10 products were found matching "Cay10010245-100"!

Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. Olomoucine is a cdk inhibitor that acts by competing for the ATP binding site of the kinase. This purine derivative is an inhibitor for CDC2/cyclin B (IC50 = 7 µM), Cdk2/cyclin A (IC50...

AICAR is an activator of AMP-activated protein kinase (AMPK). It increases AMPK kinase activity in isolated hepatocytes (EC50 = ~500 µM) and reduces HMG-CoA reductase activity and fatty acid and sterol synthesis in these cells. AICAR (0.5 mM) inhibits insulin-stimulated glucose uptake to 62% of control cells and...

Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli including insulin, growth factors, cell specification factors, and cell adhesion. SB-216763 is a potent and selective cell permeable ATP-competitive inhibitor of GSK3alpha with an IC50...

Advanced glycation end products (AGEs) are compounds formed by non-enzymatic chemical reactions following the bonding of sugars to proteins or lipids during diabetes, uremia, aging, rheumatic arthritis, and other conditions. A receptor for the AGEs (RAGE) binds certain members of this class to initiate cell...

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...

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....

Defining the mechanisms responsible for alterations in cell cycle progression is crucial to understanding many human diseases, most notably cancer. Cell proliferation assays have been widely used to assess cell cycle regulatory factors such as growth factors, cytokines, mitogens, and drugs. Cayman's XTT cell...

Apigenin is a flavonoid compound found in many fruits and vegetables that selectively inhibits casein kinase 2 (CK2). Apigenin inhibits CK2 activity in the renal cortex with an IC50 value of 30 µM to improve renal function in a rat model of glomerulonephritis. CK2 inhibition by 20 µM apigenin decreases the...

LFM-A13 is an inhibitor of Bruton's tyrosine kinase (BTK, IC50 = 2.5 µM). It is selective for BTK over JAK1, JAK3, IRK, EGFR, and HCK (IC50s = >278 µM for all), as well as a panel of seven serine/threonine and 10 tyrosine kinases as well as one lipid kinase (IC50s = >200-500 µM), but does inhibit polo-like kinase 3...

Peroxisome proliferator-activated receptor gamma (PPARgamma) is a central regulator of adipocyte differentiation and is the principle target of the thiazolidinedione (TZD) class of antidiabetic drugs. Harmine is a beta-carboline alkaloid that was first isolated from seeds of Peganum harmala (Syrian rue) and...