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Submit ReviewKN-62
Description: Non-competitive P2X7 antagonist
Chemical Name: 4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl] phenyl isoquinolinesulfonic acid ester
Purity: ≥98% (HPLC)
Biological Activity for KN-62
KN-62 is a 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 for KN-62
| M. Wt | 721.84 |
| Formula | C38H35N5O6S2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 127191-97-3 |
| PubChem ID | 5312126 |
| InChI Key | RJVLFQBBRSMWHX-DHUJRADRSA-N |
| Smiles | O=S(C1=CC=CC2=C1C=CN=C2)(N(C)[C@H](C(N4CCN(C7=CC=CC=C7)CC4)=O)CC3=CC=C(OS(C5=CC=CC6=C5C=CN=C6)(=O)=O)C=C3)=O |
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.
Solubility Data for KN-62
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 72.18 | 100 |
Preparing Stock Solutions for KN-62
The following data is based on the product molecular weight 721.84. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
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Product Datasheets for KN-62
References for KN-62
References are publications that support the biological activity of the product.
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, 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, 1277, Tocris Bioscience
28 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
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
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
Ishii and Sugimura (2015) Identification of a new pharmacological activity of the phenylpiperazine derivative naftopidil: tubulin-binding drug. Cell Rep 8 42618 PMID: 25584077
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
Galván et al (2015) Synapse-specific compartmentalization of signaling cascades for LTP induction in CA3 interneurons. Neuroscience 290 332 PMID: 25637803
Braganhol et al (2015) Nucleotide receptors control IL-8/CXCL8 and MCP-1/CCL2 secretions as well as proliferation in human glioma cells. Biochim Biophys Acta 1852 120 PMID: 25445541
Livingstone et al (2019) Secreted Amyloid Precursor Protein-Alpha Promotes Arc Protein Synthesis in Hippocampal Neurons. Front Mol Neurosci 12 198 PMID: 31474829
Sahu et al (2019) Peptide/Receptor Co-evolution Explains the Lipolytic Function of the Neuropeptide TLQP-21. Cell Rep 28 2567 PMID: 31484069
Cui et al (2016) Endocannabinoid dynamics gate spike-timing dependent depression and potentiation. Elife 5 e13185 PMID: 26920222
Qu et al (2016) Neurophysiological mechanisms of bradykinin-evoked mucosal chloride secretion in guinea pig small intestine. World J Gastrointest Pathophysiol 7 150 PMID: 26909238
Finsterwald et al (2013) Role of salt-inducible kinase 1 in the activation of MEF2-dependent transcription by BDNF. PLoS One 8 e54545 PMID: 23349925
Bodhinathan et al (2010) Intracellular redox state alters NMDA receptor response during aging through Ca2+/calmodulin-dependent protein kinase II. J Neurosci 30 1914 PMID: 20130200
Liu and Zhuo (2014) Loss of long-term depression in the insular cortex after tail amputation in adult mice. Mol Pain 10 1 PMID: 24398034
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
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
Mauger et al (2016) Targeted Intron Retention and Excision for Rapid Gene Regulation in Response to Neuronal Activity. Neuron 92 1266 PMID: 28009274
Ledderose et al (2016) Mitochondrial Dysfunction, Depleted Purinergic Signaling, and Defective T Cell Vigilance and Immune Defense. J Infect Dis 213 456 PMID: 26150546
Draganov et al (2015) Modulation of P2X4/P2X7/Pannexin-1 sensitivity to extracellular ATP via iverm. 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 isoprote. Sci Rep 10 e0132884 PMID: 26222156
Hu et al (2006) Potentiation of TRPV3 channel function by unsaturated fatty acids. J Cell Physiol 208 201 PMID: 16557504
Coba et al (2008) Kinase networks integrate profiles of N-MthD.-aspartate receptor-mediated gene expression in hippocampus. J Biol Chem 283 34101 PMID: 18815127
Do you know of a great paper that uses KN-62 from Tocris? Please let us know.
Reviews for KN-62
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KN62 treatment.
By
Xiaoyu Zhang on 02/07/2024
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: neuron cells
Mouse neuron culture treated with 10nM KN62. MAP staining showed after treatment.
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P2X and P2Y Receptors Scientific Review
Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.