Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • Cayman Chemical

    An orally available, selective inhibitor of both free and prothrombinase-bound factor Xa (Ki = 0.8 nM); effective anticoagulant in both preclinical and clinical models of venous and arterial thrombosis.

  • A small diffusible signaling molecule involved in quorum sensing in the model symbiont V. fischeri and the pathogens A. tumefaciens and P. aeruginosa.

  • Cayman Chemical

    An extract from A. lappa, a burdock plant traditionally used in Japanese Kampo medicine for its antioxidant, anti-inflammatory, antiproliferative, and antiviral activity.

  • Cayman Chemical

    A selective PAR2 agonist that stimulates cell proliferation, phosphatidylinositol hydrolysis, and calcium mobilization in in vitro functional assays (pEC50s = 6.7, 5.9, and 6.6, respectively); elicits pronociceptive activity in vivo.

  • Cayman Chemical

    The major metabolite formed during the metabolism of the non-steroidal antiandrogen flutamide by cytochrome P450 isoforms CYP1A2 and CYP3A4; inhibits the binding of testosterone to the nuclear androgen receptor (IC50 = ~300-900), blocking the expression of AR target genes.

  • Cayman Chemical

    C-6 ceramide is a cell-permeable analog of naturally occurring ceramides. With a longer carbon chain than C-2 ceramide, it is somewhat more hydrophobic, and may more closely mimic the effects of natural ceramides. C-6 ceramide mediates many diverse biological activities including apoptosis,…

  • A cell-permeable, fluorescent probe for DNA that is useful as a marker of nuclei for cell cycle studies in combination with BrdU and to distinguish nuclear morphology in apoptotic cells.

  • Cayman Chemical

    CAS Number: 1228817-38-6 Molecular Formula: C26H36N6O3 Formula Weight: 480.6

  • A latanoprost-related isomer containing both a double bond at C-13,14 and an invered (b) hydroxyl group at C-15; a potential impurity in most commercial preparations of the lantanoprost bulk drug product.

  • Cayman Chemical

    A sulfated form of taurocholic acid that may be involved in the elimination and detoxification of bile acids during hepatobiliary diseases.

  • A potent, competitive inhibitor of HO activity in vitro (Ki = 14 nM); inhibits hepatic, renal, and splenic HO activity in vivo for extended periods of time; blocks bilirubin production in vivo, decreasing HO activity in animal models of hyperbilirubinemia.

  • Cayman Chemical

    A potent, competitive inhibitor of HMG-CoA reductase (Ki = 2.3 nM).

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

  • Cayman Chemical

    A selective DNA-PK inhibitor (IC50 = 14 nM) that increases the cytotoxicity of ionizing radiation and etoposide in human colon cancer cell lines in vitro and potentiates the effects of etoposide in mice bearing human colon cancer xenograft tumors in vivo.

  • Cayman Chemical

    A trihydroxybenzoic acid that demonstrates antioxidant activity by scavenging DPPH• and HO• (IC50s = 9.4 and 191 μM, respectively) and inhibiting microsomal lipid peroxidation (IC50 = 1.51 μM).

  • LKT Labs

    Aflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin G2 is cytotoxic; it inhibits DNA synthesis and induces cell cycle arrest.

  • Cayman Chemical

    A dihydropyridine L-type calcium channel antagonist that displays antihypertensive and antianginal activity; selectively inhibits adenosine A3 receptors (Ki = 3.25 µM) and CYP3A4 catalytic activity (IC50 = 0.148 µM); activates TRPA1 channels, producing an increase in Ca2+…

  • A cyclic oligosaccharide containing seven D-(+)-glucopyranose units that is widely used to improve the aqueous solubility of various compounds, especially those containing a phenyl group.

  • Cayman Chemical

    An aminopyrimidine derivative that inhibits GSK3α and GSK3β (IC50s = 10 and 6.7 nM, respectively); activates glycogen synthesis in CHO-IR cells (EC50 = 0.8 μM) and in isolated type 1 diabetic rat skeletal muscle; has been shown to promote self-renewal of embryonic stem cells.

  • Cayman Chemical

    GSK2606414 is an orally available, selective protein kinase R-like ER kinase (PERK) inhibitor with an IC50 value of 0.4 nM. It can inhibit thapsigargin-induced PERK phosphorylation in lung carcinoma A549 cells and attenuates subcutaneous pancreatic human tumor xenograft growth in mice.…

  • Cayman Chemical

    An internal standard for the quantification of DHA by GC- or LC-MS.

  • A central component of energy storage and metabolism in vivo, providing the metabolic energy to drive metabolic pumps and serving as a coenzyme in a wide array of enzymatic reactions; acts a substrate for kinases involved in cell signaling and of adenylate cyclases that produce the second messenger cAMP.

  • Cayman Chemical

    A small molecule inhibitor of MDMX.

  • 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.

  • A first generation histamine H1 receptor antagonist (Ki = 2.6 nM) that also inhibits muscarinic acetylcholine receptors (Ki = 22 nM); penetrates the CNS, depressing central H1 receptor activity, which may relate to its sedative properties.

  • Cayman Chemical

    Docosatrienoic acid is a rare ω-3 fatty acid not readily detected in normal phospholipid PUFA pools. It inhibits [3H]-LTB4 binding to pig neutrophils at a concentration of 5 µM.

  • Butylated hydroxytoluene (BHT) is commonly used as a food and cosmetics additive; it exhibits antioxidative and anti-inflammatory activities. BHT may also display neuroprotective benefit, decreasing ethanol-induced brain damage and neurodegeneration and suppressing activation of NF-?B activation…

  • Cayman Chemical

    A potent, reversible inhibitor of AMPK (Ki = 109 nM); dose-dependently inhibits the bone morphogenetic protein type 1 receptors ACTR-I (ALK2), BMPR-IA (ALK3), and BMPR-IB (ALK6); downregulates the Akt/mTOR pathway to induce autophagy in U251 human glioma cells.

  • LKT Labs

    Acivicin is a fermentation product of Streptomyces; it is a glutamine analog. Acivicin inhibits ?-glutamyl transferase, CTP synthetase, GMP synthetase, and FGAM synthetase, preventing purine synthesis. Acivicin exhibits anticancer and antifungal activity, although its potential chemotherapeutic…

  • Cayman Chemical

    A β-lactam antibiotic in the cephalosporin class.

  • Cayman Chemical

    Blocks mitochondrial complex III; inhibits the activity of the NADH oxidase in certain bacteria.

  • Cayman Chemical

    A non-selective NSAID exhibiting IC50 values of 0.5 and 2.33 µM for human recombinant COX-1 and COX-2, respectively.

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