| 产品描述： | CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor |
| 靶点： |
PKC;CDK1-Cyclin B:26 nM (IC50);CDK2/cyclinE:3 nM (IC50);cdk2/cyclin A:4 nM (IC50);Cdk5/p25:10 nM (IC50);CDK7/cyclin H:200 nM (IC50);CDK9/cycT:13 nM (IC50);CDK4/cyclin D:216 nM (IC50);VEGFR; CDK; PKC |
| 体内研究： |
CGP-60474 (10 mg/kg; i.p.) inhibits the IL-6 level and increases the survival rate in the LPS endotoxemia model |
| 参考文献： |
1. Jorda R, et al. How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?. J Med Chem. 2018;61(20):9105-9120. 2. Han HW, et al. LINCS L1000 dataset-based repositioning of CGP-60474 as a highly potent anti-endotoxemic agent. Sci Rep. 2018;8(1):14969. Published 2018 Oct 8. 3. Stanetty P, et al. Novel and efficient access to phenylamino-pyrimidine type protein kinase C inhibitors utilizing a Negishi cross-coupling strategy. J Org Chem. 2005;70(13):5215-5220. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.81 ml |
14.052 ml |
28.104 ml |
| 5 mM |
0.562 ml |
2.81 ml |
5.621 ml |
| 10 mM |
0.281 ml |
1.405 ml |
2.81 ml |
| 50 mM |
0.056 ml |
0.281 ml |
0.562 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京