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Cayman’s FABP4 Ligand Binding Assay provides a simple, reproducible, and sensitive tool for the identification of FABP4 ligands. The assay makes use of a detection reagent that exhibits increased fluorescence at 500 nm when bound to FABP4. Any strong ligand and/or inhibitor of FABP4 will...
PGF2α is rapidly metabolized to 13,14-dihydro-15-keto PGF2α in vivo, by the enzymes 15-hydroxy PG dehydrogenase and D13-reductase. Measurement of 13,14-dihydro-15-keto PGF2α in plasma can be used as a marker of the in vivo production of PGF2α. The Cayman’s...
A potent and selective inhibitor of HDAC6 (IC50 = 36 nM) that poorly blocks other HDAC enzymes; cell permeable, inhibiting the acetylation of tubulin in cells with an IC50 value of 210 nM.
Antigen: synthetic peptide containing amino acids near the 214/215 cleavage site of human PARP Isotype: IgG2bκ Host: mouse Cross Reactivity: (+) human PARP Application(s): FC (intracellular) and WB PARP is a 116 kDa nuclear chromatin-associated enzyme that is cleaved during apoptosis by...
A small molecule radiosensitizer that has proven to be an effective and nontoxic immunochemical hypoxia marker for human squamous cell carcinomas of the cervix, head and neck.
Immunogen: Synthetic peptide from an internal region of human EP3 receptor conjugated to KLH Host: rabbit Cross Reactivity: (+) human, bovine, mouse, and rat EP3 receptors; (−) EP1, EP2, and EP4 receptors Application(s): ICC and WB As a result of splice variation, the EP3 receptor can be...
A cytotoxic compound that at 1 µM activates aryl hydrocarbon receptor signaling, inducing transcription of cytochrome P450 1A1, which leads to the formation of DNA adducts and cell cycle arrest; can increase the levels of ROS as well as activate JNK, ERK, and p38MAPK in certain ovarian,...
An indole diterpene which potently and reversibly inhibits large conductance Ca2+-activated K+ (BKCa) channels, as shown in patch clamp (Ki = 1.9 nM) and whole smooth muscle cell studies (Ki = 35.7 nM).
Peptide Sequence: rat FAAH amino acids sequence 561-579 (CLRFMREVEQLMTPQKQPS) To be used in conjunction with Cayman’s FAAH polyclonal antibody (Catalog No. 101600) to block protein-antibody complex formation during analysis for FAAH.
Antigen: phosphopeptide corresponding to amino acid residues surrounding phospho-Ser523 of human 5-LO Host: rabbit Cross Reactivity: (+) human, rat, and non-human primate 5-LO Application: WB 5-LO activity is regulated by PKA phosphorylation at serine-523. Under normal conditions, this...
A long-acting sulfonylurea that inhibits KATP channels in pancreatic β-cells (IC50 = 3 nM), which leads to the release of insulin; increases the activity of intracellular insulin receptors and prevents insulin receptor downregulation during chronic insulin stimulation through a...
An enhancer of several neurotransmitters, including acetylcholine, dopamine, serotonin, and glutamate by blocking M-type K+ current (IC50 = 2.4 µM); also acts as an agonist of TRPV1 (EC50 = 115 µM in HEK293 cells voltage clamped at -60 mV).
A potent, selective PAF receptor antagonist (Ki = 9.9 nM at human PAF receptors); displays anti-inflammatory, antiangiogenic, and anticancer activity.
A coenzyme that is tightly bound to enzymes catalyzing oxidation and reduction reactions in a variety of biosynthetic pathways; binds the FMN riboswitch (RFN element) on RNA to alter gene regulation; a substrate of FMN phosphohydrolases.
A macrolide antibiotic that inhibits the mitochondrial F1FOATPase; inhibits K-Ras plasma membrane localization in MDCK cells with an IC50 value of 3.49 nM and is cyctoxic to SW620 colon cancer cells with an IC50 value of 36 µM.
A benzimidazole that selectively disrupts the activity of IRAK 1 and 4 (IC50 = 0.3 and 0.2 µM, respectively).
A primary amide analog of (+)-JQ1 which has shown superior bioavailability with oral or i.p. administration; inhibits BRD4 binding and action in vitro or in cells; arrests the growth of leukemia T cells in vitro (EC50 = 91 nM) and rapidly suppresses leukemia burden in mice.
A potent, selective inhibitor of type I PRMTs (IC50s = 20, 119, 83, 8, and 8 nM for PRMT1, 3, 4, 6, and 8, respectively).
25-hydroxy Cholesterol is an oxysterol.{20437} It is formed from cholesterol by cholesterol-25-hydroxylase, and its production can be induced by inflammation or infection.{60052} 25-hydroxy Cholesterol suppresses endogenous cholesterol synthesis by binding to insulin-induced gene (INSIG) proteins...
A potent and selective inhibitor of Wip1 (IC50 = 6 nM); increases phosphorylation of Wip1 substrates and blocks cell cycling in cancer cells; orally bioavailable, causing inhibition of lymphoma xenograft growth in mice.
A stable metabolite of histamine.
A reversible and selective inhibitor of calpain I (μ-calpain, Ki = 19 nM), with lower affinities for calpain II (m-calpain, Ki = 120 nM) and cathepsin B (Ki = 750 nM).
An ERβ Selective agonist; exhibits 70-fold higher relative binding affinity for ERβ versus ERα.
A PGE2 metabolite found in the semen of primates, including man; potent smooth muscle relaxant and a selective agonist for the EP2 receptor (EC50 = 200 nM for relaxing cat tracheal rings).