autocamtide-2 related inhibitory peptide

Autocamtide-2 related inhibitory peptide (AIP) is a potent, highly selective, and non-phosphorylatable peptide inhibitor of Calcium/calmodulin-dependent protein kinase II (CaMKII). It is a synthetic analog of the CaMKII substrate autocamtide-2, where the phosphorylation site threonine is replaced by alanine (KKALRRQEAVDAL). AIP acts as a competitive inhibitor with respect to the protein substrate, with an IC50 in the nanomolar range. It is widely utilized as a pharmacological tool in preclinical research to investigate the role of CaMKII in various physiological and pathological processes, particularly in cardiovascular and neuroscience studies. In the context of heart failure with preserved ejection fraction (HFpEF), AIP has been used to demonstrate that CaMKII-dependent phosphorylation of NaV1.5 contributes to increased sodium influx and arrhythmic activity. While it is a critical reagent for target validation, it is primarily used as a research-use-only (RUO) tool and is not currently in clinical development as a therapeutic agent.

Other names

autocamtide-2-related inhibitory peptideautocamtide2-related inhibitory peptideautocamtide 2-related inhibitory peptideCaMKII inhibitory peptide