4 agonist GSK634775 with IC50 values of 2, 5, and 40 nM for rat, mouse, and human isoforms, respectively; effective in vivo, as it resolves pulmonary edema resulting from myocardial…
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Quercetin
Cayman ChemicalA flavonoid compound found in the bark and rinds of many plants and fruits.
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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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(+)-Etomoxir (sodium salt)
Cayman ChemicalAn irreversible inhibitor of carnitine palmitoyltransferase 1, a mitochondrial enzyme involved in fatty acid β-oxidation (IC50 = 5-20 nM in rat liver); also acts as a direct agonist of PPARα.
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4-hydroxy Diclofenac
Cayman ChemicalA CYP2C9 metabolite of the NSAID diclofenac that demonstrates anti-inflammatory and analgesic properties by inhibiting COX and suppressing PGE2 synthesis.
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Aminopterin
LKT LabsAminopterin is a folic acid analog and derivative of pterin; it is very similar to methotrexate in structure. Aminopterin exhibits anticancer chemotherapeutic and immunosuppressive activities. Like other folic acid analogs, aminopterin inhibits dihydrofolate reductase, depleting nucleotide pools…
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Capsaicin
Cayman ChemicalThe primary active component of the heat and pain-eliciting lipid-soluble fraction of the Capsicum pepper and present in natural hot pepper extracts; elicits a sensation of burning pain by activation of TRPV1 on small, non-myelinated polymodal C-type nociceptive nerve fibers and has been widely…
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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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Cycloheximide
Cayman ChemicalAn inhibitor of protein synthesis in eukaryotes (IC50 = 5-50 μM) that functions by interfering with translational elongation; can either induce or inhibit apoptosis depending on cell type.
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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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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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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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25-hydroxy Vitamin D2
Cayman ChemicalAn intermediate produced from vitamin D2 by cytochrome P450 isoforms in vertebrates; subsequently metabolized to 1,25-dihydroxy vitamin D2, which is an agonist for the vitamin D receptor.
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Sinensetin
Cayman ChemicalA polymethoxylated flavone that has been shown to enhance adipogenesis and lipolysis, to inhibit α-glucosidase and α-amylase activity, and to suppress the expression of genes associated with inflammation by regulating IκBα.