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Ins(1)P1 is a member of the inositol phosphate (InsP) molecular family of second messengers that play a critical role in the transmission of cellular signals. The most studied InsP, Ins(1,4,5)P3, is a second messenger produced in cells by PLC-mediated hydrolysis of...
An ATP-competitive inhibitor of the D2 domain of the p97 ATPase (IC50 = 0.11 µM; Ki = 0.22 µM); disrupts ERAD and autophagy pathways; blocks proliferation of HCT15 and SW403 colon cancer cell lines (GI50s = 0.76 and 0.5 µM, respectively) rapidly mobilizing caspase-3 and...
Cayman’s Histamine EIA is a derivitization-amplified competitive enzyme immunoassay which detects histamine within the range from 40 to 5,500 pg/ml. The assay can be used for the analysis of histamine in blood (plasma or serum) without extraction or purification. The use of other sample types...
The ethanolamine-amide analog of PGE1.
A chloride channel blocker (IC50 = 80 nM) that has also been identified as a GPR35 agonist; has protonophoric activity, uncoupling mitochondrial ATP synthesis in phagocytes.
A more water soluble, salt version of niclosamide that has been used to increase energy expenditure and lipid metabolism in mice; 125 mg/kg/day prevents high-fat diet-induced hepatic steatosis and insulin resistance and improves glycemic control in db/db mice.
PGE2 is one of the primary COX products of arachidonic acid and one of the most widely investigated PGs. Its activity influences inflammation, fertility and parturition, gastric mucosal integrity, and immune modulation. The effects of PGE2 are transduced by at least four distinct receptors...
13(R)-HODE is the opposite enantiomer of the 13(S)-HODE produced when linoleic acid is incubated with soybean LO. The presence of 13(R)-HODE in the supernatants and membranes of cultured bovine endothelial cells has been attributed to COX metabolism. 13(R)-HODE is a weak (IC50 = 2.7...
An immediate precursor of capsaicin as well as a by-product of capsaicin degradation that significantly increases the yield of capsaicin when added to immobilized and freely suspended cells of C. frutescens.
A form of DAG containing the saturated long-chain (18:0) stearic acid at both the sn-1 and the sn-2 position.
A plant polyphenol that is classified as a chalcone; a potent antioxidant that affects the numerous pathways modulated by oxidant tone, including inflammation, cancer, and immune response.
Source: 10 µg of recombinant N-terminal GST-tagged protein expressed in baculovirus expression system Mr: 75.2 kDa HDAC4 is a Class IIa HDAC that can shuttle between the nucleus and cytoplasm, suggesting potential extranuclear functions by regulating the acetylation status of nonhistone...
The active metabolite of the antiviral prodrug oseltamivir; acts as an inhibitor of influenza neuraminidases A and B (IC50 values are 0.1 to 4.9 nM for both enzymes), in this way preventing virus budding and release.
A metabolite of PGD2 via the 15-hydroxy PGDH pathway.
Sulprostone is a metabolism resistant synthetic analog of PGE2. It is a selective agonist for EP3 receptors with a Ki value of 0.35 nM at the human recombinant EP3-III receptor and an IC50 of 0.01 µM for the inhibition of PGE2 binding. Sulprostone is a potent stimulator of uterine...
A potent inhibitor of hedgehog-induced cellular activity (IC50 = 100-200 nM); binds directly with the pathway activator Smo (Ki = 44 nM); blocks proliferation and induces apoptosis in mouse basal cell carcinoma and causes regression of basaloid lesions triggered by ultraviolet light in...
Fluprostenol is a metabolically stable analog of PGF2α with potent FP receptor agonist activity. The isopropyl ester of fluprostenol has been approved for use as an ocular hypotensive drug for the treatment of glaucoma and is sold under the Alcon trade name Travoprost. Acting as a prodrug,...
A positive modulator of the Wnt/β-catenin pathway, as it augments Wnt-mediated signaling in cells at concentrations of 5 to 20 µM; active in vivo, altering Wnt-dependent gene expression and embryonic development in zebrafish.
SKF 38393 is a partial agonist of the dopamine D1-like receptors D1 and D5 (Kis = 1 and ~0.5 nM, respectively). It less potently binds D2, D3, and D4 receptors (Kis = ~150, 5,000, and 1,000 nM, respectively).
An endogenous ligand for the growth hormone secretagogue receptor that stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis.
A carbamate pesticide that reversibly inhibits acetylcholinesterase.
Thiazolidinediones (TZDs) are a group of structurally related PPARγ agonists with anti-diabetic actions in vivo. Rosiglitazone (BRL49653) is a prototypical TZD and has served as a reference compound for this class of PPARγ ligands. Pioglitazone is a closely related TZD which also...
An analog of valeric acid, long used as an anticonvulsant; inhibits Class I HDACs with an IC50 of ~2 mM; also inhibits GSK3 and depletes cellular IP3.
Antigen: phosphopeptide corresponding to amino acid residues surrounding phospho-Ser774 of rat dynamin Host: sheep Cross-reactivity: (+) rat dynamin Application: WB