Cat. No. 1277

KN-62 C38H35N5O6S2 [127191-97-3]

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Chemical Name: 4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl] phenyl isoquinolinesulfonic acid ester

Biological Activity

Selective, 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).

Technical Data

Soluble to 100 mM in DMSO
>98 %
Desiccate at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Chessell et al (1998) Effects of antagonists at the human recombinant P2X7 receptor. Br.J.Pharmacol. 124 1314. PMID: 9720806.

Hidaka and Yokokura (1996) 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. Adv.Pharmacol. 36 193. PMID: 8783561.

Tokumitsu et al (1990) KN-62, 1-[N-O-bis(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazine, a specific inhibitor of Ca2+/calmodulin-dependent protein kinase II. J.Biol.Chem. 265 4315. PMID: 2155222.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for KN-62 include:

Araki et al (2015) Rapid dispersion of SynGAP from synaptic spines triggers AMPA receptor insertion and spine enlargement during LTP. PLoS One 85 173. PMID: 25569349.

Draganov et al (2015) Modulation of P2X4/P2X7/Pannexin-1 sensitivity to extracellular ATP via Ivermectin induces a non-apoptotic and inflammatory form of cancer cell death. J Cell Sci 5 16222. PMID: 26552848.

Giannuzzo et al (2015) The P2X7 receptor regulates cell survival, migration and invasion of pancreatic ductal adenocarcinoma cells. J Chem Biol 14 203. PMID: 26607222.

Heo et al (2015) Biophysical Regulation of Chromatin Architecture Instills a Mechanical Memory in Mesenchymal Stem Cells. Sci Rep 5 16895. PMID: 26592929.

Ishii and Sugimura (2015) Identification of a new pharmacological activity of the phenylpiperazine derivative naftopidil: tubulin-binding drug. Cell Rep 8 42618. PMID: 25584077.

Merino et al (2015) Glucagon Increases Beating Rate but Not Contractility in Rat Right Atrium. Comparison with Isoproterenol. Sci Rep 10 e0132884. PMID: 26222156.

Oh et al (2015) Heterosynaptic structural plasticity on local dendritic segments of hippocampal CA1 neurons. Neuron 10 162. PMID: 25558061.

Guo and Feng (2012) OX2R activation induces PKC-mediated ERK and CREB phosphorylation. Exp Cell Res 318 2004. PMID: 22652455.

Trabanelli et al (2012) Extracellular ATP exerts opposite effects on activated and regulatory CD4+ T cells via purinergic P2 receptor activation. J Immunol 189 1303. PMID: 22753942.

George et al (2011) Calcium-dependent phosphorylation regulates neuronal stability and plasticity in a highly precise pacemaker nucleus. J Neurophysiol 106 319. PMID: 21525377.

Mockett et al (2011) Calcium/calmodulin-dependent protein kinase II mediates group I metabotropic glutamate receptor-dependent protein synthesis and long-term depression in rat hippocampus. J Neurosci 31 7380. PMID: 21593322.

Kobayashi et al (2010) Human eosinophils recognize endogenous danger signal crystalline uric acid and produce proinflammatory cytokines mediated by autocrine ATP. J Immunol 184 6350. PMID: 20483787.

Person and Raman (2010) Deactivation of L-type Ca current by inhibition controls LTP at excitatory synapses in the cerebellar nuclei. Neuron 66 550. PMID: 20510859.

Donnelly-Roberts et al (2009) Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors. Br J Pharmacol 157 1203. PMID: 19558545.

Díaz-Hernández et al (2008) Inhibition of the ATP-gated P2X7 receptor promotes axonal growth and branching in cultured hippocampal neurons. Mol Cancer 121 3717. PMID: 18987356.

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View Related Products by Product Action

Keywords: KN-62, supplier, CaM, kinase, II, inhibitors, inhibits, Non-competitive, P2X7, antagonists, Calmodulin-Activated, calmodulin-dependent, Protein, Kinase, Kinases, Ca2+, Binding, modulators, Calcium, Signaling, Signalling, Receptors, Purinergic, purinoceptors, Tocris Bioscience, Purinergic (P2X) Receptor Antagonist products

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