Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • Cayman Chemical

    A first generation tyrosine kinase inhibitor that is used in the treatment of CML, GIST, and other cancers; selectively targets certain tyrosine kinases, including c-ABL, PDGFR, KIT, and the oncoprotein BCR-ABL.

  • LKT Labs

    L-Citrulline is a by product of NO formation from metabolism of L-arginine that exhibits tocolytic and antioxidative activities. L-Citrulline was originally found in watermelon. In isolated rat uteri, L-citrulline decreases uterine contractile force through stimulation of the NO-cGMP relaxant…

  • 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.

  • A cell permeable analog of cAMP that activates PKA with a Ka value of 0.05 μM; more stable to hydrolysis and has increased membrane permeability compared to unmodified cAMP.

  • 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.…

  • Cayman Chemical

    Produced in fungi, including yeast, and invertebrates from ergosterol in response to ultraviolet radiation; metabolized first to 25-hydroxyvitamin D2 and subsequently to the active 1,25-dihydroxyvitamin D2.

  • Cayman Chemical

    BW 245C is a selective agonist for the DP1 receptor. The Ki of BW 245C for the inhibition of [3H]-PGD2 binding to isolated human platelet membranes is 0.9 nM. It has a reported IC50 of 2.5 nM for the inhibition of ADP-induced human platelet aggregation and an IC50 of 250 nM for the inhibition of…

  • Cayman Chemical

    This solution can be used (without further dilution) as a blocking agent for immunocytochemistry or immunohistochemistry when using a secondary antibody generated in goat.

  • Cayman Chemical

    PGB2 is a non-enzymatic dehydration product resulting from the treatment of PGE2 or PGA2 with strong base. It has weak agonist activity on TP receptors and can increase pulmonary blood pressure in the rabbit at relatively high doses (5 µg/kg).

  • Cayman Chemical

    A selective inhibitor of α/β-hydrolase domain 6 (ABHD6) (IC50 = 70 nM), a serine hydrolase that catalyzes the hydrolysis of 2-AG.

  • A homolog of DHEA, characterized by the addition of an (R)-β-methyl group at the terminal ethanolamine carbon.

  • Cayman Chemical

    A polymer film used to manufacture high-performance membranes for dialysis, reverse osmosis, ion sensing, and separation; used in the production of photographic film and polarized film for liquid crystal displays.

  • Cayman Chemical

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

  • Cayman Chemical

    A tricyclic antidepressant that inhibits the reuptake of serotonin and norepinephrine and acts as an antagonist at histamine, serotonin, adrenergic, and muscarinic receptors with Ki values in the nanomolar range.

  • Cayman Chemical

    Beraprost is an analog of prostacyclin in which the unstable enol-ether has been replaced by a benzofuran ether function. This modification increases the plasma half-life from 30 seconds to several hours, and permits the compound to be taken orally. Doses of 20-100 µg in humans, given 1 to 3…

  • Cayman Chemical

    A potent, selective, and cell-permeable inhibitor of the BRPF1 bromodomain (IC50 = 80 nM); disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3.3.

  • TBS stock solution (10X, pH 7.4) contains filtered concentrated TBS. It is ready to use as supplied.

  • Cayman Chemical

    A naturally occurring electron donor for eight different enzymes, including those related to collagen hydroxylation, carnitine synthesis (which aids in the generation of ATP), norepinephrine synthesis, tyrosine metabolism, and amidating peptides.

  • Cayman Chemical

    A potent and selective inhibitor of reticulocyte 15-LO-1.

  • Cayman Chemical

    A classical inhibitor of complex I of the mitochondrial electron transport chain, inhibiting NADH/DB oxidoreductase and NADH oxidase with IC50 values of 28.8 and 5.1 nM, respectively; used in animal models of Parkinson’s disease.

  • Cayman Chemical

    A synthetic derivative of native coelenterazine that exhibits 16-fold higher luminescence intensity (emission maximum ~466 nm; half-total time of 0.6-1.2 sec) than native coelenterazine.

  • Cayman Chemical

    An inhibitor of HIF-1α protein translation; suppresses phosphorylation of two key regulators of protein synthesis, eukaryotic translation initiation factor 4E binding protein 1 (4EBP1) and p70 S6 kinase; cytotoxic to a variety of cancer cell lines with an IC50 value of 15-25 µM.

  • Cayman Chemical

    A potent inhibitor of PARP1 and PARP2 (IC50 = 5 and 1 nM, respectively) but is less effective against the PARP tankyrase-1 (IC50 = 1.5 µM); can be used in cells and in animals, alone or in combination therapy with alkylating agents, to block BER and increase cancer cell death.

  • Aristolochic acid A is a carcinogenic compound found in Aristolochia and Radix that has commonly been used in traditional Chinese medicine. This compound inhibits phospholipase A2 (PLA2) and decreases GABA-induced release of arachidonic acid and phosphatidylcholine as well as exocytosis in vitro.

  • LKT Labs

    Carmofur is a pyrimidine analog and derivative of fluorouracil; it exhibits anticancer chemotherapeutic and anti-metastatic activities. Carmofur inhibits thymidylate synthase and acid ceramidase, preventing DNA replication. This compound is clinically used to treat curatively resected colon cancer…

  • Cayman Chemical

    A selective inhibitor of JAK1 (IC50 = 629 nM) that displays 30-fold selectivity for JAK1- over JAK2-dependent signaling in human whole blood; blocks IL-6/STAT1 and IL-2/STAT5 signaling in cell models and whole blood assays.

  • Cayman Chemical

    A selective, nonpeptide antagonist of the vasopressin V1a receptor (Ki = 1.1-6.3 nM in human); inhibits arginine vasopressin-induced human platelet aggregation with an IC50 value of 3.7 nM.

  • LKT Labs

    Adenine is a purine nucleotide base that is involved in the synthesis of RNA and DNA. Adenine also plays roles in cellular respiration as a component of ATP, NAD, and FAD. Grade: ≥98%

  • An analog of MAFP, which has been widely studied as an inhibitor of phospholipases, FAAH, and as a CB receptor ligand; pharmacology of the α-linolenyl analog of MAFP has not been completely investigated.

  • Cayman Chemical

    GSH is a tripeptide (γ-glutamylcysteinylglycine) widely distributed in both plants and animals. GSH serves as a nucleophilic co-substrate to glutathione transferases in the detoxification of xenobiotics and is an essential electron donor to glutathione peroxidases in the reduction of…

  • Cayman Chemical

    A cell-permeable dye that is cleaved by intracellular esterases, leaving membrane-impermeant calcein, a fluorescent indicator with absorption and emission maxima of 494 and 517 nm, respectively.

  • Cayman Chemical

    Furegrelate is a potent inhibitor of thromboxane synthase with little effect on other enzymes essential for arachidonate metabolism. The IC50 value is 15 nM for human platelet microsomal thromboxane synthase.

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