KN-62

4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl] phenyl isoquinolinesulfonic acid ester
An Antagonist of P2X7 Receptors and Inhibitor of CaM kinase II
Cat #: K-120
Alternative Name 4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl] phenyl isoquinolinesulfonic acid ester
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 721.85
    Purity: >98%
    Effective concentration 20 nM – 20 µM.
    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.
    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.
    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.
      • 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.

    Target P2X7 receptor, CaM kinase type II
    Last update: 28/05/2019

    KN-62 (#K-120) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use