| 货号 | 16772-1mg |
| 描述 | Diacylglycerol (DAG) kinases (DGKs) phosphorylate DAG to give phosphatidic acid (PA), reducing signaling through DAG and increasing signaling through PA.1 R-59-022 is an inhibitor of DGK (IC50 = 2.8 µM).2 This results in increased DAG-dependent PKC activity and potentiates aggregation of thrombin-stimulated platelets.2,3 R-59-022 also blocks vascular contraction induced by the thromboxane analog U-46619 (Item No. 16450).4 At 10 µM, R-59-022 induces apoptosis in glioblastoma cells without being toxic to non-cancerous cells.5 It inhibits DGK-θ in vitro at concentrations below 1 µM and blocks DGK-θ activity in vivo.6 R-59-022 also inhibits A. thaliana DGK2 (IC50 = 50 µM) and suppresses root growth but does not affect DGK7 at 50 µM.7 |
| 别名 | Diacylglycerol Kinase Inhibitor I; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Topham, M.K. and Prescott, S.M. Mammalian diacylglycerol kinases, a family of lipid kinases with signaling functions. The Journal of Biological Chemisty 274, 11447-11450 (1999). 2.de Chaffoy de Courcelles, D.C.,Roevens, P. and Van Belle, H. R 59 022, a diacylglycerol kinase inhibitor. Its effect on diacylglycerol and thrombin-induced C kinase activation in the intact platelet. The Journal of Biological Chemisty 260(29), 15762-15770 (1985). 3.Nunn, D.L. and Watson, S.P. A diacylglycerol kinase inhibitor, R59022, potentiates secretion by and aggregation of thrombin-stimulated human platelets. Biochemistry Journal 243(3), 809-813 (1987). 4.Nobe, K.,Miyatake, M.,Nobe, H., et al. Novel diacylglycerol kinase inhibitor selectively suppressed an U46619-induced enhancement of mouse portal vein contraction under high glucose conditions. British Journal of Pharmacology 143(1), 166-179 (2004). 5.Dominguez, C.L.,Floyd, D.H.,Xiao, A., et al. Diacylglycerol kinase a is a critical signaling node and novel therapeutic target in glioblastoma and other cancers. Cancer Discov. 3(7), 782-797 (2013). 6.Tu-Sekine, B.,Goldschmidt, H.,Petro, E., et al. Diacylglycerol kinase θ: Regulation and stability. Adv.Biol.Regul. 53(1), 118-126 (2013). 7.Gómez-Merino, F.C.,Arana-Ceballos, F.A.,Trejo-Téllez, L.I., et al. Arabidopsis AtDGK7, the smallest member of plant diacylglycerol kinases (DGKs), displays unique biochemical features and saturates at low substrate concentration: The DGK inhibitor R59022 differentially affects AtDGK2 and AtDGK7 activity in vitro and alters plant growth and development. The Journal of Biological Chemisty 280(41), 34888-34899 (2005). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 459.6 |
| 分子式 | C27H26FN3OS |
| CAS号 | 93076-89-2 |
| 稳定性 | ≥ 2 years |
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