Catalog Number: 1278
Chemical Name: N-[2-[[[3-(4-Chlorophenyl)-2-propenyl]methylamino]methyl]phenyl]-N-(2-hydroxyethyl)-4-methoxybenzenesulphonamide
Biological Activity
Potent, cell permeable inhibitor of CaM kinase II (IC50 = 0.37 μM). Also a direct extracellular open channel blocker of voltage-gated potassium channels (IC50 = 307 nM for KV1.5) and abolishes IKr in ventricular myocytes (IC50 = 102.6 nM) independently of CaM kinase II inhibition.

Water soluble form and Negative Control also available.

Technical Data
  • M.Wt:
    501.04
  • Formula:
    C26H29ClN2O4S
  • Solubility:
    Soluble to 100 mM in DMSO with gentle warming
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    139298-40-1
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.
Additional Information
Other Product-Specific Information:
Background References
  1. Calcium/calmodulin-dependent phosphorylation and activation of human Cdc25-C at the G2/M phase transition in HeLa cells.
    Patel et al.
    J.Biol.Chem., 1999;274:7958
  2. KN-93 (2-[N-(2-Hydroxyethyl)]-N-(4-methoxybenzenesulfonyl)]-amino-N-(4-chlorocinnamyl)-N-methylbenzylamine), a calcium/calmodulin-dependent protein kinase II inhibitor, is a direct extracellular blocker of voltage-gated
    Rezazadeh et al.
    J.Pharmacol.Exp.Ther., 2006;317:292
  3. The newly synthesized selective Ca2+/calmodulin dependent protein kinase II inhibitor KN-93 reduces dopamine content in PC12h cells.
    Sumi et al.
    Biochem.Biophys.Res.Comm., 1991;181:968
  4. KN-93 inhibits IKr in mammalian cardiomyocytes.
    Hegyi et al.
    J.Mol.Cell.Cardiol., 2015;89:173
Citations:

The citations listed below are publications that use Tocris products. Selected citations for KN 93 include:

17 Citations: Showing 1 - 10
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  1. Ca(2+)/calmodulin-dependent protein kinase II interacts with group I metabotropic glutamate and facilitates receptor endocytosis and ERK1/2 signaling: role of β-amyloid.
    Authors: Raka Et al.
    Mol Brain 2015;8:21
  2. 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.
    Apoptosis 2015;5:16222
  3. Evolutionary and functional perspectives on signaling from neuronal surface to nucleus.
    Authors: Cohen Et al.
    PLoS One 2015;460:88
  4. Calcium signals inhibition sensitizes ovarian carcinoma cells to anti-Bcl-xL strategies through Mcl-1 down-regulation.
    Authors: Bonnefond Et al.
    Oncoscience 2015;20:535
  5. Melanoma brain colonization involves the emergence of a brain-adaptive phenotype.
    Authors: Nygaard Et al.
    Biochem Biophys Res Commun 2015;1:82
  6. Activation of Phosphatidylinositol-Linked Dopamine Receptors Induces a Facilitation of Glutamate-Mediated Synaptic Transmission in the Lateral Entorhinal Cortex.
    Authors: Glovaci and Chapman
    PLoS One 2015;10:e0131948
  7. SynGAP regulates protein synthesis and homeostatic synaptic plasticity in developing cortical networks.
    Authors: Wang Et al.
    PLoS One 2014;8:e83941
  8. Oestrogen upregulates the sarcoplasmic reticulum Ca(2+) ATPase pump in coronary arteries.
    Authors: Hill and Muldrew
    Clin Exp Pharmacol Physiol 2014;41:430
  9. CaMKII phosphorylation of neuroligin-1 regulates excitatory synapses.
    Authors: Bemben Et al.
    Nat Neurosci 2014;17:56
  10. Acute simvastatin inhibits K ATP channels of porcine coronary artery myocytes.
    Authors: Seto Et al.
    Biochem Pharmacol 2013;8:e66404
  11. AMP-activated protein kinase as regulator of P2Y(6) receptor-induced insulin secretion in mouse pancreatic β-cells.
    Authors: Balasubramanian Et al.
    J Neurosci 2013;85:991
  12. Increased neuronal activity fragments the Golgi complex.
    Authors: Thayer Et al.
    Proc Natl Acad Sci U S A 2013;110:1482
  13. Interaction between αCaMKII and GluN2B controls ERK-dependent plasticity.
    Authors: Gaamouch Et al.
    J Neurosci 2012;32:10767
  14. 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
  15. Hyperdopaminergic tone erodes prefrontal long-term potential via a D2 receptor-operated protein phosphatase gate.
    Authors: Xu Et al.
    MBio 2009;29:14086
  16. Calmodulin kinase II initiates arrhythmogenicity during metabolic acidification in murine hearts.
    Authors: Pedersen Et al.
    Acta Physiol (Oxf) 2009;197:13
  17. Synapse-specific adaptations to inactivity in hippocampal circuits achieve homeostatic gain control while dampening network reverberation.
    Authors: Kim and Tsien
    Neuron 2008;58:925
Expand to show all 17 Citations
Tocris Small Molecules
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KN 93 phosphate

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