| 货号 | 17542-1mg |
| 描述 | c-Jun N-terminal kinases (JNKs) phosphorylate c-Jun and regulate transcription in response to an array of inflammatory signals.1 JNK inhibitor V is an ATP-competitive inhibitor of JNK1, JNK2, and JNK3 (IC50s = 150, 220, and 70 nM, respectively).2,3 While initial studies demonstrated 10- to 100-fold selectivity for JNK isoforms over a panel of 25 other kinases, strong interactions of JNK inhibitor V with GSK3B, Pim-1, Pim-3, and other kinases, evaluated as a shift in thermal melting point, suggest additional targets exist.2,4In vivo efficacy of JNK inhibitor V against JNK isoforms has been demonstrated in gerbils, mice, and rats via oral, intravenous, or intraperitoneal administration.4,5 This compound is commonly used to investigate the role of JNK signaling in cells and animals.6,7 |
| 别名 | AS-601245;c-Jun N-terminal Kinase Inhibitor V; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Johnson, G.L. and Lapadat, R. Mitogen-activated protein kinase pathways mediated by ERK, JNK, and p38 protein kinases. Science 298, 1911-1912 (2002). 2.Gaillard, P.,Jeanclaude-Etter, I.,Ardissone, V., et al. Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase. Journal of Medicinal Chemistry 48(14), 4596-4607 (2005). 3.Carboni, S.,Hiver, A.,Szyndralewiez, C., et al. AS601245 (1,3-benzothiazol-2-yl (2-[[2-(3-pyridinyl) ethyl] amino]-4 pyrimidinyl) acetonitrile): A c-Jun NH2-terminal protein kinase inhibitor with neuroprotective properties. Journal of Pharmacology and Experimental Therapeutics 310(1), 25-32 (2004). 4.Fedorov, O.,Marsden, B.,Pogacic, V., et al. A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proceedings of the National Academy of Sciences of the United States of America 104(51), 20523-20528 (2007). 5.Ferrandi, C.,Ballerio, R.,Gaillard, P., et al. Inhibition of c-Jun N-terminal kinase decreases cardiomyocyte apoptosis and infarct size after myocardial ischemia and reperfusion in anaesthetized rats. British Journal of Pharmacology 142(6), 953-960 (2004). 6.Oktem, O.,Buyuk, E. and Oktay, K. Preantral follicle growth is regulated by c-Jun-N-terminal kinase (JNK) pathway. Reprod.Sci. 18(3), 269-276 (2011). 7.Tu, Y.F.,Tsai, Y.S.,Wang, L.W., et al. Overweight worsens apoptosis, neuroinflammation and blood-brain barrier damage after hypoxic ischemia in neonatal brain through JNK hyperactivation. Journal of Neuroinflammation 8, 1-15 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% (sum of isomers) |
| 计算分子量 | 372.5 |
| 分子式 | C20H16N6S |
| CAS号 | 345987-15-7 |
| 稳定性 | ≥ 2 years |
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