| 货号 | 13303-1mg |
| 描述 | Three genes encode dual specificity phosphatases that are Cdc25 homologs. The phosphatases, Cdc25A through C, are proto-oncogenes and are often over-expressed in cancers. NSC 663284 is a potent, cell-permeable, and irreversible inhibitor of all Cdc25 isoforms, with preference for Cdc25A (IC50 = 29, 95, and 89 nM for Cdc25A, Cdc25B2, and Cdc25C, respectively).1 NSC 663284 poorly inhibits other phosphatases, including Vaccinia virus VH1-related (IC50 = 4.0 μM), PTP1B (no inhibition), and the mitogen-activated protein kinase phosphatases (MKP) MKP-1 or -3 (no inhibition).1,2 By inhibiting Cdc25 isoforms, NSC 663284 prevents the dephosphorylation and activation of Cdk1 and Cdk2,3,4 arrests cells at both G1 and G2/M phases,3 and prevents the proliferation of several human tumor cell lines.1,3,5 |
| 别名 | Cdc25 Phosphatase Inhibitor II;DA-3003-1;SPS8I1; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Lazo, J.S.,Aslan, D.C.,Southwick, E.C., et al. Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25. Journal of Medicinal Chemistry 44, 4042-4049 (2001). 2.Vogt, A.,McDonald, P.R.,Tamewitz, A., et al. A cell-active inhibitor of mitogen-activated protein kinase phosphatases restores paclitaxel-induced apoptosis in dexamethasone-protected cancer cells. Molecular Cancer Therapeutics 7(2), 330-340 (2008). 3.Pu, L.,Amoscato, A.A.,Bier, M.E., et al. Dual G1 and G2 phase inhibition by a novel, selective Cdc25 inhibitor 7-chloro-6-(2-morpholin-4-ylethylamino)-quinoline-5,8-dione. The Journal of Biological Chemisty 277(49), 46877-46885 (2002). 4.Han, Y.,Shen, H.,Carr, B.I., et al. NAD(P)H:quinone oxidoreductase-1-dependent and -independent cytotoxicity of potent quinone Cdc25 phosphatase inhibitors. J. Pharmacol. Exp. Ther. 309(1), 64-70 (2004). 5.Guo, J.,Parise, R.A.,Joseph, E., et al. Pharmacology and antitumor activity of a quinolinedione Cdc25 phosphatase inhibitor DA3003-1 (NSC 663284). Anticancer Research 27, 3067-3074 (2007). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 321.8 |
| 分子式 | C15H16ClN3O3 |
| CAS号 | 383907-43-5 |
| 稳定性 | ≥ 2 years |
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