Table 2.
Biochemical properties of best characterized CaMKII inhibitors.
| Inhibitor | Mechanism of action | Autonomousa kinase inhibition | Off-target effects |
|---|---|---|---|
| KN-93, KN-62 | Allosteric, CaM-competitive | No | CaMKI, CaMKIV, ion channels |
| AC3I/AIP | Peptide substrate-competitive | Yes | PKD-1 in cells |
| CaMKIIN | Peptide substrate/regulatory domain-competitive | Yes | None identified |
| Small molecule inhibitors (Scios 15b, SMP-114, Bosutinib) | ATP-competitive | Yes | Inhibit other ser/thr and tyr kinases in vivo |
a
Autonomy is based on Thr287 autophosphorylation but results are likely the same for autonomy generated by regulatory domain methionine oxidation or by GlcNAcylation.