Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • The 6-keto PGF1α Quant-PAK has been designed for the convenient, precise quantification of 6-keto PGF1α by GC- or LC-MS. It includes a 50 µg vial of 6-keto PGF1α-d4 and a precisely weighed vial of unlabeled 6-keto PGF1α, with the precise weight (2-4 mg) indicated on…

  • FTY720

    Cayman Chemical

    A structural analog of sphingosine and a novel immune modulator; inhibits lymphocyte emigration from lymphoid organs; becomes phosphorylated by sphingosine kinase in vivo to act as a potent agonist at S1P1, S1P3, S1P4, and S1P5.

  • The 1,15 lactone of 17-phenyl-trinor PGF2α with potential for suitable pharmacologic activity and an improved side-effect profile over current glaucoma therapeutics.

  • ML-345

    Cayman Chemical

    A selective IDE inhibitor that selectively targets cysteine819 in IDE with an EC50 value of 188 nM.

  • Atropine

    Cayman Chemical

    Non-selective, competitive antagonist of the muscarinic acetylcholine receptor types M1, M2, M3, M4, and M5 (pKBs range from 8.9-9.8); increases firing of the sinoatrial node and conduction through the atrioventricular node of the heart, opposes the actions of the vagus nerve, blocks acetylcholine…

  • Probenecid

    Cayman Chemical

    A benzoic acid derivative that inhibits OAT1, OAT3, and OAT6 with Ki values of 6.3, 9.0, and 8.4 µM, respectively, as well as OAT2 with an IC50 value of 0.67 µM; enhances the renal excretion of urate while reducing the elimination of many medications; acts as an agonist of…

  • Glycitin

    Cayman Chemical

    A natural isoflavone which promotes the proliferation of bone marrow stromal cells and osteoblasts and suppresses bone turnover.

  • 7(Z),11(Z)-Heptacosadiene

    Cayman Chemical

    The predominant female-specific mating pheromone of the fruit fly D. melanogaster that elicits wing vibrations in male D. melanogaster flies at amounts above 100 ng.

  • Ketorolac

    Cayman Chemical

    An NSAID, non-selective COX inhibitor, being marketed as an analgesic to manage postoperative pain as well as an ophthalmic solution to treat ocular pain and inflammation; inhibits COX-1 and COX-2 (IC50s = 20 nM) in vivo.

  • Latanoprost

    Cayman Chemical

    Latanoprost is the isopropyl ester of 17-phenyl-13,14-dihydro PGF2α. It is a prodrug form of the free acid, which is a potent agonist of the FP receptor in the eye. Latanoprost reduces intraocular pressure in glaucoma patients with few side effects. The EC50 value of latanoprost…

  • PKCe Inhibitor Peptide

    Cayman Chemical

    A synthetic peptide corresponding to an amino acid sequence found in the amino terminal C2 domain of most mammalian forms of PKC?; selectively and reversibly inhibits the translocation of PKC? to intracellular membranes, blocking activation.

  • 5a-Androst-16-en-3-one

    Cayman Chemical

    A mammalian pheromone used to prime sexual behavior of sows in estrus for mating or artificial insemination; also used to study receptor-mediated odorant detection and the genetic basis for anosmias.

  • A fundamental component of glucose metabolism involved in the homeostatic regulation of blood glucose levels by participating in glycolysis, glycogen synthesis, and gluconeogenesis.

  • Arachidonic acid ethyl ester is a more lipophilic form of arachidonic acid that can be incorporated into dietary regimens or fed to cultured cells as a source of exogenous arachidonate. It is one of the fatty acid ethyl esters that increase cytosolic Ca2+ concentration leading to pancreatic acinar…

  • Caylin-2

    Cayman Chemical

    A nutlin-3 analog; inhibits the growth of HCT116 cells at high concentrations (IC50 = ~8 µM); promotes the growth of HCT116 cells ~40% at concentrations between 5-100 nM.

  • Sunitinib Malate

    Cayman Chemical

    A small molecule, multi-targeted receptor tyrosine kinase inhibitor; potently inhibits signaling through PDGFR, VEGFR, KIT, and FLT3; inhibits both tumor cell growth and angiogenesis; approved by the FDA for the treatment of gastrointestinal stromal tumor and metastatic renal cell carcinoma.

  • CRT0066101 (hydrochloride)

    Cayman Chemical

    A pan inhibitor PKD (IC50s = 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively); blocks cell proliferation, induces apoptosis, and reduces the viability of pancreatic cancer cells both in vitro and in vivo.

