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KN-93

Cayman Chemical Item Number 13319

(CAS 139298-40-1)

KN-93 (CAS 139298-40-1)

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Description

KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM).1 It does not affect the activities of PKA, PKC, MLCK, or Ca2+-phosphodiesterase.1 It inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM).2 More recently, KN-93 has been used to implicate roles for CaMKII in Ca2+-induced Ca2+ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca2+-dependent activation of HIF-1α in colon cancer cells.3,4,5

1 Sumi, M., Kiuchi, K., Ishikawa, T., et al. The newly synthesized selective Ca2+/calmodulin dependent protein kinase II inhibitor KN-93 reduces dopamine contents in PC12th cells. Biochem Biophys Res Commun 181(3) 968-975 (1991).

2 Mamiya, N., Goldenring, J.R., Tsunoda, Y., et al. Inhibition of acid secretion in gastric parietal cells by the Ca2+/calmodulin-dependent protein kinase II inhibitor KN-93. Biochem Biophys Res Commun 195(2) 608-615 (1993).

3 Oestreich, E.A., Malik, S., Goonasekera, S.A., et al. Epac and phospholipase Ce regulate Ca2+ release in the heart by activation of protein kinase Ce and calcium-calmodulin kinase II. J Biol Chem 284(3) 1514-1522 (2009).

4 Flamand, N., Luo, M., Peters-Golden, M., et al. Phosphorylation of serine 271 on 5-lipoxygenase and its role in nuclear export. J Biol Chem 284(1) 306-313 (2009).

5 Riganti, C., Doublier, S., Viarisio, D., et al. Artemisinin induces doxorubicin resistance in human colon cancer cells via calcium-dependent activation of HIF-1a and P-glycoprotein overexpression. Br J Pharmacol 156 1054-1066 (2009).

Formal Name N-​[2-​[[[3-​(4-​chlorophenyl)-​2-​propen-​1-​yl]methylamino]methyl]phenyl]-​N-​(2-​hydroxyethyl)-​4-​methoxy-​benzenesulfonamide
CAS Number 139298-40-1
Molecular Formula C26H29ClN2O4S
Formula Weight 501.0
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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CN(C/C=C/C1=CC=C(Cl)​C=C1)​CC2=CC=CC=C2N(S(=O)​(C3=CC=C(OC)​C=C3)​=O)​CCO

Background Reading

Riganti, C., Doublier, S., Viarisio, D., et al. Artemisinin induces doxorubicin resistance in human colon cancer cells via calcium-dependent activation of HIF-1a and P-glycoprotein overexpression. Br J Pharmacol 156 1054-1066 (2009).

Flamand, N., Luo, M., Peters-Golden, M., et al. Phosphorylation of serine 271 on 5-lipoxygenase and its role in nuclear export. J Biol Chem 284(1) 306-313 (2009).

Oestreich, E.A., Malik, S., Goonasekera, S.A., et al. Epac and phospholipase Ce regulate Ca2+ release in the heart by activation of protein kinase Ce and calcium-calmodulin kinase II. J Biol Chem 284(3) 1514-1522 (2009).

Mamiya, N., Goldenring, J.R., Tsunoda, Y., et al. Inhibition of acid secretion in gastric parietal cells by the Ca2+/calmodulin-dependent protein kinase II inhibitor KN-93. Biochem Biophys Res Commun 195(2) 608-615 (1993).

Sumi, M., Kiuchi, K., Ishikawa, T., et al. The newly synthesized selective Ca2+/calmodulin dependent protein kinase II inhibitor KN-93 reduces dopamine contents in PC12th cells. Biochem Biophys Res Commun 181(3) 968-975 (1991).

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KN-93 is available in the following screening library:

Size Price Quantity Subtotal
1 mg $86.00 $0.00
5 mg $387.00 $0.00
10 mg $688.00 $0.00
25 mg $1,505.00 $0.00
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Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

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Pricing updated 2012-05-26. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

Related Products

KN-62
KN-92 (hydrochloride)
ML-9

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