CCG258747 is a potent and selective inhibitor of GRK2, demonstrating an IC50 value of 18 nM and high selectivity against GRK1, GRK5, PKA, and ROCK1. This compound effectively prevents the internalization of the µ-opioid receptor (MOR) and inhibits the IgE-mediated anaphylaxis via the GRK2 and FcεRI signaling pathway, while also activating mast cells through MRGPRX2 and MRGPRB2. CCG258747 serves as a valuable tool for investigating disease mechanisms associated with GRK2 overexpression, including heart failure and opioid tolerance.
CCG258747 is a potent and selective inhibitor of GRK2, demonstrating an IC50 value of 18 nM and high selectivity against GRK1, GRK5, PKA, and ROCK1. This compound effectively prevents the internalization of the µ-opioid receptor (MOR) and inhibits the IgE-mediated anaphylaxis via the GRK2 and FcεRI signaling pathway, while also activating mast cells through MRGPRX2 and MRGPRB2. CCG258747 serves as a valuable tool for investigating disease mechanisms associated with GRK2 overexpression, including heart failure and opioid tolerance.
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