Biologically Active Small Molecules, 100 mg, Cayman Chemical

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Cayman Chemical 100 mg Biologically Active Small Molecules

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  • Cayman Chemical

    An isoflavonoid phytoestrogenic compound found in soybeans, pea pods, and other legumes; acts as a tyrosine kinase inhibitor, has chemopreventive effects on breast, prostate, and other endocrine-dependent tumors.

  • Cayman Chemical

    A specific inhibitor of PI3K activity and a widely used inhibitor of the autophagy; at 5 mM, inhibits protein degradation in rat hepatocytes by 65% and blocks class I, II, and III PI3Ks, including some downstream targets.

  • 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

    A substrate of cathepsin C that accumulates inside lysosomes causing lysosome degradation; 50 μM can inhibit the cathepsin-dependent activation of caspase-8.

  • 8-hydroxy Guanine is produced by oxidative damage of DNA or RNA by reactive oxygen and nitrogen species, including hydroxyl radical and peroxynitrite. It serves as a measure of oxidative stress in biological systems.

  • Cayman Chemical

    A “hybrid” analog which incorporates components of both the AEA-like and dopaminergic neurotransmitter pathways; is nearly inactive as a TRPV1 ligand and fails to elicit hyperalgesic or nocifensive responses in vivo; exhibits an “entourage” effect at concentrations of 0.1-10…

  • 3-HPA is an analog of AM404, which is a selective inhibitor of carrier-mediated transport of AEA. 3-HPA is metabolized by both COX-1 and COX-2 and also selectively and irreversibly inhibits COX-2 with an IC50 value of 2 µM.

  • Cayman Chemical

    An analog of folic acid and aminopterin that is used in the treatment of cancer, autoimmune diseases, ectopic pregnancy, and for the induction of medical abortions; induces adenosine release, inhibits the metabolism of folic acid, and blocks key enzymes in the synthesis of purines and pyrimidines…

  • Cayman Chemical

    A bioactive sterol that can affect cholesterol homeostasis, membrane properties and cell survival; inhibits CYP7A1 with an IC50 = ~ 1 µM; can be used as a standard in the determination of cholesterol derivatives by GC-MS or HPLC.

  • Cayman Chemical

    A broad spectrum antibiotic that is in the β-lactam subclass known as carbapenems; effective against many Gram-negative and Gram-positive bacteria and is more effective against P. aeruginosa than other carbapenems; not effective against MSRA.

  • Cayman Chemical

    An intermediary prodrug of fluorouracil, the pyrimidine analog that inhibits thymidylate synthase selectively in tumor cells, interfering with DNA synthesis; one of two intermediary metabolites formed during metabolic conversion of the chemotherapeutic prodrug, capecitabine, to fluorouracil.

  • A potent, stable, and selective agonist analog of AEA with a Ki value of 2.2 nM at the isolated rat CB1 receptor; 325 times more potent at the CB1 receptor compared with the CB2 receptor; induces hypothermia in mice with the same efficacy as AEA, in spite of its much higher affinity for the CB1…

  • A lysosomal condensation product that selectively eliminates dipeptidyl peptidase I-expressing immune cells, including cytotoxic T cells and natural killer cells.

  • 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 platinum-containing compound that acts as an alkylating agent; used alone or in combination therapy in the treatment of several types of cancer; inhibits the RecA recombinase of M. tuberculosis (IC50 = 2 µM), blocking protein splicing and cell growth.

  • 7-Piperazin-1-yl-thieno[2,3-c] pyridine (hydrochloride) is a synthetic intermediate useful for pharmaceutical synthesis.

  • Cayman Chemical

    A member of the 2-aryl propionic acid group of NSAIDs that reduces inflammation through inhibition of NF-κB and AP-1 activation; decreases survival of prostate tumor cells by inducing p75NTR protein expression; inhibits the enzyme γ-secretase thereby preventing the formation of the…

  • 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

    Activates the aryl hydrocarbon receptor (Ki = 5.4 µM), inducing the expression of both detoxifying enzymes, resulting in pyocyanin degradation, and cytokines that facilitate the clearance of bacteria; accelerates neutrophil apoptosis, resulting in resolution of acute inflammation.

  • Cayman Chemical

    An orally active small molecule drug with antioxidant, anti-inflammatory, and anti-fibrotic effects; reduces inflammatory cytokine production, suppresses TGF-β expression, and lowers markers of oxidative stress; has effectiveness in IPF and other conditions with a significant fibrotic component.

  • Cayman Chemical

    A specific, cell-permeable inhibitor of S6K1 (IC50 = 160 nM); does not inhibit S6K2, MSK, or RSK, or many other unrelated kinases, under conditions in which it inhibits S6K1 activity.

  • Cayman Chemical

    An irreversible, noncompetitive inhibitor of PARP1 that disrupts binding between PARP1 and DNA by interacting with the DNA binding domain; produces rapid apoptosis in the various cancer cell (IC50s = 40-128 μM).

  • 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 quinone derivative that inhibits red blood cell PLA2 with a Ki value of 130 µM.

  • Cayman Chemical

    A reversible inhibitor of the H2S synthesizing enzyme cystathionine-γ-lyase; blocks H2S synthesis in rat liver preparations with an IC50 value of 6.5 µM.

  • An intermediate in the biosynthesis of NAD+ that has been used to enhance NAD biosynthesis and glucose-stimulated insulin secretion in Nampt+/- mice and high-fat diet-induced type 2 diabetes mice.

  • Cayman Chemical

    A β-adrenergic receptor agonist with potent positive inotropic effects in vivo; strongest effects on β1 receptors, with lesser but significant β2 receptor activation and only weak α1 receptor actions; strongly increases cardiac contractility.

  • 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.

  • Cayman Chemical

    A dihydropyridine used as an antihypertensive agent due to its ability to block L-type and T-type calcium channels; also binds to adenosine A1, A2A, and A3 receptors with Ki values of 8.96, 23.0, and 8.3 µM, respectively.

  • Cayman Chemical

    A synthetic intermediate useful for pharmaceutical synthesis.

  • Cayman Chemical

    A selective, endogenous TRPV1 agonist that is a “hybrid” analog, which incorporates components of both the AEA-like and dopamine neurotransmitter pathways; binds to the human recombinant TRPV1 (Ki = 36 nM) with equipotency to that of capsaicin and slightly more potency than that of…

  • Cayman Chemical

    A dipyridinyl compound that demonstrates high in vitro and ex vivo selectivity for COX-2 over COX-1.

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