Overview
Alternative Name 4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl] phenyl isoquinolinesulfonic acid ester
Lyophilized Powder yes
Source Synthetic
MW: 721.85
Purity: >98%
Effective concentration 20 nM – 20 µM.
Structure
Chemical name [4-[(2S)-2-[isoquinolin-5-ylsulfonyl(methyl)amino]-3-oxo-3-(4-phenylpiperazin-1-yl)propyl]phenyl] isoquinoline-5-sulfonate.
Molecular formula C38H35N5O6S2.
CAS No.: 127191-97-3
PubChem CID 5312126
Activity KN-62 is a potent non-competitive antagonist of the purinergic P2X7 receptors, shown to inhibit Bz-ATP-induced currents in HEK–hP2X7 cells with IC50 of 25 nM. KN-62 is also a selective, cell permeable inhibitor of Ca2+/calmodulin-dependent kinase type II, with IC50 of approximately 1 µM1.
References-Activity
- Chessell, I.P. et al. (1998) Br. J. Pharmacol.124, 1314.
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Solubility Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).
Storage of solutions -20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
Our bioassay
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.
Scientific background
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.
Target P2X7 receptor, CaM kinase type II
Lyophilized Powder
For research purposes only, not for human use
Last Update: 07/05/2024
Specifications
Citations
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