CAS: 1813527-81-9

CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, 5 and 1, respectively.

CCG215022 is a small-molecule inhibitor of GSK3β. It has been shown to induce death in cancer cells that are resistant to other chemotherapies, such as rhabdomyosarcoma, and is effective at inhibiting the growth of various cancers, including breast cancer. CCG215022 binds to the ATP-binding pocket of GSK3β and inhibits its activity by preventing the formation of phosphorylated peptides on kinase domain. The inhibition of this enzyme leads to increased contractility and increased hydrophobicity, which may be responsible for its effect on cancer cells. CCG215022 also has an excellent safety profile in pediatric patients and is effective at doses that are lower than those required for adults.

CCG215022