KN-62

Pricing Availability Delivery Time Qty
Cat.No. 1277 - KN-62 | C38H35N5O6S2 | CAS No. 127191-97-3
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)
Datasheet
Citations (15)
Literature

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

M. Wt 721.84
Formula C38H35N5O6S2
Storage Desiccate 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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 72.18 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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: 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

15 Citations for KN-62

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

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

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


Do you know of a great paper that uses KN-62 from Tocris? If so please let us know.

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