| 货号 | 14870-500ug |
| 描述 | Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival as well as angiogenesis.1,2 Akt inhibitor VIII is a potent allosteric inhibitor of Akt1 and Akt2 (IC50s = 58 and 210 nM, respectively) that less effectively blocks Akt3 activity (IC50 = 2.2 µM).3,4,5 It is a poor or ineffective inhibitor of a wide range of other serine-threonine kinases.6 Akt inhibitor VIII is cell permeable, blocking insulin regulation of forkhead box 01 activity at 1 µM in rat hepatoma cells.6 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Manning, B.D. and Cantley, L.C. AKT/PKB signaling: Navigating downstream. Cell 129, 1261-1274 (2007). 2.Yuan, T.L. and Cantley, L.C. PI3K pathway alterations in cancer: Variations on a theme. Oncogene 27(41), 5497-5510 (2008). 3.Lindsley, C.W.,Zhao, Z.,Leister, W.H., et al. Allosteric Akt (PKB) inhibitors: Discovery and SAR of isozyme selective inhibitors. Bioorganic & Medicinal Chemistry Letters 15(3), 761-764 (2005). 4.Zhao, Z.,Leister, W.H.,Robinson, R.G., et al. Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors. Bioorganic & Medicinal Chemistry Letters 15(4), 905-909 (2005). 5.Calleja, V.,Laguerre, M.,Parker, P.J., et al. Role of a novel PH-kinase domain interface in PKB/Akt regulation: Structural mechanism for allosteric inhibition. PLOS Biology 7(1), e17 (2009). 6.Logie, L.,Ruiz-Alcaraz, A.J.,Keane, M., et al. Characterization of a protein kinase B inhibitor in vitro and in insulin-treated liver cells. Diabetes 56(9), 2218-2227 (2007). | |
| 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 | 551.7 |
| 分子式 | C34H29N7O |
| CAS号 | 612847-09-3 |
| 稳定性 | ≥ 2 years |
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