20 products were found matching "Cay11750"!

Piperine is a natural alkaloid that can be isolated from black pepper. It activates transient receptor potential vanilloid type 1 receptor (TRPV1, EC50 = 38 µM) and modulates GABAA receptors (EC50s = 43-60 µM). At similar levels, piperine inhibits both monoamine oxidases (MAOs), with IC50 values of 21 and 7 µM for...

Endocannabinoids such as 2-arachidonoyl glycerol (2-AG) and arachidonoyl ethanolamide are biologically active lipids that are involved in a number of synaptic processes including activation of cannabinoid receptors. Monoacylglycerol lipase (MAGL) is a serine hydrolase responsible for the hydrolysis of 2-AG to...

NKY80 is a cell-permeable inhibitor of adenylyl cyclase (AC) that is selective for isoform AC5 over AC2 and AC3 (IC50s = 8.3 µM, 1.7 mM, and 132 µM, respectively in the presence of Gsalpha GTPgammaS-forskolin). It is a non-competitive inhibitor with respect to ATP (Cay-14498) and forskolin (Cay-11018) and tissue...

N-4-Tosyl-L-arginine methyl ester (TAME) is a synthetic substrate of serine proteases, including thrombin, trypsin, chymotrypsin, and kallikreins. It can be used to evaluate serine proteases from diverse sources. TAME also binds to and inhibits anaphase-promoting complex, a ubiquitin ligase, in Xenopus egg...

BHPI is an antagonist of estrogen receptor alpha (ERalpha) that blocks 17beta-estradiol-induced proliferation of drug-resistant breast, endometrial, and ovarian cancer cell lines at concentrations ranging from 10 to 1,000 nM. It is effective in vivo, driving tumor regression in mice bearing MCF-7 xenografts at a...

Lysergol is an ergot alkaloid that has been found in S. sorghi and an agonist of the serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT2A, and 5-HT2C (EC50s = 73, 1.6, and 6.6 nM, respectively, in a FLIPR assay). It induces contractions in isolated rat tail arteries (EC50 = 436.5 nM). Lysergol (10 µg/ml) also enhances...

Jasplakinolide is a natural macrocyclic peptide first isolated from a marine sponge. It potently inhibits the proliferation of PC3 prostate carcinoma cells (IC50 = 35 nM) by binding F-actin (KD = 15 nM). This binding of jasplakinolide to actin, which is competitive with phalloidin, stabilizes actin filaments in...

Purpurin is a naturally occurring reddish-yellow pigment found in madder root (R. tinctorum) that has been used both in herbal remedies and as food coloring. It can also be synthetically derived from 9,10-anthraquinone. Purpurin is protective against a number of food-derived heterocyclic amines in bacterial...

Ionotropic GABAA receptors are ligand-gated ion channels that facilitate the passing of chloride ions across the cell membrane and promote an inhibitory influence on target neurons. These receptors are the major targets for benzodiazepines and related anxiolytic drugs. Bicuculline is a competitive GABAA receptor...

24alpha-ethyl Cholesterol is a phytosterol that has been found in S. plebia and has diverse biological activities. It protects lard from thermal oxidation when used at concentrations of 0.02 and 0.04%. 24alpha-ethyl Cholesterol (100 µM) induces glucose uptake and lipolysis in primary rat differentiated adipocytes...

Diacerein is a prodrug form of the anthraquinone derivative rhein (Cay-17345). It inhibits RANKL- and IL-1beta-induced differentiation of RAW 264.7 cells into osteoclasts when used at a concentration of 20 µg/ml. Diacerein (20 µg/ml) reduces levels of interleukin-1beta-converting enzyme (ICE), also known as...

SER-601 is a potent and selective peripheral cannabinoid (CB2) receptor agonist with 190-fold selectivity for CB2 over the central CB1 receptor (Kis = 6.3 and 1,220 nM, respectively). At 3 mg/kg, SER-601 has analgesic effects in a formalin-induced nocifensive study in mice without cannabis-like behavioral effects...