9 products were found matching "Cay15735"!

IOX2 is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PH2, IC50 = 21 nM) with over 100-fold selectivity compared to inhibition of JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH (IC50s > 100 µM). IOX2 is active in cells, inhibiting HIF-1alpha hydroxylation in RCC4 cells at 50 µM. See the...

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...

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...

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...

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...

Alkaline phosphatases catalyze the hydrolysis of phosphate groups from many types of molecules, including nucleotides, proteins, and alkaloids. Three isozymes of alkaline phosphatases have been identified in humans, two of which are tissue-specific placental alkaline phosphatase (PLAP), intestinal alkaline...

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...

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...

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...