Biologically Active Small Molecules, Chemicals, 100 mg

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100 mg Chemicals Biologically Active Small Molecules

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  • 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.

  • A fluorescent probe that can react with ONOO-, HOCl, and H2O2 in a similar manner to CBA, yet is formulated for improved solubility.

  • A fluorescent indicator of peroxynitrite formation; neither NO, superoxide, nor hydrogen peroxide alone appear to oxidize DCFH.

  • Cayman Chemical

    A potent inhibitor of PDE5 (IC50 = 1-5 nM) that also blocks the activity of PDE11 (IC50 = 10-33 nM); IC50 values against other isoforms of PDE are in the micromolar range; pharmacokinetics are highlighted by its prolonged duration of effect.

  • Cayman Chemical

    Keystone essential fatty acid that is converted by COX, LO, and epoxygenase enzymes into more than 150 potent metabolites in species ranging from fungi to plants to mammals.

  • Cayman Chemical

    A metabolite of dimetridazole, the nitroimidazole-based antibacterial and anticoccidial agent suspected to be carcinogenic and mutagenic to humans.

  • A fluoroquinolone antibiotic that displays broad spectrum antibacterial activity by inhibiting the bacterial regulatory enzyme DNA gyrase (IC50 = 0.92 µg/ml) as well as topoisomerase IV (IC50 = 1.62 µg/ml).

  • 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

    AMT is a potent, relatively selective inhibitor of iNOS with a Ki of 4.2 nM in mouse macrophages. It inhibits other isoforms of NOS, but at higher concentrations; the IC50 values for rat nNOS and bovine eNOS are 34 and 150 nM, respectively.

  • An intermediate in the interconversion of glucose and galactose.

  • Cayman Chemical

    An imidazoquinoline compound that activates TLR7 (EC50 = 2.1 µM) on immune cells, inducing the production of IFN-α, IL-12, and other mediators; up-regulates the OGF receptor on cancer cells, blocking cell proliferation (IC50 = 2 µM).

  • 3-Tert-butyl-5-methoxy-catechol exhibits anticancer activity, inhibiting proliferation of leukemia cells. This compound may also induce cellular differentiation in vitro.

  • Cayman Chemical

    A potent and selective AhR antagonist (Ki = 1.2 nM).

  • Cayman Chemical

    A plant lectin that selectively cross-links cell-surface glycoproteins and affects the initiation of cell agglutination, mitogenesis, and apoptosis; widely used in affinity chromatography purifications of various glycoproteins and cellular structures; also used to induce liver injury in…

  • 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…

  • A potent inhibitor of iNOS (IC50 = 0.20 μM), with over 1,000-fold selectivity compared to eNOS (IC50 = 350 μM).

  • 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 antagonist of the type III receptor tyrosine kinases PDGFRβ, FLT3, and c-Kit (IC50 = 200, 220, and 170 nM, respectively); less potently inhibits CSF-1R (IC50 = 3.4 µM) and does not significantly inhibit other tyrosine or serine/threonine kinases.

  • Cayman Chemical

    A selective serotonin reuptake inhibitor (Ki = 6.2 nM in rat hypothalamus) with comparatively little effect on noradrenaline reuptake (Ki = 1,100 nM); potentiates the pharmacological effects of serotonin and its precursor, 5-hydroxy tryptophan, in the CNS resulting in antidepressant effects.

  • Cayman Chemical

    A fluorescent probe commonly used to identify dead cells; excitation at 488-535 nm and emission maximum of 617 nm.

  • 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.

  • Cayman Chemical

    A potent pan inhibitor of class I catalytic subunits of PI3K, inhibiting p110α, β, δ, and γ with IC50 values of 3, 33, 3, and 75 nM, respectively; inhibits the growth of certain types of cancer cells, and blocks signaling through PI3K to Akt, both in cells and in vivo.

  • POL is a common triglyceride component in seed and vegetable oils including olive, sesame, soybean, canola, corn, hazelnut, and many others. POL is one of the standard triglyceride components used for the USP analysis of sesame oil for pharmaceutical applications.

  • Cayman Chemical

    A natural triterpene which stimulates wound healing; induces cell cycle arrest and apoptosis in breast cancer cells (IC50 = 5.9 µM for MCF-7 cells); blocks angiogenesis in glioblastomas; down regulates BACE1 while increasing ADAM10 maturation in primary rat cortical neurons; protects against…

  • An ERβ Selective agonist; exhibits 70-fold higher relative binding affinity for ERβ versus ERα.

  • Cayman Chemical

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

  • 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 potent disruptor of microtubules used as a chemotherapeutic compound; inhibits growth of cervical (HeLa), lung (A549), breast (MCF-7), colon (HT-29), ovarian (OVG-1), and pancreatic (PC-Sh) carcinomas with IC50 values ranging from 2.5-7.5 nM; induces mitotic arrest and initiates apoptosis of…

  • Cayman Chemical

    An antipsychotic compound that displays high affinity for dopamine receptors (Kis = 2.4, 0.2, and 1.8 nM for D2, D3, and D4, respectively); also has actions as an antagonist, inverse agonist, or channel blocker, with lower affinities, at other receptors and channels.

  • Cayman Chemical

    An inhibitor of DPP-4 (IC50 = 3.5-34 nM); also inhibits DPP-8 and DPP-9 (Ki = 810 and 95 nM, respectively) but not DPP-2 or FAPα; blocks the degradation of several circulating peptides, including incretins; reduces fasting and postprandial glucose levels and decreases inflammatory…

  • Cayman Chemical

    A suicide inhibitor of LTB4 20-hydroxylase and renal CYP450 ω-hydroxylase.

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