KN-62 is a selective, cell permeable inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII; IC50 = 900 nM). It does not affect the activity of several other kinases when tested at 10 μM. KN-62 also acts as a non-competitive antagonist of the purinergic receptor P2RX7 (IC50 = 15 nM).