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KN-62CaM kinase II inhibitor

KN-62

Catalog No. A8180
Size Price Stock Qty
10mM (in 1mL DMSO) $125.00 In stock
Evaluation Sample $28.00 In stock
1mg $50.00 In stock
5mg $70.00 In stock
25mg $240.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

KN-62

Related Biological Data

KN-62

Related Biological Data

KN-62

Biological Activity

Description KN-62 is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.9 μM.
Targets Calmodulin protein kinase II          
IC50 0.9 μM          

Protocol

Kinase experiment [1]:

Kinase assay

Total kinase activity of CaMKII, determined in a standard 2 min assay (100 μL), contained 35 mM HEPES, 10 mM MgCl2, 1 mM CaCl2, 10 μg of chicken gizzard myosin 20-kD light chain, 0.1 μM calmodulin and 10 μM [γ-33]ATP at 30 °C. The kinase reaction was halted by adding 1 mL of 10% trichloroacetic acid.

Cell experiment [2]:

Cell lines

K562 cells

Preparation method

The solubility of this compound in DMSO is > 36.1 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

1, 2, 5 or 10 μM; 24 or 48 hrs

Applications

KN-62 inhibited the cell growth of K562 cells in a dose-dependent manner. Two days after the treatment of 10 μM KN-62, 63% K562 cells were inhibited. Flow cytometric analysis showed that KN-62 (10 μM, 24 hrs) caused an accumulation of K562 cells in S phase. Immunoblotting studies indicated that CaMKII was inhibited in these K562 cells.

References:

[1]. Tokumitsu H, Chijiwa T, Hagiwara M, Mizutani A, Terasawa M, Hidaka H. 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. J Biol Chem. 1990 Mar 15;265(8):4315-20.

[2]. Minami H, Inoue S, Hidaka H. The effect of KN-62, Ca2+/calmodulin dependent protein kinase II inhibitor on cell cycle. Biochem Biophys Res Commun. 1994 Feb 28;199(1):241-8.

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Chemical Properties

Cas No. 127191-97-3 SDF Download SDF
Chemical Name [4-[(2S)-2-[isoquinolin-5-ylsulfonyl(methyl)amino]-3-oxo-3-(4-phenylpiperazin-1-yl)propyl]phenyl] isoquinoline-5-sulfonate
Canonical SMILES CN(C(CC1=CC=C(C=C1)OS(=O)(=O)C2=CC=CC3=C2C=CN=C3)C(=O)N4CCN(CC4)C5=CC=CC=C5)S(=O)(=O)C6=CC=CC7=C6C=CN=C7
Formula C38H35N5O6S2 M.Wt 721.9
Solubility >36.1mg/mL in DMSO Storage Desiccate at -20°C
General tips N/A
Shipping Condition N/A

Background

KN-62, 1-[N,O-bis-(5-isoquinolinesulphonyl)-N-methyl-L-tyrosy]-4-phenylpiperazine is a highly selective inhibitor of the calcium dependent calmodulin protein kinase II (CAMKII), which binds to the calmodulin binding site of CAMKII and consequently does not inhibit other classes of calmodulin-sensitive kinases. In previous studies, KN-62 exhibits inhibitory effects on the regulated secretion of insulin by hetero-junction with intrinsic thin-layer (HIT) cells and the cholecystokinin secretion from stanniocalcin-1 (STC-1) enteroendocrine cells due to a block of Ca2+ influx through L-type Ca2+ channels in the olasma membrane. It also inhibits both insulin- and hypoxia-stimulated glucose transport activity by 46% and 40% respectively in skeletal muscle.

Reference

Joseph T. Brozinick, Jr., Thomas H. Reynolds, David Dean, Gregory Cartee and Samuel W. Cushman. 1-[N,O-bis-(5-isoquinolinesulphonyl)-N-methyl-L-tyrosy]-4-phenylpiperazine (KN-62), an inhibitor of calcium-dependent camodulin protein kinase II, inhibits both insulin- and hypoxia-stimulated glucose transport in skeletal muscle. Biochem. J. (1999) 339, 533-540

Erik S. Schweitzer, Michael J. Sanderson and C. G. Wasterlain. Inhibition of regulated catecholamine secretion from PC12 cells by the Ca2+/calmodulin kinase II inhibitor KN-62. Journal of Cell Science 108. 2619-2628 (1995)