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
Designer receptors exclusively activated by designer drugs (DREADDs) are genetically engineered GPCRs that are activated by physiologically inert synthetic small molecules (designer drugs) but not their endogenous ligand. Read our DREADDs mini-review or for practical advice on using these ligands in the lab see Stability of Water-Soluble DREADD Ligands in Solution: A Technical Review and Clozapine N-Oxide (freebase) - a technical review on stability, solubility and use in the lab).