KN-62

Catalog # Availability Size / Price Qty
1277/1
Cat.No. 1277 - KN-62 | C38H35N5O6S2 | CAS No. 127191-97-3
1 Image
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%

Product Details
Citations (24)
Supplemental Products
Reviews

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
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Desiccate at -20°C
CAS No:
127191-97-3

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.

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Citations for KN-62

The citations listed below are publications that use Tocris products. Selected citations for KN-62 include:

24 Citations: Showing 1 - 10

  1. Neurophysiological mechanisms of bradykinin-evoked mucosal chloride secretion in guinea pig small intestine.
    Authors: Qu Et al.
    World J Gastrointest Pathophysiol  2016;7:150
  2. Endocannabinoid dynamics gate spike-timing dependent depression and potentiation.
    Authors: Cui Et al.
    Elife  2016;5:e13185
  3. Identification of a new pharmacological activity of the phenylpiperazine derivative naftopidil: tubulin-binding drug.
    Authors: Ishii and Sugimura
    Cell Rep  2015;8:42618
  4. 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
  5. Biophysical Regulation of Chromatin Architecture Instills a Mechanical Memory in Mesenchymal Stem Cells.
    Authors: Heo Et al.
    Sci Rep  2015;5:16895
  6. Modulation of P2X4/P2X7/Pannexin-1 sensitivity to extracellular ATP via Ivermectin induces a non-apoptotic and inflammatory form of cancer cell death.
    Authors: Draganov Et al.
    J Cell Sci  2015;5:16222
  7. Synapse-specific compartmentalization of signaling cascades for LTP induction in CA3 interneurons.
    Authors: Galván Et al.
    Neuroscience  2015;290:332
  8. 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
  9. The P2X7 receptor regulates cell survival, migration and invasion of pancreatic ductal adenocarcinoma cells.
    Authors: Giannuzzo Et al.
    J Chem Biol  2015;14:203
  10. Glucagon Increases Beating Rate but Not Contractility in Rat Right Atrium. Comparison with Isoproterenol.
    Authors: Merino Et al.
    Sci Rep  2015;10:e0132884
  11. Heterosynaptic structural plasticity on local dendritic segments of hippocampal CA1 neurons.
    Authors: Oh Et al.
    Neuron  2015;10:162
  12. Loss of long-term depression in the insular cortex after tail amputation in adult mice.
    Authors: Liu and Zhuo
    Mol Pain  2014;10:1
  13. Role of salt-inducible kinase 1 in the activation of MEF2-dependent transcription by BDNF.
    Authors: Finsterwald Et al.
    PLoS One  2013;8:e54545
  14. OX2R activation induces PKC-mediated ERK and CREB phosphorylation.
    Authors: Guo and Feng
    Exp Cell Res  2012;318:2004
  15. 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
  16. 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
  17. Calcium-dependent phosphorylation regulates neuronal stability and plasticity in a highly precise pacemaker nucleus.
    Authors: George Et al.
    J Neurophysiol  2011;106:319
  18. Deactivation of L-type Ca current by inhibition controls LTP at excitatory synapses in the cerebellar nuclei.
    Authors: Person and Raman
    Neuron  2010;66:550
  19. 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
  20. 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
  21. Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.
    Authors: Donnelly-Roberts Et al.
    Br J Pharmacol  2009;157:1203
  22. Kinase networks integrate profiles of N-methyl-D-aspartate receptor-mediated gene expression in hippocampus.
    Authors: Coba Et al.
    J Biol Chem  2008;283:34101
  23. 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
  24. Potentiation of TRPV3 channel function by unsaturated fatty acids.
    Authors: Hu Et al.
    J Cell Physiol  2006;208:201

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