货号 | 10010233-100mg |
描述 | Akt1, 2, and 3 are serine/threonine protein kinases in the phosphatidylinositol 3 (PI3)-kinase signalling pathway that play a critical role in the regulation of cell proliferation and survival.1,2 Following recruitment of Akt to the plasma membrane, phosphorylation at threonine 308 and serine 473 (Akt1 numbering) by phosphoinositide-dependent kinases (PDK) 1 and 2 results in full activation of the enzyme. CAY10567 is an Akt1 translocation inhibitor. At a concentration of 12.5 µM, it prevents the translocation of Akt1 by apparently compromising the function of the PH domain. A structurally similar compound inhibits kinase activity in vitro with an EC50 value of 12 µM by binding to the kinase domain.3 CAY10567 also inhibits hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) with an IC50 value of 79 µM. 4 |
别名 | BML-257; |
供应商 | Cayman |
应用文献 | |
1.Vivanco, I., and Sawyers, C.L. The phosphatidylinositol 3-kinase-AKT pathway in human cancer. Nature Reviews.Cancer 2, 489-501 (2002). 2.Hennessy, B.T.,Smith, D.L.,Ram, P.T., et al. Exploiting the PI3K/AKT pathway for cancer drug discovery. Nature Reviews.Drug Discovery 4, 988-1004 (2005). 3.Lundholt, B.K.,Linde, V.,Loechel, F., et al. Identification of Akt pathway inhibitors using redistribution screening on the FLIPR and the IN cell 3000 analyzer. Journal of Biomolecular Screening 10(1), 20-29 (2005). 4.Rong, F.,Chow, S.,Yan, S., et al. Structure-activity relationship (SAR) studies of quinoxalines as novel HCV NS5B RNA-dependent RNA polymerase inhibitors. Bioorganic & Medicinal Chemistry Letters 17, 1663-1666 (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 | 326.4 |
分子式 | C21H14N2O2 |
CAS号 | 32387-96-5 |
稳定性 | ≥ 2 years |
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