Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • 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…

  • 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…

  • D-myo-Inositol-2,3,5,6-tetraphosphate (sodium salt)

    Cayman Chemical

    Produced from Ins(1,2,3,5,6)P5 via a minor enzymatic phytate degradation pathway by K. terrigena; moderately effective in opening calcium channels relative to Ins(1,4,5)P3.

  • Genipin

    Cayman Chemical

    A protein cross-linking agent isolated from G. jasminoides Ellis; inhibits UCP2 activity; 5 µM genipin increases glucose-stimulated insulin secretion in isolated pancreatic islets chronically exposed to high levels of glucose; induces apoptosis in FaO rat hepatoma cells and human…

  • Philanthotoxin 74 (hydrochloride)

    Cayman Chemical

    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.

  • Trametinib

    Cayman Chemical

    A potent inhibitor of both MEK 1 and 2 that works in an ATP-noncompetitive fashion (IC50s = 0.7 and 0.9 nM, respectively); blocks dual phosphorylation of ERK1/2 and stops cell cycling in cancer cell lines, both in vitro and in multiple tumor models in mice.

  • Forskolin

    Cayman Chemical

    A naturally occurring diterpene that directly activates adenylyl cyclase to raise levels of cAMP in a wide variety of cell types; binds to type 1 adenylyl cyclase membranes with an IC50 value of 41 nM and demonstrates an EC50 value of 0.5 μM in an activation assay.

  • 10-Nitrolinoleate

    Cayman Chemical

    The product of nitration of linoleate by NO-derived reactive species; activates PPARγ (Ki = 133 nM), inducing CD36 expression in macrophages, adipocyte differentiation, and glucose uptake; can also be metabolized to produce nitrite derivatives which in turn form NO, leading to increased cGMP production.

  • Y-27632 (hydrochloride)

    Cayman Chemical

    A potent, ATP-competitive inhibitor of ROCKs including p160ROCK (Ki = 140 nM) and ROCK-II (IC50 = 800 nM); also inhibits PRK2 with an IC50 value of 600 nM.

  • L-Ascorbic Acid

    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.

  • URMC-099

    Cayman Chemical

    An orally bioavailable, brain-penetrant inhibitor of MLKs (IC50s = 19, 42, 14, and 150 nM for MLK1, MLK2, MLK3, and the related MLK family member DLK, respectively); also inhibits LRRK2 activity (IC50 = 11 nM); demonstrates anti-inflammatory and neuroprotective effects both in…

  • Ciprofloxacin

    LKT Labs

    Ciprofloxacin is a second generation fluoroquinolone antibiotic that exhibits antibacterial activity against both gram negative and gram positive bacteria. Ciprofloxacin inhibits DNA gyrase and topoisomerase IV, preventing DNA replication.

  • Aflatoxin M1

    Cayman Chemical

    A natural oxidative metabolic of the mycotoxin aflatoxin B1; produced from aflatoxin B1 in mammals and then secreted in milk.

  • 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.

  • 25-hydroxy Vitamin D2

    Cayman Chemical

    An intermediate produced from vitamin D2 by cytochrome P450 isoforms in vertebrates; subsequently metabolized to 1,25-dihydroxy vitamin D2, which is an agonist for the vitamin D receptor.

  • 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.…

  • Glycitein

    Cayman Chemical

    An O-methylated isoflavone with weak estrogenic activity (IC50 = 3.94 μM) that has been used in research related phytoestrogen therapeutic activity applied to bone formation, cardiovascular disease, estrogen-dependent cancer, and Alzheimer’s disease.

  • CYPMPO

    Cayman Chemical

    CYPMPO is a free radical spin trap with excellent trapping capabilities toward hydroxyl and superoxide radicals in biological and chemical systems. Decay of the superoxide adduct of CYPMPO proceeds in an apparent first order fashion with half-lives of 15 and 51 minutes in a UV-illuminated hydrogen…

  • Palmitic Acid Alkyne

    Cayman Chemical

    A form of palmitic acid with an ω-terminal alkyne for use in click chemistry to isolate palmitoylated proteins.

  • GSK837149A

    Cayman Chemical

    A selective, reversible inhibitor of FAS (pIC50 = 7.8).

  • Bupivacaine

    LKT Labs

    Bupivacaine is an amino amide anesthetic that decreases current amplitude and inhibits whole cell K+ currents in Ca2+-activated (BK/SK) K+ channels and N-type voltage-gated (Kv1/shaker and Kv3 KCNA/KCNC) K+ channels. Bupivacaine also inhibits voltage-gated Na+ channels and tandem pore domain…

  • n-Dodecyl-ß-D-maltoside

    Cayman Chemical

    A non-ionic detergent commonly used to solubilize membrane-associated proteins; helps retain the native conformation and activity of membrane-associated proteins, and facilitates the reforming of these proteins after denaturation.

  • RQ-00203078

    Cayman Chemical

    A selective TRPM8 antagonist (IC50s = 8.3 and 5.8 nM in human and rat, respectively); attenuates icilin-induced wet-dog shakes in rats (ED50 = 0.65 mg/kg); reduces HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro.

  • Bafilomycin A1

    Cayman Chemical

    A selective, reversible inhibitor of vacuolar H+-ATPases (V-ATPases), blocking these proton pumps in mammalian, plant, or fungal cells with an IC50 value in the 4-400 nM range; also inhibits autophagy by preventing vacuolar acidification necessary for autophagosome maturation.

  • Ochratoxin A

    Cayman Chemical

    A mycotoxin produced by A. ochraceus, A. carbonarius, and P. verrucosum that is commonly found as a food contaminant (Tolerable Weekly Intake = 100 ng/kg body weight per day); triggers nephropathy, induces renal adenomas, and initiates skin tumors through events involving oxidative stress,…

  • Vitamin B12

    Cayman Chemical

    A corrinoid vitamin with roles in brain and nervous system functioning and blood formation through regulation of DNA synthesis, cellular metabolism, fatty acid metabolism, and amino acid metabolism; serves as a cofactor in isomerase-, methyltransferase-, and dehalogenase-catalyzed reactions,…

  • Indoxyl Sulfate (potassium salt)

    Cayman Chemical

    A metabolite of tryptophan derived from dietary protein that can accumulate to toxic levels in instances of uremia; 250 µM can induce the activation of NF-κB, promoting the expression of both TGF-β1 and Smad3 expression in proximal tubular cells of rats, which is associated with…

  • Dihydroresveratrol

    Cayman Chemical

    A major metabolite of resveratrol that is produced by the gut microbiota.

  • 13-OxoODE-d3

    Cayman Chemical

    An internal standard for the quantification of 13-OxoODE by GC- or LC-MS.

  • Rosuvastatin

    Cayman Chemical

    An inhibitor of HMG-CoA reductase (IC50 = 5 nM) that has been shown to be more effective than atorvastatin, simvastatin, or pravastatin in decreasing LDL cholesterol and increasing HDL cholesterol.

  • AZD6482

    Cayman Chemical

    A selective PI3K inhibitor that targets the β isoform more potently than PI3Kδ, PI3Kγ, or PI3Kα (IC50s = 0.69, 13.6, 47.8, and 136 nM, respectively); blocks Akt signaling and tumor growth in a large number of cancer cell lines and suppresses the growth of…

  • Estriol

    Cayman Chemical

    Estriol is a metabolite of estradiol and a major estrogen produced in the later stages of pregnancy. In a longitudinal study in healthy pregnant women, total plasma estriol levels increased from 10 weeks gestation to approximately 150 ng/ml at week 38. The majority of the estriol synthesized in the…

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