CMPD101（Cat No.:R032748）is a selective and potent inhibitor of G protein–coupled receptor kinase 2 (GRK2) and GRK3, enzymes that regulate GPCR desensitization and internalization. By blocking GRK-mediated phosphorylation, CMPD101 prolongs receptor signaling and alters downstream pathways, making it a useful tool in cardiovascular, neurological, and metabolic disease research. It has been applied to studies of β-adrenergic signaling, heart failure, and opioid receptor regulation. CMPD101’s specificity for GRK2/3 allows detailed exploration of receptor dynamics, providing insights into therapeutic strategies targeting GPCR regulation and signaling modulation.