Chemical Properties
Yellow Solid
Uses
selectively inhibits rat brain Ca2+/cadmodulin-dependent protein kinase II,
Uses
A specific inhibitor of Ca2+/Calmodulin-dependent protein kinase II
Uses
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).
Definition
ChEBI: 5-isoquinolinesulfonic acid [4-[(2S)-2-[5-isoquinolinylsulfonyl(methyl)amino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl]phenyl] ester is a member of piperazines.
General Description
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.
Biological Activity
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™ .
Biochem/physiol Actions
Selectively inhibits rat brain Ca2+/calmodulin-dependent protein kinase II.
storage
-20°C (desiccate)