  • ML-030

    Cayman Chemical

    A triazolothiadiazine that inhibits PDE4 (EC50 = 18.7 nM in a cell-based assay); selectively inhibits PDE4A (IC50 = 6.7 nM) over PDE4B1, PDE4B2, PDE4C1, and PDE4D2 (IC50 = 48.2, 37.2, 452, and 49.2 nM, respectively).

  • NADPH (sodium salt)

    Cayman Chemical

    The reduced form of the electron acceptor NADP+ and acts as an electron donor in various biological reactions.

  • 9,12-Octadecadiynoic Acid

    Cayman Chemical

    Ro 3-1314 is an inhibitor of both COX and lipoxygenase. Ro 3-1314 inhibits ram seminal vesicle COX with a Ki of 0.6 µM. It is a more effective inhibitor of COX-1 than of 15-LO, inhibiting 95% and 68%, respectively, of these enzymatic activities when used at a concentration of 48 µM.

  • Bortezomib

    Cayman Chemical

    A dipeptide boronic acid derivative that reversibly inhibits the 20S proteasome (Ki = 0.6 nM); drives cell cycle arrest and apoptosis in cancer cell lines and has applications in multiple myeloma and certain lymphomas, as well as other types of cancer.

  • A stable analog of ATP that acts as a potent agonist of G protein-coupled P2Y2 and P2Y11 receptors (pEC50 = 5.52 for P2Y11).

  • Omeprazole

    Cayman Chemical

    A selective and irreversible inhibitor of the gastric H+/K+ ATPase pump (IC50 = 1.1 μM).

  • GSK-3ß Inhibitor II

    Cayman Chemical

    GSK3β Inhibitor II is a potent inhibitor of glycogen synthase kinase-3β (GSK3β; IC50 = 390 nM) that does not inhibit GSK-3α. Also referred to as tip-oxadiazole, this compound blocks the functional regulation of p53 by GSK3β, decreasing levels of MDM2, p21, and…

  • A potent, selective antagonist of the serotonin (5-HT) receptor 5-HT3 (pKi = 10.4 in rat cortex); orally bioavailable and potently inhibits emesis induced by chemotherapeutic drugs; remarkable for its long duration of action, related to its high receptor-binding affinity and long half-life.

  • Anisomycin

    LKT Labs

    Anisomycin is an antibiotic initially produced by Streptomyces that retains no antibacterial activity. Anisomycin exhibits neuromodulatory and anticancer chemotherapeutic activities. Anisomycin inhibits peptidyl transferase in the 80S ribosome, suppressing protein synthesis. In animal models,…

  • Thidiazuron

    Cayman Chemical

    A synthetic cytokinin used as a media supplement to regulate growth in woody plant tissue cultures and micropropagations; concentrations below 1 µM promote axillary proliferation, whereas concentrations above 1 µM can stimulate the formation of callus, adventitious shoots, or somatic embryos.

  • Hydroperoxy HPLC Mixture

    Cayman Chemical

    The hydroperoxy HPLC mixture contains several of the principle LO-derived hydroperoxides of arachidonic acid and linoleic acid supplied in ethanol. This HPLC mixture contains 5 µg of the following fatty acid hydroperoxides: 5(S)-HpETE, 12(S)-HpETE, 15(S)-HpETE, 9(S)-HpODE, and 13(S)- HpODE.

  • Retinoic Acid

    Cayman Chemical

    A metabolite of vitamin A that acts as a ligand for both the RAR and the RXR.

  • Cantharidin

    Cayman Chemical

    Inhibits PP1 (IC50 = 1.7 μM) and PP2A (IC50 = 0.2 μM) while only weakly inhibiting the activity of PP2B (IC50 = 1 mM); stimulates cell cycle progression and induces premature mitosis and has been shown to be active in various cancer cell lines.

  • LY83583

    Cayman Chemical

    LY83583 is an inhibitor of soluble guanylate cyclase and of cGMP production. It inhibits soluble guanylate cyclase in human platelets with an IC50 value of 2 µM. LY83583 also inhibits leukotriene synthesis in guinea pig lung and rat peritoneal cells with an IC50 value of…

  • D-myo-Inositol

    MP Biomedicals

    D-myo-Inositol is a growth factor for animals as well as microorganisms. Myo-Inositol is the most abundant form of polyols that serves as a structural element of secondary messengers in eukaryotic cells. Inositol or cyclohexane-1,2,3,4,5,6-hexol is a chemical compound, a sixfold alcohol (polyol) of…

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