Biologically Active Small Molecules, Chemicals

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Chemicals Biologically Active Small Molecules

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  • Cayman Chemical

    A pan-caspase inhibitor that blocks apoptosis, prevents the production of cytokines, and inhibits T cell proliferation dose-dependently at 1-100 μM.

  • Cayman Chemical

    A naturally-occurring dimethyl ether analog of resveratrol; acts as a powerful antioxidant, suppresses the synthesis of PGE2 from LPS-stimulated human peripheral blood mononuclear cells (IC50 = 1.0 μM), and inhibits cell proliferation (IC50 = ~60 μM); evokes effects that…

  • Cayman Chemical

    A reversible, selective, allosteric antagonist of mGluR7 that blocks agonist-induced calcium mobilization (IC50 = 26 nM).

  • Cayman Chemical

    A stable, cell-permeable form of α-ketoglutarate which accumulates rapidly and preferentially in cells with a dysfunctional TCA cycle; stimulates PHD activity and increases HIF-1α turnover when used at 1 mM; competitively blocks succinate- or fumarate-mediated inhibition of PHD.

  • Cayman Chemical

    A cell permeable analog of BAPTA that binds calcium only after the AM group is removed by cytoplasmic esterases; commonly used at 10-100 μM to evaluate the role of intracellular calcium in cell signaling; also inhibits Kv channels, including Kv1.3, Kv1.5, and Kv11.1 (Ki = 1.45, 1.23, and 1.30…

  • An EPA-containing MAG amide analog that inhibits the growth of human lung carcinoma A549 cells, producing 98.4% growth inhibition when applied at 3 µM; an analog of EPEA, a natural N-acylethanolamide that impacts aging and inflammation.

  • Cayman Chemical

    A macrolide antibiotic with antifungal activity; also cytotoxic against trypanosomes (IC50 = 120-540 ng/ml) while being more than 25,000 times less effective against mammalian cells; inhibits bacterial and mitochondrial ATP synthases.

  • Cayman Chemical

    15-OxoETE is produced by oxidation of the 15-hydroxyl of 15-HETE. Whether this is a major pathway of 15-HETE metabolism is yet to be clearly established.

  • An inhibitor of S1P lyase; treatment of mice (50 µg/ml in drinking water) increases lymphoid tissue S1P concentrations 100-fold, reducing lymphocyte egress from thymus and peripheral lymphoid organs, resulting in reversible lymphopenia.

  • Cayman Chemical

    BW 245C is a selective agonist for the DP1 receptor. The Ki of BW 245C for the inhibition of [3H]-PGD2 binding to isolated human platelet membranes is 0.9 nM. It has a reported IC50 of 2.5 nM for the inhibition of ADP-induced human platelet aggregation and an IC50 of 250 nM for the inhibition of…

  • Cayman Chemical

    A natural type B trichothecene produced by certain species of the fungus Fusarium; inhibits protein biosynthesis, binds to peptidyl transferase, and inhibits the synthesis of RNA and DNA; passes the blood-brain barrier at different rates in different animals.

  • Cayman Chemical

    A cell-permeable and selective inhibitor of PIKfyve (IC50 = 33 nM); reversibly impairs endosomal trafficking in NIH3T3 cells and blocks retroviral exit by budding from cells; inhibits basal and insulin-activated 2-deoxyglucose uptake (IC50 = 54 nM) in adipocytes.

  • 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…

  • Cayman Chemical

    A polysaccharide made of α-D-glucose units that constitutes about 20% of starch; acts as an indicator, turning blue in the presence of iodine, and has also been coupled to magnetic beads for the isolation and purification of maltose-binding protein fusion proteins.

  • Cayman Chemical

    A mixture of oligomycins A, B, and C

  • Cayman Chemical

    PLC catalyzes the hydrolysis of phosphatidyl inositol (4,5) bisphosphate (PIP2) on the cytoplasmic side of the cell membrane to yield diacylglycerol and inositol-1,4,5-triphosphate (IP3). This reaction initiates a well-known signal transduction pathway common to most cells. PLC thio-PIP2 is an…

  • A phosphonic analog of ATP and agonist of P2X1 and P2X3 (EC50 = ~1 µM); ~1,000-fold less potent at P2X2, P2X receptors 4-7, and P2Y receptors; used as a stable analog of ATP to study the interaction of ATP with kinases and other proteins.

  • A major organic tracer generated by burned cellulose; used to evaluate, in atmospheric samples, the burning of wood.

  • 2-Tert-butyl-4-hydroxyanisole (2-BHA) is one component of butylated hydroxyanisole (BHA). This compound is commonly used as a food additive; it exhibits antioxidative activity. 2-BHA acts as a phase II enzyme inducer, increasing levels of glutathione and glutathione-S-transferase.

  • LKT Labs

    Antimycin A was initially produced by Streptomyces. Antimycin A binds cytochrome c reductase, inhibiting electron transport chain activity, oxidative phosphorylation, and ATP synthesis. Antimycin A is used in research models to study mitochondrial respiration and superoxide production. Grade: ≥98%

  • Cayman Chemical

    An inactive metabolite of artemisinin.

  • A cell-permeable, reversible inhibitor of a mitochrondrial glutaminase splice variant, glutaminase C (IC50 = ~2.5 µM), which is commonly found in cancer cells; blocks transformation induced by Rho GTPases and inhibits the proliferation of cancer cell lines without affecting normal cells.

  • N-Acetyl-S-(N’-phenylthiocarbamoyl)-L-cysteine (PITC) is a cysteine conjugate of N-acetyl-phenylisothiocyanate. Isothiocyanates are typically found in plants of the Brassicaceae family, including broccoli, cabbage, and radish. Isothiocyanates are best known for their antioxidative, anticancer…

  • Cayman Chemical

    Best known as a potent dual inhibitor of c-Src and Abl (IC50 = 1.2 and 1.0 nM, respectively); can be effective in regulating tumor growth and differentiation; also inhibits other members of the Src and TEC families and certain other kinases at nanomolar concentrations.

  • 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

    A potent uncoupler of oxidative phosphorylation in mitochondria that disrupts ATP synthesis by transporting protons across cell membranes.

  • Cayman Chemical

    The diol resulting from the sEH opening of (±)11(12)-EET; contracts artery rings with approximately 70% of the magnitude of (±)11(12)-EET.

  • Chenodeoxycholic acid is an endogenous bile acid synthesized by the liver; it acts as an agonist at the farnesoid X receptor (FXR). Chenodeoxycholic acid exhibits anticancer and gastrointestinal motility modulating activities. This compound treats chronic constipation and displays protective…

  • Cayman Chemical

    A selective NMDA receptor antagonist (Kd = 1.4 μM) that competitively inhibits the glutamate binding site of NMDA receptors; widely used to study the activity of NMDA receptors particularly in regard to researching synaptic plasticity, learning, and memory.

  • Cayman Chemical

    An anthracycline antitumor antibiotic agent that inhibits DNA topoisomerase II by inducing double-stranded DNA breaks; inhibits nucleic acid synthesis and induces apoptosis by intercalating within DNA.

  • AFC is a synthetic substrate for the isoprenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase). Because it is able to serve as a substrate for the methyltransferase, it effectively functions as an inhibitor of methylation of endogenous isoprenylated proteins.

  • Cayman Chemical

    A quinazoline that inhibits the tyrosine kinase activity of EGFR (IC50 = 0.025 nM); inhibits the growth of SKOV3 and MDA-468 tumor cell lines (EC50s = 6.5 and 30 µM, respectively).

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