Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • A nonenzyme-dependent degradation product of rapamycin resulting from ester hydration followed by dehydration; secreted from cells by P-glycoprotein; poorly activates mTOR but, like rapamycin, inhibits the proteasome.

  • 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.

  • Skepinone-L

    Cayman Chemical

    An ATP-competitive inhibitor of p38 MAPK isoform p38α (IC50s = 5 nM) and p38β (97% inhibition at 1 µM); has little effect on a range of other kinases, including p38γ and p38δ; blocks the phosphorylation of HSP27, a p38 MAPK substrate, in response to…

  • Aminophylline is a non-selective adenosine receptor antagonist and phosphodiesterase (PDE) inhibitor. Aminophylline exhibits vasodilatory and anti-inflammatory activity and is occasionally clinically used to treat chronic obstructive pulmonary disorder (COPD). In animal models of allergen-induced…

  • 13-Docosenamide

    Cayman Chemical

    An amide of docosenoic acid first identified in the CSF of sleep-deprived cats; causes reduced mobility and slightly lessened awareness in rats.

  • ProClin™ 300

    MilliporeSigma

    ProClin biocides are immediately microstatic upon contact with microbial organisms as a result of their ability to quickly penetrate cell membranes and inhibit specific enzymes crucial to cellular respiration. Multiple specific sites of ProClin toxicity prevent microorganisms from developing high…

  • Acetaminophen

    Cayman Chemical

    An analgesic and antipyretic compound; inhibits COX-2 activity by more than 80%, albeit at relatively high doses, while it is less effective against COX-1.

  • 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.

  • N-4AIA is one of several aromatic amides of indomethacin reported to be potent and selective reversible inhibitors of COX-2. N-4AIA inhibits human recombinant and ovine COX-2 with IC50 values of 0.1 and 0.625 µM, respectively. It is about 80 times less potent as an inhibitor of…

  • IPTG (dioxane free)

    Cayman Chemical

    Induces protein expression where the gene is under the control of the lac operator by triggering transcription of the lac operon in cloning procedures.

  • A non-cholestatic regioisomer of E217G that acts as a substrate for MRP2, competing with E217G for MRP2-mediated transport (IC50 = 14.2 µM).

  • Resazurin (sodium salt)

    Cayman Chemical

    A blue non-fluorescent dye that is used as an oxidation-reduction indicator in cell viability assays in a variety of cells; can be reduced to the highly red-fluorescent product resorufin (excitation: 530-540 nm; emission: 585-595 nm) and used as a quantifiable detection agent in enzyme activity or…

  • Streptozotocin

    Cayman Chemical

    A glucosamine-nitrosourea which is commonly used to induce experimental diabetes in animals; specifically targets beta cells, entering via the glucose transporter GLUT2 and causing alkylation of DNA, leading to the destruction of beta cells.

  • 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.

  • 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.

  • Cafestol is a diterpene initially found in brewed, unfiltered coffee that exhibits anti-angiogenic, anticancer, chemopreventive, neuromodulatory, anti-inflammatory, and hyperlipidemic activities. Cafestol inhibits proliferation, migration, and tube formation in vitro, potentially through decreasing…

  • 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.

  • Coomassie Blue R-250

    Cayman Chemical

    A dye that is commonly used in laboratories to stain or quantify proteins; typically gives blue bands on a clear background with a sensitivity of 50-100 ng/band; displays metachromasia by appearing pink-red, rather than blue, when binding certain proteins, such as collagen and histone H1.

  • Torin 1

    Cayman Chemical

    A potent and selective inhibitor of mTOR (IC50 = 2 and 10 nM for mTORC1 and mTORC2, respectively); efficacious at a dose of 20 mg/kg in inhibiting downstream effectors of mTOR in mice.

  • Aflatoxin B1

    Cayman Chemical

    Naturally occuring mycotoxin and food contaminant that induces the transversion of G to T at codon 249 of the p53 tumor suppressor gene and is a likely pathogen that causes hepatocellular carcinoma.

  • N6-(?2-Isopentenyl)adenine

    Cayman Chemical

    A naturally occurring cytokinin that regulates cell division, development, and nutrient processing in plants and serves as a precursor to zeatin synthesis.

  • WYE-354

    Cayman Chemical

    A selective, potent, and cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTORC1 and mTORC2; induces G1 cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cancer cell lines and reduces tumor growth in nude mice with PTEN-null tumors.

  • Chlorthalidone

    Cayman Chemical

    A nonthiazide diuretic that inhibits the sodium/chloride cotransporter in the distal convoluted tubule of the kidney; also effectively inhibits the activity of most platelet carbonic anhydrase isozymes (IC50s = 2.8 nM - 11 µM).

  • D-myo-Inositol-3,4,5-triphosphate (Ins(3,4,5)-P3) is a structural analog of Ins(1,4,5)-P3 and a member of the inositol phosphate (InsP) cell signaling family of molecules. D-myo Ins(3,4,5)-P3 is 200-fold less potent than D-myo Ins(1,4,5)-P3 at initiating Ca++ release when injected into Xenopus…

  • Biotin hydrazide

    Cayman Chemical

    A biotinyl derivative used to label surface functional groups, antibodies, lectins, sugars, nucleic acids, or molecules with free carboxylic or keto groups; probe for determining protein carbonylation.

  • Fludarabine

    Cayman Chemical

    A nuclesoside analog that disrupts DNA synthesis in blood cells; effective in a number of animal tumor systems including LI210 leukemia, CD8F mammary adenocarcinoma, P388 leukemia, and human LX-1 lung tumor xenograft and displays anticancer activity against human hematological malignancies in vivo.

  • Caffeine

    LKT Labs

    Caffeine is a xanthine alkaloid found in coffee, tea, and many other plant sources; it exhibits stimulant, bronchodilatory, anti-asthma, vasoconstrictive, anti-inflammatory, antioxidative, anti-aging, and anti-fibrotic activities. Caffeine activates adenosine receptors and inhibits…

  • TCEP (hydrochloride)

    Cayman Chemical

    An odorless, selective, and water-soluble reducing agent that is commonly used in many laboratory applications; commonly used to rapidly reduce protein and peptide disulfide bonds.

  • A subtype-selective AMPA receptor antagonist that inhibits homomeric GluR1 and GluR3 as well as heteromeric GluR1/2 receptors (80-100% of glutamate-evoked currents inhibited at 100 µM); inhibits the GluR5(Q) receptor with a Ki value of 0.29 µM.

  • A fluoroquinolone antibiotic that is administered either orally or parenterally.

  • 3-methoxythio Benzamide

    Cayman Chemical

    A synthetic intermediate useful for pharmaceutical synthesis.

  • 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.

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