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KN-93

Cayman Chemical Item Number 13319

(CAS 139298-40-1)

KN-93 (CAS 139298-40-1)

See more	Inhibitors (493) Cell Biology (281) Signal Transduction (314)

Description

KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase (K_i = 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	Copy SMILES to clipboard 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:

Bio-active Lipid I Screening Library (96-Well)

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
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-02-10. 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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