Biologically Active Small Molecules, 1 mg, UN2811

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UN2811 1 mg Biologically Active Small Molecules

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  • Cayman Chemical

    A PAR4 antagonist (IC50 = 140 nM) that exhibits 71-fold selectivity for PAR4 over PAR1 (IC50 = 10 μM) in isolated human platelets.

  • 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.

  • Cayman Chemical

    A type B trichothecene mycotoxin found in cereals contaminated with certain Fusarium species.

  • Cayman Chemical

    A synthetic prodrug of 1,25-dihydroxy vitamin D2; used to suppress the synthesis and secretion of parathyroid hormone in secondary hyperparathyroidism; stimulates bone growth; inhibits the growth of certain blastomas and prostate cancer cells.

  • Cayman Chemical

    An anticoagulant; differs from (+)-warfarin by being five times more potent as a vitamin K antagonist; has a shorter terminal elimination half-life (24-33 hours) than (+)-warfarin (35-58 hours).

  • Cayman Chemical

    A major metabolite of clozapine; used in designer receptor exclusively activated by designer drug, also known as DREADD, technology to modulate synthetic receptors in vivo.

  • Cayman Chemical

    An ATP-competitive B-Raf inhibitor (IC50 = 10 nM; Kd = 2.4 nM) that inhibits cell proliferation both in B-Raf mutated and wild-type melanoma cell lines.

  • Cayman Chemical

    A potent, selective inhibitor of BMP1 (IC50 = 44 nM); effective in a cell-based model of collagen deposition is very effective at penetrating human skin in vitro.

  • Cayman Chemical

    A c-Myc inhibitor that binds to and distorts the bHLH-ZIP domain of c-Myc (Kd = 2.8 µM), thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity (IC50 = 146 µM); cytotoxic to c-Myc-overexpressing cells lines (IC50s = 15.6 and…

  • Cayman Chemical

    An A2A adenosine receptor antagonist.

  • Cayman Chemical

    A potent inhibitor of the STAT3/JAK signaling pathway; suppresses levels of tyrosine phosphorylated STAT3, STAT3 DNA binding and STAT3-mediated gene transcription; suppresses tumor growth in vivo.

  • Cayman Chemical

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

  • Cayman Chemical

    A natural product which acts as a small molecule inhibitor of HIF signaling, disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar concentrations; effectively attenuates the HIF pathway both in cells and in vivo, in mice.

  • Cayman Chemical

    The active circulating metabolite of vitamin D2 formed by 25-hydroxylase in the liver and 25-hydroxyvitamin D-hydroxylase in the kidney.

  • Cayman Chemical

    An anti-cancer natural product that acts on a variety of cellular pathways; activates caspases, inhibits anti-apoptotic proteins, alters expression of Bcl-2 and Bax; acts as a potent, slow inhibitor of Kir2.1 channels; inhibits the chymotrypsin activity of the 20S proteasome; has effects on AMPK,…

  • Cayman Chemical

    A mycotoxin that inhibits the mitochondrial ATP synthetase system; inhibits soluble ATPase (KD = 4.1 µM), ADP-stimulated respiration in isolated rat liver mitochondria (KD = 0.15 µM), and ATP-driven reduction of NAD+ by succinate (KD = 2 µM).

  • An internal standard for the quantification of verapamil (hydrochloride) by GC- or LC-MS.

  • Cayman Chemical

    A non-competitive, cell permeable inhibitor of calcium transport by SERCAs (IC50 values are cell type-dependent and range from ~2-80 nM); increases intracellular calcium, leading to cell activation, histamine release, and increased cell proliferation; has anti-inflammatory and anti-cancer effects…

  • Cayman Chemical

    A type A trichothecene mycotoxin.

  • Cayman Chemical

    A macrolide that causes the formation of bundles of intracellular microtubules in non-mitotic cells, induces the formation of hyperstable tubulin polymers, and arrests cell cycling in mitosis; induces mitotic arrest at nanomolar IC50 values in cell lines from ovarian, breast, lung, colon, prostate,…

  • Cayman Chemical

    A mycotoxin produced by fungi of the Fusarium genus that is phytotoxic to various agriculture grain crops, cardiotoxic to poultry and rats, and cytotoxic to human red blood cell progenitors (IC50 = 4.1 μM).

  • Cayman Chemical

    A trichothecene mycotoxin that can be converted to DON in the body.

  • Cayman Chemical

    A fungal toxin that demonstrates selective inhibition of HDAC3/NcoR over HDAC6 (IC50s = 15.8 and 665.1 nM, respectively); has broad spectrum activity against Apicomplexan parasites and exhibits antiproliferative activity against various cancer cell lines (IC50s = 0.13-2.36 μM).

  • Cayman Chemical

    A non-irritant bronchodilator with relaxant activity on human bronchial muscle; binds to the mouse recombinant EP3 and EP4 receptors with Ki values of 330 and 190 nM, respectively.

  • Cayman Chemical

    6-keto PGE1 is a metabolite isolated after the incubation of PGI2 with rabbit liver microsomes. However, it is not produced in appreciable amounts following IV infusion of PGI2 in humans. 6-keto PGE1 is equipotent with PGI2 as a vasodilator; in most other aspects its activity resembles PGE1.

  • Cayman Chemical

    A muscarinic receptor agonist (EC50s = 23, 48, and 63 nM for M1, M3, and M5, respectively, and >1 µM for M2 and M4); stimulates secretion by salivary glands and is useful in ameliorating xerostomia (dry mouth).

  • Cayman Chemical

    A group A trichothecene mycotoxin derived by the metabolism of T-2 toxin.

  • Cayman Chemical

    A major Alternaria mycotoxins commonly found as a food contaminant (LD50 = 548 μg/egg in the chicken embryo toxicity assay) and linked to esophageal cancer in human populations at risk of high exposure; Mice fed 100 mg/kg/day orally for 10 months developed precancerous lesions on the esophageal mucosa.

  • Cayman Chemical

    A nonapeptide hormone primarily synthesized in the hypothalamus with roles in uterine contraction and lactation, social memory and attachment, sexual and maternal behavior, aggression, learning, anxiety, feeding, and pain perception.

  • Cayman Chemical

    A natural mycotoxin that binds F-actin; contains a carboxyl group for coupling reactions.

  • Cayman Chemical

    A mycotoxin from F. moniliforme, a fungus of grains; at 1 μM, inhibits sphingosine N-acyltransferase; fumonisins, found as contaminants in foods, induce apoptosis via altered sphingolipid metabolism, resulting in hepatotoxicity and nephrotoxicity.

  • Cayman Chemical

    An intermediate in the pathway leading to the production of 1,25-dihydroxy vitamin D3; plasma or serum levels are commonly used as an indicator of an individual’s vitamin D status.

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