| 货号 | 13812-10mg |
| 描述 | 17β-hydroxy Wortmannin is an analog of wortmannin. It irreversibly binds phosphoinositide 3-kinase (PI3K) and potently blocks fMLP-stimulated respiratory burst in neutrophils (IC50 = 5 nM).1 17β-hydroxy Wortmannin inhibits recombinant PI3K and mTOR (IC50 = 2.7 and 193 nM, respectively) and prevents the growth of LNCap prostate cancer cells (IC50 = 1.46 μM).2 The 17-hydroxyl group has been used to further modify this compound, e.g., by pegylation and conjugation with rapamycin.3,4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Thelen, M.,Wymann, M.P. and Langen, H. Wortmannin binds specifically to 1-phosphatidylinositol 3-kinase while inhibiting guanine nucleotide-binding protein-coupled receptor signaling in neutrophil leukocytes. Proceedings of the National Academy of Sciences of the United States of America 91, 4960-4964 (1994). 2.Zask, A.,Kaplan, J.,Toral-Barza, L., et al. Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: Potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy. Journal of Medicinal Chemistry 51, 1319-1323 (2008). 3.Zhu, T.,Gu, J.,Yu, K., et al. Pegylated wortmannin and 17-hydroxywortmannin conjugates as phosphoinositide 3-kinase inhibitors active in human tumor xenograft models. Journal of Medicinal Chemistry 49, 1373-1378 (2006). 4.Ayral-Kaloustian, S.,Gu, J.,Lucas, J., et al. Hybrid inhibitors of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR): Design, synthesis, and superior antitumor activity of novel wortmannin-rapamycin conjugates. Journal of Medicinal Chemistry 53(1), 452-459 (2010). | |
| 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 | 430.4 |
| 分子式 | C23H26O8 |
| CAS号 | 58053-83-1 |
| 稳定性 | ≥ 2 years |
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