Bottle, Glass, Clear, UN2811
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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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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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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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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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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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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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Capsaicin (technical grade)
Cayman ChemicalCapsaicin is the primary active component of the heat and pain-eliciting lipid-soluble fraction of the Capsicum pepper. Capsaicin is present in natural hot pepper extracts along with a number of impurities, including dihydrocapsaicin and several lesser impurities. Separation by HPLC is required in…
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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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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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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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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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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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4-deoxy Nivalenol
Cayman ChemicalA natural type B trichothecene produced by certain species of the fungus Fusarium; inhibits protein biosynthesis, binds to peptidyl transferase, and inhibits the synthesis of RNA and DNA; passes the blood-brain barrier at different rates in different animals.
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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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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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Melphalan
Cayman ChemicalA DNA alkylating agents that induces DNA interstrand and intrastrand crosslinks, cytotoxicity, and apoptosis; inhibits the growth of PC-3 prostate cancer cells with IC50 values of 0.074 or 0.77 μM for sequential dosing or single dosing, respectively.
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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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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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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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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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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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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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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-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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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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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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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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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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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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KT195
Cayman ChemicalA selective inhibitor of ABHD6 (IC50 = 10 nM) with negligible activity against other serine hydrolases such as DAGLβ; used both as a probe to study ABHD6 and as a negative control for studies of DAGLβ.
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Amlodipine
Cayman ChemicalA dihydropyridine L-type calcium channel blocker that selectively inhibits calcium influx in cardiac and vascular smooth muscle; inhibits calcium-induced contractions in depolarized rat aorta (IC50 = 1.9 nM), displaying a slow rate of association and dissociation in isolated vascular and…