| 货号 | 15500-2.5mg |
| 描述 | Cercosporamide is a natural antifungal phytotoxin isolated from the Cercosporidium fungus, which infects the leaves of cassava plants.1 Its antifungal effect results from its selective and potent inhibition of fungal PKC-like 1 kinases (Pkc1), which are central to cell wall integrity (IC50 = 25 nM for CandidaPkc1).2 Cercosporamide less effectively inhibits human PKC isoforms PKCα, β, and γ (IC50s = 1.02, 0.35, and 5.8 μM, respectively), an action linked to lowering of plasma glucose in hyperglycemic mice.2,3 However, it potently inhibits MAPK-interacting kinases Mnk1 and Mnk2 (IC50 = 115 and 11 nM, respectively), reducing protein translation in cancer cells.4,5 Cercosporamide is orally bioavailable.2,3 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Sugawara, F.,Strobel, S.,Strobel, G., et al. The structure and biological activity of cercosporamide from Cercosporidium henningsii. The Journal of Organic Chemistry 56, 909-910 (1991). 2.Sussman, A.,Huss, K.,Chio, L.C., et al. Discovery of cercosporamide, a known antifungal natural product, as a selective Pkc1 kinase inhibitor through high-throughput screening. Eukaryot.Cell 3(4), 932-943 (2004). 3.Furukawa, A.,Arita, T.,Satoh, S., et al. (−)-Cercosporamide derivatives as novel antihyperglycemic agents. Bioorganic & Medicinal Chemistry Letters 19(3), 724-726 (2009). 4.Konicek, B.W.,Stephens, J.R.,McNulty, A.M., et al. Therapeutic inhibition of MAP kinase interacting kinase blocks eukaryotic initiation factor 4E phosphorylation and suppresses outgrowth of experimental lung metastases. Cancer Research 71(5), 1849-1857 (2011). 5.Hou, J.,Lam, F.,Proud, C., et al. Targeting Mnks for cancer therapy. Oncotarget 3(2), 118-131 (2012). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 331.3 |
| 分子式 | C16H13NO7 |
| CAS号 | 131436-22-1 |
| 稳定性 | ≥ 2 years |
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