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KN-62

Cat. No. 1277

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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

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.

Resources

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

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. PMID: 2155222.

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.

Chessell et al (1998) Effects of antagonists at the human recombinant P2X₇ receptor. Br.J.Pharmacol. 124 1314. PMID: 9720806.

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Calcium Binding Protein Modulators Calcium Signaling CaM Kinase

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Keywords: KN-62, supplier, CaM, kinase, II, inhibitors, Non-competitive, P2X7, antagonists, Calmodulin-Activated, calmodulin-dependent, Protein, Kinase, Kinases, Ca2+, Binding, modulators, Calcium, Signaling, Signalling, Receptors, Purinergic, purinoceptors