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KN-62

Cat. No. M1928

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KN-62 Structure
Size Price Availability Quantity
5mg USD 80  USD80 In stock
10mg USD 150  USD150 In stock
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Biological Activity

KN-62 is a cell-permeable, reversible, and selective inhibitor of CaM kinase II (Ki = 900 nM for rat brain CaM kinase II). KN-62 is also a potent non-competitive antagonist at the P2X7 receptor (IC50 = 15 nM). KN-62 inhibits the growth of K562 cells in a dose-dependent manner. KN-62 could inhibit the Ca2+/CaM kinase II activity in vivo. However, KN-62 only slightly influenced PC secretion from type II cells stimulated by phorbol 12-myristate 13-acetate, terbutaline and ATP that are known to increase surfactant secretion via the protein kinase C and protein kinase A pathways. KN-62 affects the interaction between calmodulin and Ca2+/CaM kinase II following inhibition of this kinase activity by directly binding to the calmodulin binding site of the enzyme but does not affect the calmodulin-independent activity of already autophosphorylated (activated) enzyme.

Chemical Information
Molecular Weight 721.84
Formula C38H35N5O6S2
CAS Number 127191-97-3
Solubility (25°C) DMSO: ≥ 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Liu L. Biochem Mol Biol Int. Inhibition of lung surfactant secretion by KN-62, a specific inhibitor of the calcium- and calmodulin-dependent protein kinase II.

[2] Okazaki K, et al. J Pharmacol Exp Ther. KN-62, a specific Ca++/calmodulin-dependent protein kinase inhibitor, reversibly depresses the rate of beating of cultured fetal mouse cardiac myocytes.

[3] Tokumitsu H, et al. J Biol Chem. KN-62, 1-[N,O-bis(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazi ne, a specific inhibitor of Ca2+/calmodulin-dependent protein kinase II.

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Keywords: KN-62 supplier, CaMK, inhibitors, activators

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