Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • Cayman Chemical

    Microcystins are hepatotoxic cyclic heptapeptide toxins produced by cyanobacteria. They are responsible for periodic poisonings of humans and livestock drinking fresh water where the blue-green algae are endemic. Microcystin-LR is a selective inhibitor of protein phosphatase 2A (PP2A) (IC50= 0.04…

  • Cayman Chemical

    A selective inhibitor of CaMKII, competitively blocking CaM binding to the kinase (Ki = 370 nM); inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM).

  • Amitriptyline exhibits antidepressant, antipsychotic, analgesic, and antinociceptive activities; it acts as an antagonist at 5-HT2A/2C/6/7 receptors, M1-5 muscarinic acetylcholine receptors (mAChRs), H1/4 histamine receptors, a1-adrenergic receptors, and also on the serotonin transporter (SERT) and…

  • Cayman Chemical

    A long chain saturated fatty acid ethyl ester found in small quantities in liverwort, C. concium.

  • Cayman Chemical

    A dehydration product of PGD2 formed by the elimination of the C-9 hydroxyl group; inhibits platelet aggregation (IC50 ~ 5-10 nM); has antimitotic and antiproliferative effects on a variety of cultured normal cells and tumor cell lines.

  • Cayman Chemical

    A 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…

  • A competitive inhibitor of 15-hydroxy PGDH; acts as an agonist on most EP receptor subtypes (Kd d~ 1 nM for isolated EP2 receptors); preserves the self-renewal properties while preventing the differentiation of hematopoietic stem cells during expansion in culture.

  • Cayman Chemical

    An inhibitor of human recombinant PDE5 (IC50 = 5.9 µM); used to treat erectile dysfunction and has been shown to have anti-cancer and antioxidant activity; induces differentiation of cardiomyocytes and increases the proliferation and differentiation of cultured human osteoblasts.

  • Cayman Chemical

    Can be formed by the dimerization of two molecules of α-trans-cinnamic acid; significantly blocks inflammatory pain while having little effect on neurogenic pain, as indicated by the formalin test in mice.

  • A bile salt formed in the liver by conjugation of cholic acid with taurine that can be used to solubilize lipids and membrane-bound proteins.

  • Cayman Chemical

    Cloprostenol is a synthetic PGF2α analog and a potent FP receptor agonist. (+)-15-epi Cloprostenol is the 15(S), or 15β-hydroxy enantiomer of (+)-cloprostenol. This epimer is less active by several orders of magnitude as an FP receptor ligand when compared to 15(R)-cloprostenol. However,…

  • AFC is a synthetic substrate for the isoprenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase). Because it is able to serve as a substrate for the methyltransferase, it effectively functions as an inhibitor of methylation of endogenous isoprenylated proteins.

  • Cayman Chemical

    A β-adrenergic receptor agonist with potent positive inotropic effects in vivo; strongest effects on β1 receptors, with lesser but significant β2 receptor activation and only weak α1 receptor actions; strongly increases cardiac contractility.

  • Cayman Chemical

    A pan-caspase inhibitor that blocks apoptosis, prevents the production of cytokines, and inhibits T cell proliferation dose-dependently at 1-100 μM.

  • Cayman Chemical

    CAS Number: 444932-31-4 Molecular Formula: C20H19N3O4 Formula Weight: 365.4

  • An inhibitor of ethylene biosynthesis that, at 1 µM, blocks the activity of both ACSs and ACOs; reduces ethylene-mediated plant changes in growth and development; inhibits cystathionine γ-lyase (Ki = 10.5 μM) with slow- and tight-binding characteristics.

  • Cayman Chemical

    A membrane-permeable cationic dye that is a substrate for P-gp and is rapidly exported from cells with functional P-gp; also accumulates within mitochondria and can be used to both localize mitochondria and study their properties.

  • Cayman Chemical

    A dual purpose probe; a chemiluminescent probe that detects superoxide production by enzymatic and cellular sources; a fluorescent chloride-sensitive indicator, with fluorescence being quenched by chloride (excitation: 455 nm; emission: 505 nm).

  • Cayman Chemical

    An 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.

  • Cayman Chemical

    An antipsychotic compound that displays high affinity for dopamine receptors (Kis = 2.4, 0.2, and 1.8 nM for D2, D3, and D4, respectively); also has actions as an antagonist, inverse agonist, or channel blocker, with lower affinities, at other receptors and channels.

  • An organophosphorus ester that antagonizes the CB1 receptor and inhibits FAAH with similar potencies (IC50s = 2 nM).

  • Cayman Chemical

    A reversible inhibitor of the cis-Golgi ArfGEF, GBF1 (IC50 = 3.3 µM); induces rapid dissociation of COPI vesicle coat protein from Golgi membranes and disassembly of the Golgi and trans-Golgi network, preventing bidirectional transport of endocytic cargo.

  • Cayman Chemical

    A methyl ester prodrug form of the NOS inhibitor L-NNA; exhibits Ki values of 15 nM, 39 nM, and 4.4 µM for nNOS (bovine), eNOS (human), and iNOS (mouse), respectively.

  • Brain natriuretic peptide (BNP) binds the natriuretic peptide receptor type B (NPR-B) to exert cardiomodulatory activity. BNP is secreted by the heart; it displays lipolytic effects, contributing to fatty acid mobilization in congestive heart failure. High levels of BNP are predictive of…

  • Cayman Chemical

    Intended for use as an internal standard for the quantification of diclofenac by GC- or LC-MS.

  • Brain natriuretic peptide (BNP) binds the natriuretic peptide receptor type B (NPR-B) to exert cardiomodulatory activity. BNP is secreted by the heart; it displays lipolytic effects, contributing to fatty acid mobilization in congestive heart failure. High levels of BNP are predictive of…

  • A derivative of fluphenazine that contains an alkylating chlorethylamine chain, which produces irreversible protein binding; a relatively selective, irreversible antagonist of D2 receptors both in vitro (IC50 = 100 nM) and in vivo; irreversibly inhibits calmodulin at higher doses…

  • Cayman Chemical

    An internal standard for the quantification of ±11(12)-EET by GC- or LC-MS.

  • Tris-HCl Stock Solution (1 M, pH 7.0) contains filtered Tris-HCl (1 M, pH7.0). It is ready to use as supplied.

  • Cayman Chemical

    A cell permeable sulfonamide-based hydroxamic acid that binds to the active site of MMP-3 (Ki = 23 nM) and prevents its activity; inhibits mouse macrophage metalloelastase MME/MMP-12 (IC50 = 13 nM).

  • An irreversible inhibitor of ornithine decarboxylase that suppresses polyamine biosynthesis; displays antiangiogenic, cytostatic, and antiparasitic effects.

  • Cayman Chemical

    A nonpurine inhibitor of xanthine oxidoreductase (Ki = 0.7 nM) that has proven effective in lowering serum urate levels when administered to manage hyperuricemia in patients with gout.

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