KN 93

Cat. No. 1278

KN 93 C26H29ClN2O4S [139298-40-1]

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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 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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Hegyi et al (2015) KN-93 inhibits IKr in mammalian cardiomyocytes. J.Mol.Cell.Cardiol. 89 173. PMID: 26463508.

Rezazadeh et al (2006) 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 potassium channels. J.Pharmacol.Exp.Ther. 317 292. PMID: 16368898.

Patel et al (1999) Calcium/calmodulin-dependent phosphorylation and activation of human Cdc25-C at the G2/M phase transition in HeLa cells. J.Biol.Chem. 274 7958. PMID: 10075693.

Sumi et al (1991) The newly synthesized selective Ca2+/calmodulin dependent protein kinase II inhibitor KN-93 reduces dopamine content in PC12h cells. Biochem.Biophys.Res.Comm. 181 968. PMID: 1662507.

If you know of a relevant reference for KN 93 please let us know.

Citations are publications that use Tocris products. Selected citations for KN 93 include:

Bonnefond et al (2015) Calcium signals inhibition sensitizes ovarian carcinoma cells to anti-Bcl-xL strategies through Mcl-1 down-regulation. Oncoscience 20 535. PMID: 25627260.

Cohen et al (2015) Evolutionary and functional perspectives on signaling from neuronal surface to nucleus. PLoS One 460 88. PMID: 25998737.

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. Apoptosis 5 16222. PMID: 26552848.

Glovaci and Chapman (2015) Activation of Phosphatidylinositol-Linked Dopamine Receptors Induces a Facilitation of Glutamate-Mediated Synaptic Transmission in the Lateral Entorhinal Cortex. PLoS One 10 e0131948. PMID: 26133167.

Nygaard et al (2015) Melanoma brain colonization involves the emergence of a brain-adaptive phenotype. Biochem Biophys Res Commun 1 82. PMID: 25593989.

Raka et al (2015) 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. Mol Brain 8 21. PMID: 25885040.

Bemben et al (2014) CaMKII phosphorylation of neuroligin-1 regulates excitatory synapses. Nat Neurosci 17 56. PMID: 24336150.

Hill and Muldrew (2014) Oestrogen upregulates the sarcoplasmic reticulum Ca(2+) ATPase pump in coronary arteries. Clin Exp Pharmacol Physiol 41 430. PMID: 24684418.

Wang et al (2014) SynGAP regulates protein synthesis and homeostatic synaptic plasticity in developing cortical networks. PLoS One 8 e83941. PMID: 24391850.

Balasubramanian et al (2013) AMP-activated protein kinase as regulator of P2Y(6) receptor-induced insulin secretion in mouse pancreatic β-cells. J Neurosci 85 991. PMID: 23333427.

Seto et al (2013) Acute simvastatin inhibits K ATP channels of porcine coronary artery myocytes. Biochem Pharmacol 8 e66404. PMID: 23799098.

Thayer et al (2013) Increased neuronal activity fragments the Golgi complex. Proc Natl Acad Sci U S A 110 1482. PMID: 23297202.

Gaamouch et al (2012) Interaction between αCaMKII and GluN2B controls ERK-dependent plasticity. J Neurosci 32 10767. PMID: 22855824.

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.

Pedersen et al (2009) Calmodulin kinase II initiates arrhythmogenicity during metabolic acidification in murine hearts. Acta Physiol (Oxf) 197 13. PMID: 19416122.

Xu et al (2009) Hyperdopaminergic tone erodes prefrontal long-term potential via a D2 receptor-operated protein phosphatase gate. MBio 29 14086. PMID: 19906957.

Kim and Tsien (2008) Synapse-specific adaptations to inactivity in hippocampal circuits achieve homeostatic gain control while dampening network reverberation. Neuron 58 925. PMID: 18579082.

Do you know of a great paper that uses KN 93 from Tocris? If so please let us know.show all ▼show less ▲

View Related Products by Product Action

Keywords: KN 93, supplier, K+, channel, blockers, KV, inhibitors, inhibits, Potassium, Channels, voltage-gated, voltage-dependent, CaM, Kinase, II, kinases, Calmodulin-Activated, calmodulin-dependent, Protein, Ca2+, Binding, modulators, Calcium, Signaling, Signalling, hERG, Human, Ether-A-Go-Go, Gene, KCNQ, KN93, IKr, Tocris Bioscience, Calmodulin-Dependent Kinase Inhibitor products

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