| 货号 | 13297-1mg |
| 描述 | Tyrphostins are a family of protein tyrosine kinase inhibitors originally developed to inhibit cell growth by blocking the activity of certain growth factor receptor kinases (GFRK). The tyrphostin AG-126 selectively inhibits the phosphorylation of ERK1 (p44) and ERK2 (p42) at 25-50 μM.1,2 It blocks the production of TNF-α in vitro2andin vivo,1 attenuating signaling through NF-κB,1 the induced expression of COX-2 and iNOS,3,4 and the inflammatory response in diverse animal models.3,5 AG-126 is a poor inhibitor of epidermal GFRK (IC50 = 450 μM)6 and platelet-derived GFRK (IC50 > 100 μM).7 |
| 别名 | Tyrphostin AG-126; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Novogrodsky, A.,Vanichkin, A.,Patya, M., et al. Prevention of lipopolysaccharide-induced lethal toxicity by tyrosine kinase inhibitors. Science 264(5163), 1319-1322 (1994). 2.Hanisch, U.K.,Prinz, M.,Angstwurm, K., et al. The protein tyrosine kinase inhibitor AG126 prevents the massive microglial cytokine induction by pneumococcal cell walls. European Journal of Immunology 31, 2104-2115 (2001). 3.Cuzzocrea, S.,McDonald, M.C.,Mazzon, E., et al. The tyrosine kinase inhibitor tyrphostin AG126 reduces the development of acute and chronic inflammation. American Journal of Pathology 157(1), 145-158 (2000). 4.Ruetten, H., and Thiemermann, C. Effects of tyrphostins and genistein on the circulatory failure and organ dysfunction caused by endotoxin in the rat: A possible role for protein tyrosine kinase. British Journal of Pharmacology 122, 59-70 (1997). 5.Chatterjee, P.K.,Patel, N.S.A.,Kvale, E.O., et al. The tyrosine kinase inhibitor tyrphostin AG126 reduces renal ischemia/reperfusion injury in the rat. Kidney International 64, 1605-1619 (2003). 6.Gazit, A.,Yaish, P.,Gilon, C., et al. Tyrphostins I: Synthesis and biological activity of protein tyrosine kinase inhibitors. Journal of Medicinal Chemistry 32(10), 2344-2352 (1989). 7.Sagara, Y.,Ishige, K.,Tsai, C., et al. Tyrphostins protect neuronal cells from oxidative stress. The Journal of Biological Chemisty 277(39), 36204-36215 (2002). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 215.2 |
| 分子式 | C10H5N3O3 |
| CAS号 | 118409-62-4 |
| 稳定性 | ≥ 2 years |
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