Product overview

  • Name
    KN-62
  • Short description
    Selective CaM kinase II inhibitor. P2X7 receptor antagonist.
  • Biological description
    Selective CaM kinase II inhibitor (IC50 = 500 nM). Also potent, non-competitive P2X7 receptor antagonist (IC50 = 15 nM). Also inhibits GSK3β, PRAK and MAPKAP-K2. Cell-permeable, potential anticancer actions through suppression of HIF-1α.
  • Biological action
    Inhibitor
  • Purity
    >98%
  • Our products in action

Properties

  • Chemical name
    4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl] phenyl isoquinolinesulfonic acid ester
  • Molecular Weight
    721.84
  • Chemical structure
    KN-62  [127191-97-3]
  • Molecular Formula
    C38H35N5O6S2
  • CAS Number
    127191-97-3
  • PubChem identifier
    5312126
  • SMILES
    CN([C@@H](CC1=CC=C(C=C1)OS(=O)(=O)C2=CC=CC3=C2C=CN=C3)C(=O)N4CCN(CC4)C5=CC=CC=C5)S(=O)(=O)C6=CC=CC7=C6C=CN=C7

Storing and Using Your Product

  • Storage instructions
    -20°C (desiccate)
  • Solubility overview
    soluble in DMSO (100mM)

References for KN-62

  • Specificity and mechanism of action of some commonly used protein kinase inhibitors.

    Davies SP et al (2000) Biochem J 351(Pt 1) : 95-105.
    PubMedID: 10998351
  • Effects of antagonists at the human recombinant P2X7 receptor.

    Chessell IP et al (1998) Br J Pharmacol 124(6) : 1314-20.
    PubMedID: 9720806
  • KN-62, 1-[N,O-bis(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazi ne, a specific inhibitor of Ca2+/calmodulin-dependent protein kinase II.

    Tokumitsu H et al (1990) J Biol Chem 265(8) : 4315-20.
    PubMedID: 2155222

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