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Category: Ion ChannelsarrowLigand-gated Ion ChannelsarrowP2X ReceptorsarrowAntagonists
Cat.No. Product Name
1277 KN-62
Price and Availability

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KN-62
Chemical Name: 4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo- 3-(4-phenyl-1-piperazinyl)propyl] phenyl isoquinolinesulfonic acid ester

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:

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M.Wt: 721.84
Formula: C38H35N5O6S2
Storage: Desiccate at -20°C
Solubility: Soluble to 100 mM in DMSO
Purity: >98%
CAS No: [127191-97-3]

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    References:

    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. 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. Chessell et al (1998) Effects of antagonists at the human recombinant P2X7 receptor. Br.J.Pharmacol. 124 1314.
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    Keywords: KN-62, Ligand-gated Ion Channels, Non-competitive P2X7 Antagonist, KN62, Tocris Bioscience
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