| 货号 | 10010237-10mg |
| 描述 | Akt-1, -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 (Akt-1 numbering) by phosphoinositide-dependent kinases (PDK) 1 and 2 results in full activation of the enzyme. Triciribine is a cell-permeable tricyclic nucleoside that inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3.3 It does not inhibit phosphatidylinositol 3 (PI3)-Kinase or PDK1, the direct upstream activators of Akt, nor does it inhibit PKC, PKA, ERK1/2, serum- and glucocorticoid-inducible kinase, p38, STAT3, or JNK signalling pathways.3 Triciribine effectively inhibits growth of Akt-overexpressing human cancer cell lines in vitro with 50% inhibition at ~5-10 µM. It also inhibit growth of tumor xenografts in mice by greater than 80% at a dose of 1 mg/kg/day.3,4 |
| 别名 | API 2;NSC 154020;Tricyclic Nucleoside; |
| 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.Yang, L.,Dan, H.C.,Sun, M., et al. Akt/protein kinase B signaling inhibitor-2, a selective small molecule inhibitor of Akt signaling with antitumor activity in cancer cells overexpressing Akt. Cancer Research 64, 4394-4399 (2004). 4.Karst, A.M.,Dai, D.L.,Cheng, J.Q., et al. Role of p53 up-regulated modulator of apoptosis and phosphorylated Akt in melanoma cell growth, apoptosis, and patient survival. Cancer Research 66(18), 9221-9226 (2006). | |
| 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 | 320.3 |
| 分子式 | C13H16N6O4 |
| CAS号 | 35943-35-2 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |