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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 yes
  • Bioassay Tested
    • 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
    1. 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.
      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.
    References - Scientific background
    1. Chessell, I.P. et al. (1998) Br. J. Pharmacol.124, 1314.
    2. Min, J.W. et al. (2017) Oncotarget 8, 25513.
    3. Bhattacharya, A. et al. (2013) Br. J. Pharmacol. 170, 624.
    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
    Last update: 12/08/2021

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

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    For research purposes only, not for human use
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