Chemical Name: 4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl] phenyl isoquinolinesulfonic acid ester
Biological ActivitySelective, cell-permeable inhibitor of CaM kinase II (IC50 = 0.9 μM). Binds directly to the calmodulin binding site of the enzyme. Potent non-competitive antagonist at the P2X7 receptor (IC50 = 15 nM).
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Effects of antagonists at the human recombinant P2X7 receptor.
Chessell et al.
Molecular and cellular pharmacology of a calcium/calmodulin-dependent protein kinase II (CaM kinase II) inhibitor, KN-62, and proposal of CaM kinase phosphorylation cascades.
Hidaka and Yokokura
KN-62, 1-[N-O-bis(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazine, a specific inhibitor of Ca2+/calmodulin-dependent protein kinase II.
Tokumitsu et al.
Citations for KN-62
The citations listed below are publications that use Tocris products. Selected citations for KN-62 include:
28 Citations: Showing 1 - 10
Peptide/Receptor Co-evolution Explains the Lipolytic Function of the Neuropeptide TLQP-21.
Authors: Sahu Et al.
Cell Rep 2019;28:2567
Secreted Amyloid Precursor Protein-Alpha Promotes Arc Protein Synthesis in Hippocampal Neurons.
Authors: Livingstone Et al.
Front Mol Neurosci 2019;12:198
Targeted Intron Retention and Excision for Rapid Gene Regulation in Response to Neuronal Activity.
Authors: Mauger Et al.
Neurophysiological mechanisms of bradykinin-evoked mucosal chloride secretion in guinea pig small intestine.
Authors: Qu Et al.
World J Gastrointest Pathophysiol 2016;7:150
Endocannabinoid dynamics gate spike-timing dependent depression and potentiation.
Authors: Cui Et al.
Mitochondrial Dysfunction, Depleted Purinergic Signaling, and Defective T Cell Vigilance and Immune Defense.
Authors: Ledderose Et al.
J Infect Dis 2016;213:456
Identification of a new pharmacological activity of the phenylpiperazine derivative naftopidil: tubulin-binding drug.
Authors: Ishii and Sugimura
Cell Rep 2015;8:42618
Rapid dispersion of SynGAP from synaptic spines triggers AMPA receptor insertion and spine enlargement during LTP.
Authors: Araki Et al.
PLoS One 2015;85:173
Biophysical Regulation of Chromatin Architecture Instills a Mechanical Memory in Mesenchymal Stem Cells.
Authors: Heo Et al.
Sci Rep 2015;5:16895
Modulation of P2X4/P2X7/Pannexin-1 sensitivity to extracellular ATP via iverm. induces a non-apoptotic and inflammatory form of cancer cell death.
Authors: Draganov Et al.
J Cell Sci 2015;5:16222
Synapse-specific compartmentalization of signaling cascades for LTP induction in CA3 interneurons.
Authors: Galván Et al.
Nucleotide receptors control IL-8/CXCL8 and MCP-1/CCL2 secretions as well as proliferation in human glioma cells.
Authors: Braganhol Et al.
Biochim Biophys Acta 2015;1852:120
The P2X7 receptor regulates cell survival, migration and invasion of pancreatic ductal adenocarcinoma cells.
Authors: Giannuzzo Et al.
J Chem Biol 2015;14:203
Glucagon Increases Beating Rate but Not Contractility in Rat Right Atrium. Comparison with isoprote.
Authors: Merino Et al.
Sci Rep 2015;10:e0132884
Heterosynaptic structural plasticity on local dendritic segments of hippocampal CA1 neurons.
Authors: Oh Et al.
Loss of long-term depression in the insular cortex after tail amputation in adult mice.
Authors: Liu and Zhuo
Mol Pain 2014;10:1
Role of salt-inducible kinase 1 in the activation of MEF2-dependent transcription by BDNF.
Authors: Finsterwald Et al.
PLoS One 2013;8:e54545
OX2R activation induces PKC-mediated ERK and CREB phosphorylation.
Authors: Guo and Feng
Exp Cell Res 2012;318:2004
Extracellular ATP exerts opposite effects on activated and regulatory CD4+ T cells via purinergic P2 receptor activation.
Authors: Trabanelli Et al.
J Immunol 2012;189:1303
Calcium/calmodulin-dependent protein kinase II mediates group I metabotropic glutamate receptor-dependent protein synthesis and long-term depression in rat hippocampus.
Authors: Mockett Et al.
J Neurosci 2011;31:7380
Calcium-dependent phosphorylation regulates neuronal stability and plasticity in a highly precise pacemaker nucleus.
Authors: George Et al.
J Neurophysiol 2011;106:319
Deactivation of L-type Ca current by inhibition controls LTP at excitatory synapses in the cerebellar nuclei.
Authors: Person and Raman
Intracellular redox state alters NMDA receptor response during aging through Ca2+/calmodulin-dependent protein kinase II.
Authors: Bodhinathan Et al.
J Neurosci 2010;30:1914
Human eosinophils recognize endogenous danger signal crystalline uric acid and produce proinflammatory cytokines mediated by autocrine ATP.
Authors: Kobayashi Et al.
J Immunol 2010;184:6350
Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.
Authors: Donnelly-Roberts Et al.
Br J Pharmacol 2009;157:1203
Kinase networks integrate profiles of N-MthD.-aspartate receptor-mediated gene expression in hippocampus.
Authors: Coba Et al.
J Biol Chem 2008;283:34101
Inhibition of the ATP-gated P2X7 receptor promotes axonal growth and branching in cultured hippocampal neurons.
Authors: Díaz-Hernández Et al.
Mol Cancer 2008;121:3717
Potentiation of TRPV3 channel function by unsaturated fatty acids.
Authors: Hu Et al.
J Cell Physiol 2006;208:201
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