Cayman Chemical

A selective inhibitor of PDGFRβ and PDGFRα kinases (IC₅₀s = 1 and 10 nM, respectively); antiangiogenic and antitumor activity in several in vivo tumor models.

A VEGFR inhibitor (IC₅₀s = 0.82, 0.037, and 0.42 µM for hVEGFR1, 2, and 3, respectively); also inhibits Tie2 and RET with IC₅₀ values of 0.65 and 0.41, respectively; reduces inflammation in a mouse model of psoriasis and in pig models of contact hypersensitivity and...

A potent and selective histamine H4 receptor antagonist, with a Ki value of approximately 4 nM against the human, mouse, and rat H4 receptors; inhibits mast cell chemotaxis induced by 10 μM histamine (IC50 = 40 nM), reduces neutrophil influx in mouse peritonitis models (10 mg/kg s.c.), and...

9-OxoODE results from oxidation of the allylic hydroxyl of either 9(S)- or 9(R)-HODE. Rabbit reticulocyte plasma and mitochondrial membranes contain both 9- and 13-oxoODEs, representing about 2% of the total linoleate residues in the membranes. Most of these oxidized linoleate residues are...

A formylated form of tetrahydrofolic acid, the reduced form of folic acid; used to prevent toxicity following high-dose methotrexate therapy, to enhance the antitumor activity of 5-fluorouracil, and as a folate supplement.

EPA is an ω-3 fatty acid abundantly available in marine organisms. Peroxide free EPA has been chromatographed under scrupulously oxygen free conditions to insure the removal of all contaminating fatty acid peroxides. The peroxide free EPA is protected from autoxidation by the antioxidant BHT...

A non-nucleoside DNA methyltransferase inhibitor (IC₅₀ = 115 nM in vitro) that significantly reduces the methylation of genomic DNA in cells at 10 μM without detectable toxicity.

A potent, irreversible inhibitor of EGFR kinase activity (IC₅₀ = 370 pM); halts cell cycling in cells that overexpress EGFR or c-ErbB2 (IC₅₀s = 31-125 nM); profoundly blocks the growth of EGFR-overexpressing tumors in nude mice when given orally at 80 mg/kg/day for 10 days.

Antigen: human COX-2 amino acids 567-599 Host: rabbit Cross-Reactivity: (+) human, mouse, and ovine COX-2; (−) COX-1 (all species) Application(s): WB Expression of COX-2, the inducible form of COX, is regulated by growth factor tumors, tumor promoters, bacterial endotoxin, and cytokines.

An inhibitor of RGS4 (IC50 = 30 nM); blocks GTPase activity and Gα0-dependent translocation of RGS4 to the membrane.

Active recombinant N-terminal His-tagged protein expressed in E. coli O6-methylguanine-DNA Methyltransferase (MGMT) is a DNA repair enzyme responsible for demethylating O6-methylguanine (O6-mG).

A metabolite of vardenafil that is formed by the action of CYP3A4 and CYP3A5.

Antigen: human and rat Cav-3 amino acids 19-41 (CKEIDLVNRDPKNINEDIVKVDF) The sequence is 77% homologous to Cav-1 from mouse, human, chicken, and dog. Host: rabbit Cross-reactivity: (+) bovine and rat Cav-1, human and rat Cav-3; other species not tested Application: WB; other applications not tested...

Antigen: human 11β-HSD2 amino acids 25-40 (RSDLRLGRPLLAALAL) Host: rabbit Cross Reactivity: (+) human, mouse, and rat 11β-HSD2 Application(s): WB 11β-HSD2 plays a critical role in normal physiology in the corticosteroid regulation of sodium homeostasis and the pathophysiology of...

A natural quinone found in cell membranes, primarily mitochondrial membranes, with highest concentrations in the heart, lungs, liver, kidneys, spleen, pancreas, and adrenal glands; component of the electron transport chain; participates in aerobic cellular respiration, generating ATP and also acts...

A cell-permeable suppressor of TSA action, reducing TSA-induced acetylation of histone and tubulin in A549 cells when given at 50 µM; prevents TSA-mediated cell cycle arrest and apoptosis; blocks the action of the HDAC inhibitor SAHA, preventing SAHA-induced hyperacetylation of tubulin in A549...

Induces neuronal differentiation in skeletal muscle cells, as indicated by the upregulated expression of neuron-specific markers; effective with mature muscle fibers as well as myoblasts.

A para-nitro aniline chromophore cleaved by caspases (Km = 18, 11, 32, 180, and 12 µM for caspases-1, -3, -4, -6, and -7, respectively); not cleaved by caspase-2; monitored colorimetrically at 405 nm.

A structural analog of 14(15)-EET that antagonizes EET-induced relaxation of vascular smooth muscle.

An endogenous agonist of the CB1 and CB2 receptors; it is the most abundant molecular species of monoacylglycerol found in rat brain.

An F-series PG analog in which the C-1 carboxyl group has been modified to an unsubstituted amide; expected to show the typical intraocular effects of latanoprost, but with the much slower hydrolysis pharmacokinetics of the PG N-amides.

Cayman's OX2R Reporter Assay Kit consists of a 96-well plate coated with both OX2R and Secreted Alkaline Phosphatase (SEAP) reporter constructs (OX2R Reverse Transfection Strip Plate). Cells grown on the transfection complex will express OX2R at the cell surface and the recombinant G-protein...

A potent allosteric inhibitor of PRMT3 (IC₅₀ = 50 nM) with >100-fold selectivity over other methyltransferases and other non-epigenetic targets; avidly binds PRMT3 (Kd = 50 nM by isothermal titration calorimetry) and inhibits histone methylation in cells with an IC₅₀ value...

A broad spectrum caspase inhibitor, blocking caspases-3, -7, -8, -9, -10, and -12 and inhibiting apoptosis when used at 10 µM; more effectively inhibits apoptosis and is much less cytotoxic than Z-VAD-FMK; can be used in vivo.