| 货号 | 13643-1mg |
| 描述 | The mammalian target of rapamycin (mTOR) is a serine-threonine kinase that is central to two protein complexes, mTORC1 and mTORC2. These complexes are differentially regulated (e.g., only mTORC1 is sensitive to rapamycin) and regulate different pathways. PP242 is an inhibitor of the active site of mTOR kinase in both mTORC1 and mTORC2 (IC50 = 8 nM).1,2 It less effectively inhibits PKCα, PI3-kinase subunit p110γ, JAK2, PKCβI, and PKCβII (IC50 = 49, 102, 110, 198, and 185, respectively).2,3 PP242 has been shown to cause the death of certain human and murine leukemia cells more potently than rapamycin and, in vivo, delays leukemia onset and augments the effects of tyrosine kinase inhibitors in suppressing leukemic expansion and extending survival.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Apsel, B.,Blair, J.A.,Gonzalez, B., et al. Targeted polypharmacology: Discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nature Chemical Biology 4(11), 691-699 (2008). 2.Feldman, M.E.,Apsel, B.,Uotila, A., et al. Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2. PLOS Biology 7(2), 0371-0383 (2009). 3.Kojima, F.,Kapoor, M.,Kawai, S., et al. Prostaglandin E2 activates Rap1 via EP2/EP4 receptors and cAMP-signaling in rheumatoid synovial fibroblasts: Involvement of Epac1 and PKA. Prostaglandins & Other Lipid Mediators 89(1-2), 26-33 (2009). 4.Janes, M.R.,Limon, J.J.,So, L., et al. Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor. Nature Medicine 16(2), 205-213 (2010). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 308.3 |
| 分子式 | C16H16N6O |
| CAS号 | 1092351-67-1 |
| 稳定性 | ≥ 2 years |
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