| 货号 | 13317-1mg |
| 描述 | Cyclin-dependent kinases (CDKs) play a key role in regulating cell division by phosphorylating distinct substrates in different phases of the cell cycle. Cell cycle deregulation in many cancers often results from altered CDK activity. Thus, CDKs are potential pharmacological targets for anticancer agents. NU 6102 is a potent inhibitor of Cdk1 and Cdk2 with Ki values of 9 and 6 nM and IC50 values of 9.5 and 5.4 nM, respectively.1,2 NU 6102 inhibits Cdk4 activity with an IC50 value of 1.6 μM, suggesting it is most selective for Cdk2.3 Time-lapse videomicroscopy reveals that 20 μM NU 6102 delays cell entry into mitosis where most cells appear to eventually complete mitotic division but cannot correctly undergo cytokinesis, and hence become binucleated with an abnormal number of centrosomes.4 In SKUT-1B cancer cells a 24 h exposure to NU 6102 induced G2 arrest, inhibition of target protein phosphorylation, and cytotoxicity with an LC50 value of 2.6 μM.5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Sayle, K.L.,Bentley, J.,Boyle, F.T., et al. Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2. Bioorganic & Medicinal Chemistry Letters 13(18), 3079-3082 (2003). 2.Hardcastle, I.R.,Arris, C.E.,Bentley, J., et al. N2-substituted O6-cyclohexylmethylguanine derivatives: Potent inhibitors of cyclin-dependent kinases 1 and 2. Journal of Medicinal Chemistry 47, 3710-3722 (2004). 3.Pratt, D.J.,Bentley, J.,Jewsbury, P., et al. Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity. Journal of Medicinal Chemistry 49, 5470-5477 (2006). 4.Krasinska, L.,Cot, E. and Fisher, D. Selective chemical inhibition as a tool to study Cdk1 and Cdk2 functions in the cell cycle. Cell Cycle 7(12), 1702-1708 (2008). 5.Thomas, H.D.,Wang, L.Z.,Roche, C., et al. Preclinical in vitro and in vivo evaluation of the potent and specific cyclin-dependent kinase 2 inhibitor NU6102 and a water soluble prodrug NU6301. European Journal of Cancer 47(13), 2052-2059 (2011). | |
| 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 | 402.5 |
| 分子式 | C18H22N6O3S |
| CAS号 | 444722-95-6 |
| 稳定性 | ≥ 2 years |
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