Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • GW 9508

    Cayman Chemical

    A small-molecule agonist of GPR40 (EC50 = 47 nM) and GPR120 (EC50 = 2.2 µM), GPCRs that are activated by medium and long-chain fatty acids; potentiates glucose-stimulated insulin secretion and the KCl-mediated increase in insulin secretion in MIN6 cells.

  • Castanospermine

    LKT Labs

    Castanospermine acts as an inhibitor of N-glycosylation, inhibiting O-GlcNAcase, resulting in immunosuppressive, anti-inflammatory, and antiviral activities. In leukocytes and endothelial cells, castanospermine decreases expression of cellular adhesion molecules ICAM-1, ICAM-2, L-selectin, LFA-1a,…

  • 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.

  • Anabaenopeptin 872

    LKT Labs

    Anabaenopeptins are cyclopentapeptides found in cyanobacteria such as Microcystis aeruginosa and Oscillatoria agardhii. Anabaenopeptins and other cyanotoxins are typically inhibitors of serine proteases and protein phosphatases (PPs). Anabaenopeptins may also inhibit carboxypeptidases.…

  • Cholesterol

    MP Biomedicals

    Cholesterol is the principal sterol of the higher animals, found in all body tissues. It is the main constituent of gallstones and all biological membranes. Approximately 25% of total brain lipid is cholesterol. Cholesterol, followed by the chemical suffix -ol for an alcohol, is an organic chemical…

  • Tigecycline

    Cayman Chemical

    A glycylcycline antibiotic with a broad spectrum of activity against many Gram-positive, Gram-negative, and anaerobic organisms, including many multidrug-resistant strains.

  • CAY10640

    Cayman Chemical

    Inhibits recombinant human and mouse sEH (IC50s both = 0.4 nM) and demonstrates a 1,000-fold increase in potency compared to morphine in reducing hyperalgesia in an in vivo carrageenan-induced inflammatory pain model.

  • SAHA-BPyne

    Cayman Chemical

    A SAHA derivative with a benzophenone crosslinker and an alkyne tag to be used for profiling HDAC activities in proteomes and live cells; labels HDAC complex proteins both in proteomes at 100 nM and in live cells at 500 nM; IC50 = ~3 μM for inhibition of HDAC activity in HeLa cell nuclear…

  • Cilostazol

    LKT Labs

    Cilostazol is a quinolone inhibitor of phosphodiesterase 3B (PDE 3B) that exhibits vasodilatory, antiplatelet, anti-inflammatory, anti-diabetic, antidepressant, anxiolytic, and pro-angiogenic activities. Cilostazol is clinically used to treat intermittent claudication associated with peripheral…

  • AICAR

    Cayman Chemical

    A selective activator of AMPK; inhibits synthesis of fatty acids and sterols in hepatocytes and insulin-stimulated glucose uptake in adipocytes.

  • Caffeine, Anhydrous

    MP Biomedicals

    Caffeine is a well-known drug commonly used as a mild stimulant, found in dietary sources such as coffee, tea, and cocoa. A central nervous system stimulant believed to act through adenosine receptors and monoamine neurotransmitters. It is an adenosine receptor antagonist and adenosine…

  • 17-phenyl trinor Prostaglandin F2a cyclohexyl amide

    Cayman Chemical

    A form of 17-phenyl trinor PGF modified with a cyclohexane moiety at the alpha carbon; insoluble in aqueous media, soluble in organic solvents; activity at the FP receptor has not been evaluated.

  • Cisplatin

    LKT Labs

    Cisplatin is a platinum-based cross-linking agent that exhibits anticancer chemotherapeutic activity. Cisplatin induces crosslinks between guanine bases on DNA; it is clinically used to treat various forms of cancer. In lung cancer cells, cisplatin decreases phosphorylation of PI3K, Akt, and FOXO3a…

  • Tetrodotoxin Citrate

    Cayman Chemical

    A potent marine-derived neurotoxin that reversibly inhibits the inward sodium current through NaV channels (IC50s = 4.1 and 5.2 nM, respectively, in frog muscle and squid axon; Kd = 1.8 nM in rat brain), blocking nerve and muscle action potentials.

  • Monastrol

    Cayman Chemical

    A reversible, cell-permeable inhibitor of the motor protein Eg5, blocking basal ATPase activity in vitro (IC50 = 6.1 µM) and inducing the formation of monoastral spindles in cell-based assays (IC50 = 51.3 μM).

