Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • Amylose

    Cayman Chemical

    A polysaccharide made of α-D-glucose units that constitutes about 20% of starch; acts as an indicator, turning blue in the presence of iodine, and has also been coupled to magnetic beads for the isolation and purification of maltose-binding protein fusion proteins.

  • SAG

    Cayman Chemical

    A SMO agonist (EC50 = 3 nM) which inhibits hedgehog signaling at high concentrations (>1 μM); directly binds to SMO and can block SMO inhibition by cyclopamine; at 15-240 nM, prevents the neurotoxic effects of glucocorticoids; at 0.4 mM, improves the conversion of iPSC to the neural lineage.

  • SC-51322

    Cayman Chemical

    A selective EP1 antagonist that inhibits PGE2 signaling in a guinea pig ileum muscle strip assay (pA2 = 8.1); demonstrates analgesic activity in a mouse writhing assay (ED50 = 0.9 mg/kg); potentiates the vasorelaxation of human pulmonary vein induced by PGE2 (EC50 = 7.75 µM).

  • Cycloheximide

    Cayman Chemical

    An inhibitor of protein synthesis in eukaryotes (IC50 = 5-50 μM) that functions by interfering with translational elongation; can either induce or inhibit apoptosis depending on cell type.

  • 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…

  • Aztreonam

    LKT Labs

    Aztreonam is a synthetic ß-lactam antibiotic that displays antibacterial activity against gram negative bacteria. Like similar compounds, aztreonam inhibits penicillin binding proteins.

  • 6-Gingerol

    Cayman Chemical

    A natural chemical found in fresh ginger that activates TRPV1 (EC50 = 3.3 µM) as well as the TRP ankyrin receptor TRPA1 (EC50 = 10.4 µM).

  • DPPH

    Cayman Chemical

    A cell-permeable, stable free radical that is commonly used to evaluate the ability of compounds to act as free radical scavengers or hydrogen donors and to measure the antioxidant activity of tissue extracts; followed by color change from purple (absorbance at 515-528 nm) to yellow.

  • Galeterone

    Cayman Chemical

    A CYP17 inhibitor (IC50 = 300 nM) that competitively blocks synthetic androgen binding (EC50 = 845 nM) and antagonizes the androgen receptor in transcriptional activation assays; inhibits the growth of castration-resistant prostate cancer cells (IC50 = 2.9 µM).

  • Gö 6976

    Cayman Chemical

    A PKCα and PKCβ1 inhibitor with IC50 values of 2.3 and 6.2 nM, respectively; also inhibits the checkpoint kinases Chk1/2 and abrogates DNA damage-induced cell cycle arrest, leading to cytotoxicity in p53 mutant tumor cells.

  • Antimycin A

    LKT Labs

    Antimycin A was initially produced by Streptomyces. Antimycin A binds cytochrome c reductase, inhibiting electron transport chain activity, oxidative phosphorylation, and ATP synthesis. Antimycin A is used in research models to study mitochondrial respiration and superoxide production. Grade: ≥98%

  • JC-1

    Cayman Chemical

    A membrane-permeable cationic dye that is used to study mitochondrial integrity in the context of cellular apoptosis; changes fluorescence characteristics with alteration in mitochondrial transmembrane potential, a very early event in apoptosis.

  • Abiraterone Acetate

    Cayman Chemical

    Blocks CYP17A1 by potently inhibiting both the 17α-hydroxylase and the 17,20 lyase activities (IC50 = 18 and 17 nM, respectively); essentially eliminates plasma testosterone while producing a 3- to 4-fold increase in plasma luteinizing hormone.

  • N-acetyl Dapsone

    Cayman Chemical

    A metabolite of dapsone, an anti-inflammatory and antibacterial compound that is widely used in the treatment of leprosy, malaria, acne, and various immune disorders.

  • Kanamycin A

    Cayman Chemical

    A broad spectrum antibiotic that alters translation by prokaryotic ribosomes, resulting in bacterial cell death; used as a selective agent to isolate transformants that are expressing a kanamycin resistance gene, usually neomycin phosphotransferase (NptII/neo).

  • Aflatoxin M2

    LKT Labs

    Aflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin M2 is the hydroxylated metabolite of aflatoxin B2; it inhibits DNA synthesis and induces cell cycle arrest.

  • Daidzin

    Cayman Chemical

    A naturally-occurring isoflavone with anti-oxidant, anti-carcinogenic, and anti-atherosclerotic activities; directly inhibits mitochondrial aldehyde dehydrogenase 2 (IC50 = 80 nM) and is an effective anti-dipsotropic isoflavone.

