Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • A lipophilic, nontoxic, iron-chelating agent that shows high iron chelation efficacy both in vitro in cell culture models and also in vivo in rats and mice.

  • Cayman Chemical

    A selective, irreversible inhibitor of BTK (IC50 = 0.5 nM in vitro in B cell lymphoma cell lines) that targets and covalently binds to BTK at cysteine-481; inhibits osteoclast function and reduces osteoclast-stimulated proliferation of multiple myeloma cells in animal models of…

  • Cayman Chemical

    A nutlin-3 analog; inhibits the growth of HCT116 cells at high concentrations (IC50 = ~8 µM); promotes the growth of HCT116 cells ~40% at concentrations between 5-100 nM.

  • Cayman Chemical

    A 5-series LO derived from EPA; contracts pulmonary parenchymal strips from guinea pig with similar potency to that of LXA4 and LXB4, yet does not exert the vasodilatory effects on aortic smooth muscle exhibited by LXA4 and LXB4.

  • Cayman Chemical

    A natural fungal metabolite which reversibly interferes with protein trafficking and secretion mediated by the Golgi apparatus and endoplasmic reticulum; directly and reversibly inhibits Sec7 domain-containing GEFs which are necessary for Arf activation associated with vesicular transport (IC50 =…

  • A potent inhibitor of several NHE isoforms, inhibiting NHE1, NHE2, NHE3, and NHE5 with Ki values of 0.02, 0.5, 2.4, and 0.42 μM, respectively; less effectively inhibits NHE4 (IC50 ≥10 μM).

  • 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.

  • Cayman Chemical

    A natural nitroaryl-substituted polyketide that exhibits antitumor, antifungal, and insecticidal activities; non-competitive inhibitor NADH:ubiquinone oxidoreductase of bovine heart, N. crassa, and E. coli (IC50s = 0.07, 0.08, and 22 nmol/mg protein, respectively).

  • Cayman Chemical

    A non-protein amino acid that chelates iron and copper; inhibits certain enzymes that contain iron or copper, including arginase (IC50 = 3.7 µM).

  • Cayman Chemical

    An inactive control for the selective PAD4 inhibitors, GSK484 and GSK199 (IC50s >100 µM).

  • Cayman Chemical

    An inhibitor of SRE activation in PC3 cells (IC50 = 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM; inhibits PC3 cell migration (IC50 = 4.2 μM), as determined by a scratch wound assay; causes no cytotoxicity when evaluated by WST-1 assay.

  • Cayman Chemical

    A monobactam antibiotic that is effective against Gram-negative bacteria but inactive against Gram-positive bacteria.

  • 4-Aminophenyl phosphate is an alkaline phosphatase substrate used to quantify enzyme activity in research models.

  • Cayman Chemical

    An unsaturated fatty acid found in royal jelly produced from honeybees; demonstrates longevity-promoting effects in C. elegans, down regulates matrix metalloproteinases (MMPs) in rheumatoid arthritis, inhibits VEGF-induced angiogenesis in HUVECs, facilitates differentiation of neurons from neural…

  • 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

    11-deoxy PGE2 is a stable, synthetic analog of PGE2. In contrast to PGE2 which has bronchodilation effects, 11-deoxy PGE2 is a powerful bronchoconstrictor and is 5 to 30 times more potent than PGF2α in the contraction of human respiratory tract smooth muscle in vitro.

  • Cayman Chemical

    A steroidal saponin that displays cytotoxicity against a range of cancer cells in vitro, including leukemia, colon cancer, and prostate cancer cells (GI50 ≤ 2 µM).

  • Cayman Chemical

    An essential fatty acid and the most abundant ω-3 fatty acid in neural tissues, especially in the retina and brain; constitutes as much as 40% of the total PUFA pool in retinal and neuronal membranes; dietary supplementation via fish oil inhibits the progression of atherosclerosis and delays…

  • Cayman Chemical

    A selective inhibitor of 15-hydroxy PGDH (IC50 = ~10 µM).

  • A muscarinic M1 and M2 mACh receptor agonist (pKB = 5 and 3.7, respectively) that is typically used as an animal model for temporal lobe epilepsy.

  • A grasshopper neuropeptide from a family of arthropod hormones and neuroregulators, found in Locusta migratoria.

  • Cayman Chemical

    Hexanolamino PAF C-16 is a PAF analog with mixed PAF receptor agonist/antagonist properties. In human monocyte-derived macrophages, it is an antagonist which inhibits the production of reactive oxygen species in response to PAF C-16. On the other hand, in rabbit platelets and guinea pig…

  • Cayman Chemical

    8(S)-HETrE is a monohydroxy PUFA produced by rabbit neutrophil lipoxygenase when DGLA is used as a substrate. Although the biological activities of 8(S)-HETrE have not been well characterized, it is expected to behave similarly to 8(S)-HETE.

  • 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…

  • Cayman Chemical

    A small molecule inhibitor of human cytomegalovirus viral replication (EC50 = ~5 nM with a selectivity index >15,000) that targets viral DNA cleavage and packaging.

  • Cayman Chemical

    A potent inhibitor of neprilysin, a membrane metallo-endopeptidase that cleaves peptide hormones, such as enkephalins, glucagon, and bradykinin (Ki = 4-140 nM); produced in vivo via the metabolism of the prodrug acetorphan.

  • Cayman Chemical

    A metabolite of vitamin A that acts as a ligand for both the RAR and the RXR.

  • A synthetic analog of natural PtdIns containing C6:0 fatty acids at the sn-1 and sn-2 positions; contains the same inositol and DAG stereochemistry as the natural compound.

  • Cayman Chemical

    A tumor-promoting teleocidin compound that activates PKC (Ki = 3.4 nM and 1 μM for PKCη and PKCγ, respectively); induces differentiation of human embryonic stem cells into pancreatic progenitors.

  • 8-iso PGE2 isopropyl ester is a more lipophilic form of the free acid, 8-iso PGE2. Prostaglandin esters have enhanced lipid solubility compared to their parent compounds. They are generally hydrolyzed to the free acid upon in vivo administration, making the esters useful prodrugs. In general, the…

  • Cayman Chemical

    An inhibitor of PLC-dependent processes by an undefined mechanism; inhibits platelet aggregation induced by collagen or thrombin with IC50 values of 0.6 and 5 µM, respectively.

  • Cayman Chemical

    Specifically inhibits the histone acetyltransferase Gcn5 (IC50 = 100 μM) and can inhibit pre-RNA splicing with an IC50 value of 0.5 mM.

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