| 货号 | 13864-10mg |
| 描述 | KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase type 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 |
| 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.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). 4.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). 5.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 | 537.5 |
| 分子式 | C26H29ClN2O4S • HCl |
| CAS号 | 1956426-56-4 |
| 稳定性 | ≥ 2 years |
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