  • Alamethicin

    LKT Labs

    Alamethicin is a peptabiol peptide initially produced by species of Trichoderma. Alamethicin is an antimicrobial peptide (AMP) that disturbs the lipid layer of the cell membrane, aggregating and forming pores and causing cell lysis. Grade: ≥95%

  • DAPI (hydrochloride)

    Cayman Chemical

    A fluorescent probe which is commonly used to stain DNA and chromosomes for fluorescent microscopy and flow cytometry applications; characterized by ultraviolet (max 358 nm) excitation and blue (max 461 nm) emission wavelengths.

  • 17-chlorophenyl trinor Prostaglandin F2a ethyl amide

    Cayman Chemical

    Has a chlorine atom substituted into the meta position of the phenyl group of 17-phenyl PGF2α ethyl amide; the meta substitution of a halogen (fluorine) at this site on the free acid increases its affinity for the FP receptor and greatly decreases its affinity for the EP1 receptor.

  • Butylated Hydroxytoluene

    LKT Labs

    Butylated hydroxytoluene (BHT) is commonly used as a food and cosmetics additive; it exhibits antioxidative and anti-inflammatory activities. BHT may also display neuroprotective benefit, decreasing ethanol-induced brain damage and neurodegeneration and suppressing activation of NF-?B activation…

  • Bilirubin from Porcine Gall Bladder

    MP Biomedicals

    Bilirubin is the principal pigment of bile and constituent of many biliary calculi and also found in blood. As the major end-product of the biological breakdown of heme, bilirubin is the chromophore responsible for coloration in various forms of jaundice. Bilirubin is suitable for use in the…

  • Stearic Acid

    Cayman Chemical

    A long-chain saturated fatty acid that does not affect plasma total cholesterol or LDL-cholesterol but may reduce HDL-cholesterol.

  • Luminol

    Cayman Chemical

    A cyclic diacyl hydrazide that exhibits chemiluminescence upon oxidation; HRP combined with H2O2 causes luminescent peroxidation of luminol; can also be oxidized, and chemiluminesce, by compounds containing iron, copper, gold, and cyanide.

  • ITSA1

    Cayman Chemical

    A cell-permeable suppressor of TSA action, reducing TSA-induced acetylation of histone and tubulin in A549 cells when given at 50 µM; prevents TSA-mediated cell cycle arrest and apoptosis; blocks the action of the HDAC inhibitor SAHA, preventing SAHA-induced hyperacetylation of tubulin in…

  • GSK126

    Cayman Chemical

    A selective, SAM-competitive small molecule inhibitor of EZH2 methyltransferase activity (Ki = 0.57 nM; IC50 = 9.9 nM versus that of EZH1: Ki = 89 nM; IC50 = 680 nM); inhibits global H3K27me3 levels, inhibiting the proliferation of EZH2 mutant DLBCL cell lines (IC50

  • RITA

    Cayman Chemical

    An inhibitor of p53-HDM-2 interaction that can reactivate the tumor suppressor function of wild-type p53; binds to p53 with an apparent Kd value of 1.5 nM and prevents interaction with HDM-2 resulting in p53 stabilization, accumulation, and activation.

  • Ciclesonide

    Cayman Chemical

    A corticosteroid prodrug that is converted to its active form, des-CIC, a glucocorticoid receptor agonist (Ki = 0.31 nM); used to ameliorate symptoms of airway inflammatory diseases.

  • 3-Pyrimidin-2-yl-2-pyrimidin-2-ylmethyl-Propionic Acid

    Cayman Chemical

    3-Pyrimidin-2-yl-2-pyrimidin-2-ylmethyl-propionic acid is a synthetic intermediate useful for pharmaceutical synthesis.

  • Chlorogenic Acid (from Eucommia)

    LKT Labs

    Chlorogenic acid is a polyphenol derivative of caffeic acid found in Eucommia bark that exhibits a wide variety of beneficial properties, including antibacterial, antioxidative, anti-inflammatory, hepatoprotective, neuroprotective, anti-allergic, anticancer chemotherapeutic, and chemopreventive…

  • CAY10649

    Cayman Chemical

    A thiazolinone compound that directly inhibits 5-LO product formation in intact polymorphonuclear leukocytes and a soluble fraction of a S100 PMNL cell lysate (IC50s = 0.28 and 0.09 μM, respectively).

  • Romidepsin

    Cayman Chemical

    A natural bicyclic depsipeptide that, following reduction, selectively inhibits class I HDACs (IC50s = 53, 39, 53, and 26 nM, for HDACs 1, 2, 3, and 8, respectively); has anti-cancer activities, particularly against certain T cell lymphomas.

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