| 产品描述： | NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor (Ki=32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C); IC50=22.3 nM (human Cdc25A), 56.9 nM (human Cdc25C), 125 nM (Cdc25B)). NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway |
| 靶点： |
Ki: 32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C) IC50: 22.3 nM (human Cdc25A) , 56.9 nM (human Cdc25C), 125 nM (Cdc25B);Apoptosis; Phosphatase |
| 体外研究： |
NSC 95397 (0, 10, and 20 µM; 24 hour) decreases the cell viability of three colon cancer cell lines SW480, SW620, and DLD-1 in a concentration-dependent manner. NSC 95397(10 μM; 24 hour) upregulates p21 while downregulates CDK4 and CDK6 were d in all three colon cancer cell lines SW480, SW620, and DLD-1 cells. NSC 95397 (10 μM; 24 hour) reduces the phosphorylation of retinoblastoma protein (Rb) on Ser795 and Ser807/811. NSC 95397 (20 μM; 24 hours) significantly increases cleaved caspase-9, -3, -7 and PARP levels. NSC 95397 (10 μM; 6 hours) enhances the phosphorylation of its downstream ERK1/2 at Thr202/Tyr 204. Cell Viability Assay Cell Line: Human colon cancer cell lines, SW480, SW620, and DLD-1 Concentration: 0, 10, and 20 µM Incubation Time: 24 hours Result: The IC50 values of NSC 95397 for the cell growth of SW480, SW620, and DLD-1 cells were 9.9, 14.1 and 18.6 μM, respectively. Western Blot Analysis Cell Line: SW480, SW620, and DLD-1 cells Concentration: 10 μM Incubation Time: 24 hours Result: p21 was upregulated while CDK4 and CDK6 were downregulated.Rduced the phosphorylation of Rb on Ser795 and Ser807/811 |
| 参考文献： |
1. Lazo JS, et al. Identification of a potent and selective pharmacophore for Cdc25 dual specificity phosphatase inhibitors. Mol Pharmacol. 2002 Apr;61(4):720-8. 2. Dubey NK, et al. NSC 95397 Suppresses Proliferation and Induces Apoptosis in Colon Cancer Cells through MKP-1 and the ERK1/2 Pathway. Int J Mol Sci. 2018 May 31;19(6). pii: E1625. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.222 ml |
16.109 ml |
32.218 ml |
| 5 mM |
0.644 ml |
3.222 ml |
6.444 ml |
| 10 mM |
0.322 ml |
1.611 ml |
3.222 ml |
| 50 mM |
0.064 ml |
0.322 ml |
0.644 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