Biologically Active Small Molecules, 500 mg

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500 mg Biologically Active Small Molecules

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  • Cayman Chemical

    A prodrug that is rapidly catabolized in vivo to 5-fluorouracil when administered by rapid injection; inhibits thymidylate synthase (EC50 = 0.6 nM), interfering with DNA synthesis; used to treat various cancers, particularly metastases to the liver.

  • Cayman Chemical

    A selective estrogen receptor (ER) modulator; an ER antagonist in breast tissue, effective in treating early breast cancer; an ER agonist in bone and blood vessels and a partial ER agonist in uterine tissues.

  • Cayman Chemical

    An orally active broad spectrum antifungal agent that blocks ergosterol biosynthesis by inhibiting the fungal CYP isoform CYP51; potently inhibits the mammalian analog CYP51A1 (IC50 = 63.5 nM), as well as a variety of other CYP isoforms.

  • Cayman Chemical

    An aminonucleoside antibiotic that blocks protein synthesis in both prokaryotes and eukaryotes by causing premature termination of nascent polypeptide chains; used in assays for peptide-bond formation and elongation and also often used as selective agent in cell culture systems.

  • A low molecular weight nonionic detergent that is commonly used for cell lysis and non-denaturing protein solubilization.

  • Cayman Chemical

    A selective and irreversible inhibitor of the gastric H+/K+ ATPase pump (IC50 = 1.1 μM).

  • Cayman Chemical

    A nonfixable red fluorescent dye (excitation max: 586 nm; emission max: 605 nm) that can be used as a specific marker for astrocytes and an activity-dependent probe for monitoring regulated exocytosis.

  • An intermediate in the interconversion of glucose and galactose.

  • Cayman Chemical

    A broad-spectrum nitrofuran antibiotic used against urinary tract infections and as therapy for acute diarrhea of bacterial origin; inhibits the survival and migration of cancer cells, suppressing tumor growth and metastasis in vivo, at least in part by inhibiting STAT3 (IC50 = 10 µM).

  • Cayman Chemical

    An agonist of GPR81 (EC50 = 16 µM) that is inactive against the related GPR109a (HCAR2) receptor; stimulates lipolysis (increased serum free fatty acids) in mice fed high fat chow for 10 weeks; blocks basal ghrelin secretion by primary gastric mucosal cells.

  • Cayman Chemical

    A steroid hormone produced in the cortex of the adrenal glands that binds to both glucocorticoid and mineralocorticoid receptors; also is the precursor to aldosterone synthesis.

  • Cayman Chemical

    CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.

  • Cayman Chemical

    Chlorogenic acid is a phenolic natural product isolated from the leaves and fruits of dicotyledonous plants, including the coffee bean. Structurally, chlorogenic acid is the ester of caffeic acid with the 3-hydroxyl group of quinic acid. Chlorogenic acid is an important factor in plant metabolism.…

  • DGLA is a metabolite produced by chain elongation of the essential fatty acid γ-linolenic acid. Ethyl DGLA is an esterified version of the free acid which is less water soluble, but more ammenable for the formulation of DGLA-containing diets and dietary supplements. DGLA has been advanced as…

  • Cayman Chemical

    A class III antiarrhythmic agent; inhibits KCNH2 with an IC50 value of 1 µM; also inhibits CYP2C8 and CYP3A4 in vitro at low micromolar concentrations.

  • Cayman Chemical

    The major estrogen secreted by the premenopausal ovary.

  • Cayman Chemical

    An elongation product of γ-linolenic acid (18:3), rapidly metabolized by fatty acid desaturases to produce arachidonic acid (20:4); metabolized through the cyclooxygenase pathway to produce 1-series prostaglandins; can reduce atopic dermatitis and atherosclerosis when added to the diet of mice.

  • Cayman Chemical

    Can be formed by the dimerization of two molecules of α-trans-cinnamic acid; significantly blocks inflammatory pain while having little effect on neurogenic pain, as indicated by the formalin test in mice.

  • Cayman Chemical

    A potent dopamine receptor agonist that binds the D2 receptor with highest affinity (Ki = 2.5 nM); avidly binds the serotonin receptors 5-HT1A and 5-HT1D (Ki = 12.9 and 10.7 nM, respectively), as well as α and β adrenoreceptors.

  • Cayman Chemical

    A cell-permeable, chromogenic substrate for β-galactosidase used in histochemical and molecular biology applications, including detection of lacZ activity in cells and tissues.

  • Cayman Chemical

    A mixture of at least four closely related components, polymyxin B1 to B4, with polymyxin B1 and B2 being the two major components; demonstrates rapid in vitro bactericidal activity against major multidrug-resistant Gram-negative bacteria, including P. aeruginosa, A. baumannii, and K. pneumonia.

  • A synthetic intermediate useful for pharmaceutical synthesis.

  • Cayman Chemical

    A cell permeable derivative of GSH that undergoes hydrolysis by intracellular esterases to release GSH; used to protect cells against damage from radiation, oxidants, and various toxic compounds including heavy metals.

  • Cayman Chemical

    A potent and selective PPARγ ligand, binding to the PPARγ ligand-binding domain with a Kd value of 43 nM.

  • Cayman Chemical

    A broad-spectrum β-lactam antibiotic used for parenteral administration.

  • A phospholipid containing the long-chain (14:0) myristic acid inserted at the sn-1 and sn-2 positions.

  • 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.

  • Cayman Chemical

    An 18-carbon saturated fatty acid that is structurally similar to the phospholipid-derived N-acyl ethanolamines; inhibits heat-induced firing of nociceptive neurons in rat dorsal horn; induces transient calcium influx in native dorsal root ganglion (DRG) cells and in the PTX-sensitive, DRG-like…

  • Cayman Chemical

    A dual purpose probe; a chemiluminescent probe that detects superoxide production by enzymatic and cellular sources; a fluorescent chloride-sensitive indicator, with fluorescence being quenched by chloride (excitation: 455 nm; emission: 505 nm).

  • 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…

  • Cayman Chemical

    A potent PR and GR antagonist with Ki value of approximately 1 nM.

  • Cayman Chemical

    A potent anti-mitotic drug that is 100-fold more active than resveratrol at inhibiting the growth of human colon cancer Caco-2 cells; inhibits tubulin polymerization in a dose-dependent manner (IC50 = 4 μM) and enzymes involved in the synthesis of the polyamines, putrescine, and spermidine.

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