12 products were found matching "Cay10010425"!

Prostaglandin D1 (PGD1) is the theoretical D-series metabolite of dihomo-gamma-linolenic acid (DGLA), but to date it has not been isolated as a natural product. It is an inhibitor of ADP-induced platelet aggregation in humans with an IC50 value of 320 ng/ml, about 1/10 as potent as PGD2. 13,14-dihydro-15-keto...

Nilotinib is an inhibitor of wild-type and mutant Bcr-Abl (IC50s = 15 and 9-400 nM, respectively). It is selective for wild-type and mutant Bcr-Abl over Src and LYN (IC50s = >5,000 nM for both). Nilotinib inhibits Bcr-Abl autophosphorylation and cell proliferation in Ba/F3 cells expressing wild-type or mutant...

KRP 203 is a sphingosine-1-phosphate receptor 1 (S1P1) agonist. It selectively induces calcium mobilization in CHO-K1 cells expressing mouse S1P1 over mouse S1P3 and S1P4 (EC50s = 0.84, >1,000, and 9.61 nM, respectively). In vivo, KRP 203 (0.3 mg/kg) prevents the development of wasting syndrome, decreases diarrhea...

ADHP is a highly sensitive, stable substrate for horseradish peroxidase (HRP) that enables selective detection of H2O2. This colorless, non-fluorescent reagent reacts with H2O2 to produce the fluorescent compound resorufin, which can be analyzed using an excitation wavelength of 520-550 nm and an emission wavelength...

SP6000125 is a pan-inhibitor of JNK (IC50s = 0.04, 0.04, and 0.09 µM for JNK1, -2, and -3, respectively). It is greater than 300-fold selective for these enzymes over a panel of 17 additional kinases at 10 µM. SP6000125 reduces LPS-induced production of IL-1beta, IL-8, and TNF-alpha in isolated human peripheral...

Pyridinylimidazoles, often termed CSAIDs, are a class of anti-inflammatory compounds that inhibit eicosanoid production and suppress the synthesis of cytokines in human monocytes. Because of its high specificity, one predominant pyridinylimidazole, SB203580, is frequently used to inhibit p38 MAPK, the tyrosine...

Epoxyeicosatrienoic acids (EETs), such as 11(12)-EET and 14(15)-EET, are cytochrome P450 metabolites of arachidonic acid that have been identified as endothelium-derived hyperpolarizing factors with vasodilator activity. 14,15-EE-8(Z)-E is a structural analog of 14(15)-EET that demonstrates potent vasodilator...

Bimatoprost is the Allergan trade name for 17-phenyl trinor prostaglandin F2alpha ethyl amide (17-phenyl trinor PGF2alpha ethyl amide), an F-series PG analog which has been approved for use as an ocular hypotensive drug. Oxidation of the C-15 hydroxyl group produces 15-keto-17-phenyl trinor PGF2alpha ethyl amide....

Lubiprostone is an activator of chloride channel protein 2 (ClC-2) and a bicyclic derivative of prostaglandin E1 (PGE1, Cay-13010). It induces chloride currents in HEK293 cells expressing recombinant human ClC-2 (EC50 = ~17 nM), but not CFTR, chloride channels. Lubiprostone (1 µM) induces short-circuit currents, a...

Prostacyclin (PGI2) is a potent vasorelaxant and inhibitor of platelet aggregation. It mediates its actions by binding to a specific G protein-coupled receptor, the IP receptor, on the surface of endothelial cells, arterial smooth muscle, and platelets. The IP receptor also participates in signal transduction of the...

Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative, compounds that act as PTK blockers. PTK inhibitors that preferentially inhibit the epidermal growth factor (EGF) receptor kinase block...

Prostaglandin F2alpha (PGF2alpha), acting through the FP receptor, causes smooth muscle contraction and exhibits potent luteolytic activity. Both 17-phenyl trinor PGF2alpha and 16-phenoxy tetranor PGF2alpha are metabolically stable analogs of PGF2alpha and potent agonists for the FP receptor. 17-phenoxy trinor...