KN-62 is a potent and specific Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor with Ki of 0.9 μM.

CaMK II:0.9 μM(Ki), CaMK V:0.8 μM(Ki)

KN-62 administration in adult rats reduces the expression levels of brain-derived neurotrophic factor (BDNF) mRNA induced by epilepsy in the brain.

KN-62 inhibits the proliferation of K562 cells and blocks cell cycle progression. When administered at 10 μM to rat pancreatic islet cells, KN-62 inhibits insulin secretion stimulated by carbachol and potassium. Furthermore, KN-62 suppresses the phosphorylation of Ca2+/CaM kinase induced by A23187 in PC12 D cells.

Kinase assay: Total kinase activity of CaMKII, determined in a standard 2 min assay (100 μL), contained 35 mM HEPES, 10 mM MgCl2, 1 mM CaCl2, 10 μg of chicken gizzard myosin 20-kD light chain, 0.1 μM calmodulin, and 10 μM [γ-33]ATP at 30 °C. The kinase reaction is halted by adding 1 mL of 10% trichloroacetic acid.

For cell growth analysis, K562 cells are plated in a 3-cm dish with 5 mL of culture medium containing various concentration of KN-62. After two days in these condition cell numbers are counted. (Only for Reference)