3,5-dimethyl PIT-1
货号：
10727-1mg 基本售价：
280.0 元 规格：
1 mg
产品信息
概述| 货号 | 10727-1mg |
| 描述 | PtdIns-(3,4,5)-P3(PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer.1 3,5-dimethyl PIT-1 is a dimethyl analog of PIT-1, the selective inhibitor of PIP3/Akt PH domain binding, that is designed for more favorable solubility in vivo. 3,5-dimethyl PIT-1 inhibits PI3K/Akt signaling (IC50 = 27 μM), suppressing PI3K-PDK1-Akt-dependent phosphorylation, which has been shown to reduce cell viability and induce apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 36 μM).2 4T1 breast cancer growth is significantly attenuated in BALB/c mice with a dose of 1 mg/kg of 3,5-dimethyl PIT-1 per day. |
性能| 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.Miao, B.,Skidan, I.,Yang, J., et al. Small molecule inhibition of phosphatidylinositol-3,4,5-triphosphate (PIP3) binding to pleckstrin homology domains. Proceedings of the National Academy of Sciences of the United States of America 107(46), 20126-20131 (2010).
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| 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 | 345.4 |
| 分子式 | C16H15N3O4S |
| CAS号 | 701947-53-7 |
| 稳定性 | ≥ 2 years |
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