Novel tool for studying GPCR desensitization
An exclusive from Hello Bio, Cmpd101 is a novel, potent, selective G-protein coupled receptor kinase 2 and 3 inhibitor (IC50 values are 35, 290 nM and 125 µM at GRK2, GRK3 and GRK5 respectively). Selective over other kinases. Can be used to study roles of GRK2/3 in GPCR desensitization...Read more
G protein coupled receptors
G-protein-coupled receptors (also known as GPCRs, transmembrane receptors, or 7-TM receptors), are integral membrane proteins that contain seven membrane-spanning domains (helices). They are coupled to heterotrimeric G proteins on the intracellular side of the cell membrane. Ligand binding causes a conformational change in the GPCR, that is then transmitted to the G protein, activating a signal transduction pathway. GPCRs include acetycholine muscarinic, adenosine, GABAB, and histamine receptors, and the metabotropic glutamate receptors (Group I, Group II and Group III). Researchers can save up to 50% on GPCR receptor agonists, antagonists and allosteric modulators from Hello Bio - they are up to half the price of other suppliers.