| 货号 | 21472-1mg |
| 描述 | KN-93 (phosphate) is a potent and selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII) (Ki = 370 nM), inhibiting both the α- and β-subunits of CaMKII.1 It does not have significant effects on cAMP-dependent protein kinase, Ca2+/phospholipid-dependent protein kinase, myosin light chain kinase, or Ca2+ phosphodiesterase activity. It inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM).2 KN-93 can block voltage-gated potassium (Kv) channels when applied extracellularly, independent of its CaMKII action.3 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.4,5,6 |
| 供应商 | Cayman |
| 应用文献 | |
| 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. 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. Biophys. Res. Commun. 195(2), 608-615 (1993). 3.Rezazadeh, S.,Claydon, T.W., and Fedida, D. KN-93 (2-[N-(2-hydroxyethyl)]-N-(4-methoxybenzenesulfonyl)]amino-N-(4-chlorocinnamyl)-N-methylbenzylamine), a calcium/calmodulin-dependent protein kinase II inhibitor, is a direct extracellular blocker of voltage-gated potassium channels. J. Pharmacol. Exp. Ther. 317(1), 292-299 (2006). 4.Oestreich, E.A.,Malik, S.,Goonasekera, S.A., et al. Epac and phospholipase Cε regulate Ca2+ release in the heart by activation of protein kinase Cε and calcium-calmodulin kinase II. J. Biol. Chem. 284(3), 1514-1522 (2009). 5.Flamand, N.,Luo, M.,Peters-Golden, M., et al. Phosphorylation of serine 271 on 5-lipoxygenase and its role in nuclear export. The Journal of Biological Chemisty 284(1), 306-313 (2009). 6.Riganti, C.,Doublier, S.,Viarisio, D., et al. Artemisinin induces doxorubicin resistance in human colon cancer cells via calcium-dependent activation of HIF-1α and P-glycoprotein overexpression. Br. J. Pharmacol. 156, 1054-1066 (2009). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 599 |
| 分子式 | C26H29ClN2O4S • H3PO4 |
| CAS号 | 1188890-41-6 |
| 稳定性 | ≥ 2 years |
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