Impaired trafficking of cholesterol to or from the endoplasmic reticulum (ER) has been implicated in many disease states including Neimann-Pick disease type C (NPC), Alzheimers disease and atherosclerosis. U-18666A is a cell permeable drug that inhibits cholesterol trafficking. It inhibits cholesterol transport from...

Phosphoinositide 3-kinase gamma (PI3Kgamma), expressed primarily in hematopoietic cells, plays several important roles in immunity. CAY10505 is a potent inhibitor of PI3K, selectively inhibiting the gamma isoform (IC50 = 30 nM) better than the alpha, beta, and delta isoforms (IC50 = 0.94, 20, and 20 µM,...

The peroxisome proliferator-activated receptors (PPARs) alpha, gamma, and delta are ligand-activated transcription factors that play a key role in lipid homeostasis. Activation of PPARalpha results in increased clearance of triglyceride (TG) rich very low-density lipoprotein (VLDL) via a reduction in plasma levels...

GPR40 (free fatty acid receptor 1, FFAR1) is a G protein-coupled receptor (GPCR) that is activated by saturated and unsaturated long chain fatty acids. It is thought to play a role in the potentiation of insulin secretion by fatty acids in a glucose-sensitive manner. GW 1100 is a selective antagonist of...