| 货号 | 15344-1mg |
| 描述 | Ku-0060648 is an ATP-competitive inhibitor of DNA-dependent protein kinase (DNA-PK) and an inhibitor of PI3K. In a cell-free assay, it has IC50s of 5, 4, 0.5, <0.1, and 594 nM for DNA-PK, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively.1 In cells, the level of PI3K inhibition is variable, depending upon the cell line utilized. In MCF-7 cells, it has IC50s of 19 and 39 nM, for DNA-PK and PI3K, respectively, while in SW620 cells, it has an IC50 of 170 nM for DNA-PK but >10,000 nM for PI3K.1 Ku-0060648 is useful for Cas9 editing due to its DNA-PK inhibition, which reduces the frequency of non-homologous end joining and increases homology-directed recombination.2 It also shows promise in cancer research in vitroandin vivo.3,4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Munck, J.M.,Batey, M.A.,Zhao, Y., et al. Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K. Mol. Cancer Ther. 11(8), 1789-1798 (2012). 2.Robert, F.,Barbeau, M.,Éthier, S., et al. Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing. Genome Med. 7, 93 (2015). 3.Chen, M.-B.,Zhou, Z.-T.,Yang, L., et al. KU-0060648 inhibits hepatocellular carcinoma cells through DNA-PKcs-dependent and DNA-PKcs-independent mechanisms. Oncotarget 7(13), 17047-17059 (2016). 4.Lan, T.,Zhao, Z.,Qu, Y., et al. Targeting hyperactivated DNA-PKcs by KU0060648 inhibits glioma progression and enhances temozolomide therapy via suppression of AKT signaling. Oncotarget 7(34), 55555-55571 (2016). | |
| 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 | 582.7 |
| 分子式 | C33H34N4O4S |
| CAS号 | 881375-00-4 |
| 稳定性 | ≥ 2 years |
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