  • Pinolenic Acid

    Cayman Chemical

    Pinolenic acid is a PUFA found in Korean pine (Pinus orientalis) and maritime pine (Pinus pinaster) seed oils. Both oils have been found to have lipid-lowering properties. A diet containing maritime pine seed oil (MPSO) lowered HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO…

  • Cytochalasin E

    Cayman Chemical

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

  • Dehydrocostus lactone

    Cayman Chemical

    A natural sesquiterpene with anti-cancer and anti-inflammatory actions.

  • Acridine Orange

    Cayman Chemical

    A cell-permeable, fluorescent dye that accumulates in acidic organelles in a pH-dependent manner and is used for autophagy detection and cell cycle determination; emits green fluorescence (ex. max: 502 nm; ,em. max: 525 nm) at neutral pH or when bound to dsDNA and red fluorescence (ex. max: 460 nm;…

  • Fluoxetine (hydrochloride)

    Cayman Chemical

    An SSRI, displaying a marked preference for the serotonin tranporter (Kd = 0.81 nM) over the norepinephrine transporter (Kd = 240 nM) and the dopamine transporter (Kd = 3,600 nM).

  • Cisplatin

    Cayman Chemical

    A platinum-containing compound that acts as an alkylating agent; used alone or in combination therapy in the treatment of several types of cancer; inhibits the RecA recombinase of M. tuberculosis (IC50 = 2 µM), blocking protein splicing and cell growth.

  • Astaxanthin

    Cayman Chemical

    Astaxanthin is a carotenoid pigment found primarily in marine animals including shrimp and salmon; it is a potent lipid-soluble antioxidant.

  • (±)-Jasmonic Acid methyl ester

    Cayman Chemical

    A mixture of trans (3R/7R and 3S/7S) isomers; induces the synthesis of proteinase inhibitors in plant leaves; in cancer cells, suppresses proliferation and induces apoptosis; inhibits hexokinase that is bound to mitochondria; methyl jasmonate derivatives also have potential as anti-inflammatory agents.

  • 16,16-dimethyl Prostaglandin F2ß

    Cayman Chemical

    16,16-dimethyl PGF2β is a metabolically stable analog of PGF2β. It prevents bronchospasm in asthmatics but is less potent than PGE2.

  • Microcystin-LR

    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…

  • Natamycin

    Cayman Chemical

    A naturally occurring macrolide polyene used to treat fungal infections, including Candida, Aspergillus, Cephalosporium, Fusarium and Penicillium (minimal inhibitory concentrations ~ 4-64 μM); also used in the food industry as a "natural" preservative.

  • Hypophyllanthin

    Cayman Chemical

    An active principle of P. amarus that has been shown to reversibly inhibit P-glycoprotein (also known as multidrug resistance protein 1 (MDR1)) function without effect on MDR2 activity.

  • Odd-Chain Fatty Acid LC-MS Mixture

    Cayman Chemical

    Features Each vial contains a mixture of standards packaged in amber ampules purged with argon >1 ml provided at the concentration specified in the insert Designed for direct snap and inject use in mass spectrometry applications Ideally suited for method development and as a…

  • Cefapirin

    Cayman Chemical

    A first generation cephalosporin antibiotic that is broadly effective against gram-negative and gram-positive bacteria; mainly used in veterinary medicine for intramammary treatment of mastitis and intrauterine treatment of endometritis in cattle.

  • Concanavalin A from Canavalia ensiformis seeds (jack beans)

    MP Biomedicals

    Pure Canavalia ensiformis lectin (Con A) from Jackbean. Isolated by affinity chromatography on cross-linked dextran. Con A exists as a dimer below pH 5.0 and and at pH >7 it exists as a tetramer. Con-A is not a glycoprotein. The monomeric molecular weight of Con-A is 25,500. Con-A does not…

  • Ruxolitinib

    Cayman Chemical

    A potent ATP mimetic that inhibits both JAK1 and JAK2 with IC50 values of 2.7 and 4.5 nM, respectively; blocks IL-6 signaling (IC50 = 281 nM) and proliferation of JAK2V617F+ Ba/F3 cells (IC50 = 127 nM); reduces splenomegaly, decreases circulating levels of IL-6 and TNF-α, eliminates…

  • AZ 20

    Cayman Chemical

    A potent, selective inhibitor of ATR (IC50 = 5 nM); inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro and significantly reduces the growth of LoVo xenografts in mice.

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