• 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。

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• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *