Biologically Active Small Molecules

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UN2811 Cayman Chemical Biologically Active Small Molecules

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  • Cycloheximide

    Cayman Chemical

    An 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.

  • Resiniferatoxin

    Cayman Chemical

    A natural analog of capsaicin that activates TrpV1 with a Ki value of 20 pM; potently and selectively activates of a sub-population of primary afferent neurons.

  • Ketoprofen

    Cayman Chemical

    A non-selective NSAID exhibiting IC50 values of 0.5 and 2.33 µM for human recombinant COX-1 and COX-2, respectively.

  • Cucurbitacin B

    Cayman Chemical

    A plant-derived steroidal triterpene that induces cell cycle arrest or apoptosis in a range of cancer cell lines; inhibits the growth of several breast cancer cell lines (IC50s = 18-50 nM); suppresses the growth of tumors developed from MDA-MB-231 and 4T-1 breast cancer cells in mice.

  • Capsaicin (technical grade)

    Cayman Chemical

    Capsaicin 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…

  • Sinensetin

    Cayman Chemical

    A 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.

  • Quercetin

    Cayman Chemical

    A flavonoid compound found in the bark and rinds of many plants and fruits.

  • Prostaglandin E1

    Cayman Chemical

    PGE1 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…

  • Quinacrine (hydrochloride hydrate)

    Cayman Chemical

    An anti-protozoal agent; prevents misfolding of prion protein (EC50 = 0.3 μM), blocks voltage-dependent sodium channels (IC50 = 3.3 μM), inhibits aldehyde oxidase (IC50 = 3.3 μM), antagonizes the riboflavin-binding protein (Ki = 6.7 μM), inhibits…

  • Cytochalasin E

    Cayman Chemical

    Inhibits actin polymerization; potently and selectively inhibits the growth of endothelial cells (IC50 1 protease activity.

  • DPPH

    Cayman Chemical

    A 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.

  • Rotenone

    Cayman Chemical

    A 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.

  • Genipin

    Cayman Chemical

    A 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…

  • Miltefosine-50 mg

    Cayman Chemical

    An inhibitor of CTP:phosphocholine cytidylyl transferase with antimetastatic properties.

  • Calcitriol

    Cayman Chemical

    Calcitriol is synthesized from 7-dehydrocholesterol in humans via a non-enzymatic photochemical reaction with 290-310 nm UV light in the skin. Hydroxylation of the resulting cholecalciferol in the liver produces 25-hydroxy Vitamin D3, the principal circulating form of Vitamin D. A second, tightly…

  • GNF-5

    Cayman Chemical

    A 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…

  • Aceclidine (hydrochloride)

    Cayman Chemical

    An agonist of muscarinic receptors (EC50 = 1.8-17 µM for human M2).

  • Brimonidine (tartrate)

    Cayman Chemical

    A selective α2-adrenergic receptor agonist (Ki = 183 nM) that lowers intraocular pressure by decreasing aqueous humor synthesis and increasing drainage through uveoscleral outflow; protects rat retinal ganglion cells against glutamate excitotoxicity by inhibiting glutamate release and…

  • Chlorcyclizine (hydrochloride)

    Cayman Chemical

    A histamine H1 receptor antagonist (Ki = 9 nM) that is effective against HCV (EC50 = 44 nM), preventing viral entry into host cells.

  • Phenylbutazone

    Cayman Chemical

    Phenylbutazone is a NSAID and efficient reducing cofactor for the peroxidase activity of COX. It enhances hydrogen peroxide inactivation of both COX and PGI synthase.

  • (±)-Thalidomide

    Cayman Chemical

    An immunomodulatory and antiproliferative compound that interacts directly with the protein CRBN (IC50 = 8.5 nM), a ubiquitously-expressed E3 ligase, and DDB1 complexes.

  • Carprofen

    Cayman Chemical

    An 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).

  • Voriconazole

    Cayman Chemical

    A triazole, antifungal agent that inhibits a broad range of pathogenic yeasts, including Candida (MIC = 0.03-8 µg/ml), and filamentous fungi such as Aspergillus, Scedosporium, and Fusarium by disrupting ergosterol synthesis.

  • 4-deoxy Nivalenol

    Cayman Chemical

    A 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.

  • Pentylenetetrazole

    Cayman Chemical

    A 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.

  • Antimycin A1

    Cayman Chemical

    An antibiotic that inhibits complex III of the mitochondrial ETC, preventing electron transport between cytochromes b and c, which results in the production of superoxide and eventual cell death; inhibits Bcl-2 and Bcl-xL proteins, inducing apoptosis.

  • (+)-Etomoxir (sodium salt)

    Cayman Chemical

    An 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.

  • (±)-Anatoxin A (fumarate)

    Cayman Chemical

    A nicotinic acetylcholine receptor agonist that binds α4β2- and α7-type nicotinic receptors (Kis = 1.3 nM and 1.8 μM, respectively); stimulates [3H]-dopamine release from striatal synaptosomes (EC50 = 134 nM).

  • Idarubicin (hydrochloride)

    Cayman Chemical

    A 4-demethoxy analog of daunorubicin which intercalates in DNA and inhibits topoisomerase II, resulting in cancer cell cytotoxicity at low concentrations (IC50 = 20-120 nM); effective in combination therapy for the treatment of different types of leukemia.

  • Wortmannin

    Cayman Chemical

    A potent, cell-permeable, and irreversible inhibitor of PI3K enzymes (IC50 = 1-10 nM).

  • (+)-Warfarin

    Cayman Chemical

    An anti-coagulant; differs from (−)-warfarin by being five times less potent as a vitamin K antagonist; has a longer terminal elimination half-life (35-58 hours) than (−)-warfarin (24-33 hours).

  • Prostaglandin E1 ethyl ester

    Cayman Chemical

    An esterified form of the free acid which may be more amenable for certain applications.

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