Autocamtide-2-related inhibitory peptide is a calmodulin-dependent protein kinase II (CaMKII) inhibitor (IC50 = 40 nM) that was designed based on the sequence around the autophosphorylation site (Thr286/Thr287) in the autoinhibitory domain of the protein kinase.[1],[2] It is nonphosphorylatable and selective for CaMKII over PKC, PKA and CaMKIV (IC50s > 10 μM).[1],[2] This compound is a useful tool for studying the physiological roles of CaMKII.[3]
References:
[1].Ishida, A., Kameshita, I., Okuno, S., et al.A novel highly specific and potent inhibitor of calmodulin-dependent protein kinase IIBiochem. Biophys. Res. Commun.212(3)806-812(1995).
[2].Ishida, A., and Fujisawa, H.Stabilization of calmodulin-dependent protein kinase II through autoinhibitory domainJ. Biol. Chem.270(5)2163-2170(1995).
[3].Takasawa, S., Ishida, A., Nata, K., et al.Requirement of calmodulin-dependent protein kinase II in cyclic ADP-ribose-mediated intracellular Ca2+ mobilizationJ. Biol. Chem.270(51)30257-30259(1995).