KN-62 是一种选择性的、可逆的钙调蛋白依赖性蛋白激酶 II (CaMK-II) 抑制剂，直接与 CaMK-II 酶的钙调蛋白结合位点结合，对大鼠脑 CaMK-II 的IC50值为 0.9 μM。它是非竞争性的P2X7受体拮抗剂，IC50约为 15 nM。

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

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)

127191-97-3

C38H35N5O6S2

721.85

DMSO:72.2 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years