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).
|Storage||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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 721.84. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.39 mL||6.93 mL||13.85 mL|
|5 mM||0.28 mL||1.39 mL||2.77 mL|
|10 mM||0.14 mL||0.69 mL||1.39 mL|
|50 mM||0.03 mL||0.14 mL||0.28 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
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 KN-62, please let us know.
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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, P2X, Receptors, Calcium, Binding, Protein, CaM, Kinase, P2X, Receptors, Tocris Bioscience
15 Citations for KN-62
Citations are publications that use Tocris products. Selected citations for KN-62 include:
Heo et al (2015) Biophysical Regulation of Chromatin Architecture Instills a Mechanical Memory in Mesenchymal Stem Cells. Sci Rep 5 16895 PMID: 26592929
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
Oh et al (2015) Heterosynaptic structural plasticity on local dendritic segments of hippocampal CA1 neurons. Neuron 10 162 PMID: 25558061
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
Merino et al (2015) Glucagon Increases Beating Rate but Not Contractility in Rat Right Atrium. Comparison with Isoproterenol. Sci Rep 10 e0132884 PMID: 26222156
Ishii and Sugimura (2015) Identification of a new pharmacological activity of the phenylpiperazine derivative naftopidil: tubulin-binding drug. Cell Rep 8 42618 PMID: 25584077
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
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
George et al (2011) Calcium-dependent phosphorylation regulates neuronal stability and plasticity in a highly precise pacemaker nucleus. J Neurophysiol 106 319 PMID: 21525377
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
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
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
Do you know of a great paper that uses KN-62 from Tocris? If so please let us know.
Literature in this Area
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.