Select up to 3 products
An active metabolite of propranolol, inhibiting β1- and β2-adrenergic receptors with KD values of 2.4 and 5.8 nM, respectively; comparable to propranolol in potency in antagonizing the effects of isoprenaline on heart rate and blood pressure in cats and dogs.
A selective small molecule inhibitor of PKD (IC50s = 182, 280, 227 nM for PKD1, 2, and 3, respectively); 25 µM has been shown to inhibit prostate cancer cell proliferation, cell migration, and invasion.
12(S)-hydroxy-16-Heptadecynoic acid is a mechanism-based inhibitor of CYP450 ω-hydroxylase. It inhibits prostaglandin ω-hydroxylase with a Ki value of 1.8 µM.
2-Arachidonoyl glycerol (2-AG; Item No. 62160) has been isolated from porcine brain, and has been characterized as the natural endocannabinoid ligand for the CB1 receptor. Incubation of 2-AG with COX-2 and specific PGH2 isomerases in cell cultures and isolated enzyme preparations results in...
PGA1 ethyl ester is a prodrug form of PGA1 with enhanced lipid solubility. Prostaglandins of the A-series are natural products of gorgonian soft coral. PGA1 has been shown to cause renal vasodilation, increased urine sodium excretion, and lowered arterial pressure in hypertensive patients. There are...
PGG2 is the first intermediate in the COX pathway which is stable enough to be isolated and characterized. It is the C-15 hydroperoxide of PGH2. Under normal conditions, PGG2 is quickly metabolized by the peroxidase activity intrinsic to both COX-1 and -2 to give PGH2, which serves as the key...
A selective, orally active CysLT1 receptor antagonist; blocks the binding of LTD4 to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively.
The sirtuins represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs) that catalyze a reaction coupling lysine deacetylation to the formation of nicotinamide and O-acetyl-ADP-ribose. Cayman’s Direct Fluorescent Screening Assay Kits provide a convenient...
An ATP-competitive, reversible inhibitor of FAK (IC50 = 1.5 nM) and PYK2 (IC50 = 14 nM); inhibits FAK phosphorylation (EC50 = 93 ng/ml) in glioblastoma-bearing mice and has been shown to regress tumors in multiple xenograft models.
A competitive, non-NMDA glutamate receptor antagonist (IC50s = 0.3 and 1.5 μM for AMPA and kainate receptors, respectively, versus IC50 = 25 μM for NMDA receptors).
A single enantiomer of a potent and selective inactivator of KIAA1363, a MAGE hydrolase an enzyme that is upregulated in aggressive cancers from various tissues (IC50 = 150 nM when tested as a racemic mixture in SK0V-3 cells); activity of the individual enantiomers of AS 115, i.e,. (+)-AS 115 and...
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.
A primary metabolite of the anti-cancer compound paclitaxel, produced by the action of the CYP450 isoform CYP2C8.
A natural proteasome inhibitor that irreversibly inhibits all three protease activities within the proteasome (IC50s = 3.5, 28, and 430 nM for β5 (chymotrypsin), β2 (macropain), and β1 (C5) subunits, respectively), both in vitro and in vivo.
A 13R,14S-dihydroxy DHA formed by recombinant human macrophage 12-LO and sEH co-incubated with DHA; reduces neutrophil infiltration in a mouse model of peritonitis and enhances human macrophage phagocytosis of zymosan A.
An analytical reference standard categorized as a phytocannabinoid; a constituent of hashish that has also been isolated from C. sativa plants; regulated as a Schedule I compound in the United States; intended for research and forensic applications
A naturally occurring macrotetrolide antibiotic that acts as an ionophore for monovalent cations, including K+, NH4+, and Tl+.
For the quantification of TXB2 in urine, serum, tissue culture supernatants, and other sample matrices Sensitivity (80% B/B0): 5 pg/ml Assay Range: 1.6-1,000 pg/ml Thromboxane A2 (TXA2) is produced from arachidonic acid by many cells and causes irreversible platelet aggregation and...
A ceramide analog that contains a mixture of all four possible stereoisomers.
PGF3α is a COX product of EPA. The biosynthesis of PGF3α from EPA was demonstrated in vitro in human and rabbit ocular tissues. It has only 25% affinity at the ovine luteal FP receptor compared to PGF2α.
A glycopeptide antitumor antibiotic that produces single and double-strand DNA breaks in tumor cells to interrupt their cell cycle; has been used for the treatment of Hodgkin’s lymphoma in combination with doxorubicin, squamous cell carcinomas, testicular cancer, as well as in animal models of...
A broad-spectrum antibiotic used in cell culture systems as a selective agent for cells harboring the bacterial tetR gene, which are resistant to the antibiotic.
An organic phosphorus supplement that is given, most commonly with cyanocobalamin, to cattle, swine, horses, and poultry for the prevention or treatment of deficiencies.
A selective ROCK inhibitor (IC50s = 1.6 and 6 nM for ROCK-I and ROCK-II, respectively); blocks the generation of inflammatory cytokines in LPS-stimulated monocytes and induces vasorelaxation in preconstricted rat aorta (IC50 = 35 nM).