8 products were found matching "Cay15731"!

Inactivation of the tumor suppressor p53 commonly coincides with increased signaling through NF-kappaB in cancer. CAY10681 is a dual modulator of p53-MDM2 interaction and NF-kappaB signaling. It potently binds MDM2 (Ki = 250 nM), reducing MDM2-mediated turnover of p53. CAY10681 also inhibits phosphorylation of...

Tiotropium is an antagonist that binds to M1, M2, and M3 muscarinic acetylcholine receptors (Kds = 0.43, 0.54, and 0.69 nM, respectively, for human receptors). It decreases acetylcholine-induced contraction of isolated guinea pig trachea in a concentration-dependent manner. In vivo, tiotropium (1 g/L inhaled...

Orexin A is a 33 amino acid hypothalamic neuropeptide with a role in appetite regulation, wakefulness, locomotor activity, hypothalamic-pituitary-adrenal activity, and pain thresholds. Orexin signaling is activated by nutrient depletion, causing an increase in food intake by delaying the signals of satiety. It...

Aldosterone is a steroid hormone secreted by the adrenal cortex and is the principle mineralocorticoid controlling sodium and potassium balance. Its primary role is to promote unidirectional salt reabsorption in epithelial tissues. Aldosterone is synthesized from cholesterol in the zona glomerulosa of the adrenal...

Transcriptional activation by NF-kappaB is limited by IkappaBalpha binding, which masks the NF-kappaB nuclear localization signal that initiates nuclear translocation. Cytokines trigger a signaling cascade of kinases that target IkappaBalpha for degradation, enabling NF-kappaB to promote gene expression. Because...

Dehydroepiandrosterone sulfate (DHEAS) is a metabolite of dehydroepiandrosterone that is the major secretory product of adrenal glands and is the predominant circulating precursor for active steroid hormones in humans. For example, in the fetoplacental-maternal unit, DHEAS acts as the primary precursor for placental...

Prostaglandin E2 (PGE2, Cay-14010) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, inflammation, cancer, and atherosclerosis. MF498 is a selective EP4 receptor antagonist (Ki...

The anaphylatoxin C3a induces a range of responses by activating its G protein-coupled receptor, C3aR, resulting in calcium mobilization. SB 290157 is a non-peptide antagonist of C3aR, competitively blocking C3a binding with an IC50 value of 200 nM. It potently inhibits a wide variety of C3a-induced responses in...