- Chessell, I.P. et al. (1998) Br. J. Pharmacol.124, 1314.
- Alomone Labs KN-62 inhibits human P2X7 receptors expressed in HEK-293 cells.Dose-response curve of hP2X7 inhibition by KN-62 (#K-120). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of KN-62, and stimulated with 80 µM BzATP. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was calculated at 2.6 µM.
KN-62 is a potent and non-competitive antagonist of purinergic P2X7 receptors. In addition, KN-62 acts as a selective cell permeable inhibitor of Ca2+/calmodulin-dependent kinase type II (CaM kinase II)1. KN-62 inhibits Bz-ATP-induced currents in HEK–human P2X7 cells and CaM kinase II with IC50 value of 25 nM and 1 µM respectively1.
CaM kinase II is very important to synaptogenesis and plasticity during brain development2. The P2X receptors are a family of ion channels that gated by ATP, a ligand that mediates wide critical physiologic functions. P2X7 receptor is responsible for mediating the release of proinflammatory cytokines in inflammatory/immune conditions and pain3.
KN-62 (#K-120) is a highly pure, synthetic, and biologically active compound.