5-イソキノリンスルホン酸4-[(S)-2-[[(5-イソキノリニル)スルホニル]メチルアミノ]-3-オキソ-3-(4-フェニル-1-ピペラジニル)プロピル]フェニル

外観

白色～黄褐色, 結晶性粉末～粉末

溶解性

メタノール及びジメチルスルホキシドに溶ける。エタノールに溶ける。

用途

阻害剤。

化学的特性

Yellow Solid

使用

It is used as a potent and selective inhibitor of CaMKII. KN-62 has demonstrated potent and selective inhibition of Ca2+/calmodulin-dependent protein kinase II (CaMKII; Ki=0.9 ?M) which causes cells to arrest in the S phase. In HEK-293 cells expressing type III adenylyl cyclase (III-AC), 10 ?M of KN-62 blocked CaMKII phosphorylation of III-AC, and inhibited hormone-stimulated Ca2+ oscillations. Additionally, KN-62 is a potent non-competitive antagonist at the P2X7 receptor (IC50 = 15 nM).

一般的な説明

A cell-permeable, reversible, and selective inhibitor of CaM kinase II (K_i = 900 nM for rat brain CaM kinase II) that binds directly to the calmodulin binding site of the enzyme. Also inhibits the growth of K562 cells in a dose-dependent manner.

生物活性

Selective, cell-permeable inhibitor of CaM kinase II (IC 50 = 0.9 μ M). Binds directly to the calmodulin binding site of the enzyme. Potent non-competitive antagonist at the P2X 7 receptor (IC 50 = 15 nM). Also available as part of the Mixed Kinase Inhibitor Tocriset™ .