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作用于成年大鼠,降低其脑中癫痫诱导的脑源性神经生长因子mRNA的表达水平.

KN-62抑制K562细胞的增殖,并阻断细胞周期进程。10 μM KN-62作用于大鼠胰岛细胞,抑制卡巴胆碱和钾刺激的胰岛素分泌。KN-62抑制PC12 D细胞中A23187诱导的Ca2+/CaM激酶磷酸化作用。

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)