NU 6102 是一种有效的 CDK1 和 CDK2 抑制剂，对 CDK1/cyclinB 和 CDK2/cyclinA3 的 IC50 分别为 9.5 nM 和 5.4 nM。 NU 6102 对 CDK1/CDK2 的选择性优于 CDK4（IC50 为 1.6 μM）、DYRK1A（IC50 为 0.9 μM）、PDK1（IC50 为 0.8 μM）和 ROCKII（IC50 为 0.6 μM）。
| Cas No. | 444722-95-6 |
| 别名 | 4-[[6-(环己基甲氧基)-1H-嘌呤-2-基]氨基]苯磺酰胺 |
| 化学名 | 4-[[6-(cyclohexylmethoxy)-9H-purin-2-yl]amino]-benzenesulfonamide |
| Canonical SMILES | NS(C(C=C1)=CC=C1NC2=NC(NC=N3)=C3C(OCC4CCCCC4)=N2)(=O)=O |
| 分子式 | C18H22N6O3S |
| 分子量 | 402.5 |
| 溶解度 | DMSO: >1 mg/ml,Ethanol: >1 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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. NU 6102 inhibits Cdk4 activity with an IC50 value of 1.6 μM, suggesting it is most selective for Cdk2. 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. 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. |
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