Molecular structure of CDC25 Phosphatase Inhibitor II, NSC 663284, CAS Number: 383907-43-5
CDC25 Phosphatase Inhibitor II, NSC 663284 (CAS 383907-43-5)
See product citations (4)
Alternate Names:
6-chloro-7-[[2-(4-morpholinyl)ethyl]amino]-5,8-quinolinedione; DA-3003-1; SPS8I1
Application:
CDC25 Phosphatase Inhibitor II, NSC 663284 is a competitive CDC25 inhibitor and cell cycle arresting compound
CAS Number:
383907-43-5
Purity:
≥98%
Molecular Weight:
321.76
Molecular Formula:
C15H16ClN3O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
CDC25 Phosphatase Inhibitor II, NSC 663284 is a cell-permeable, 7-substituted quinolinedione compound that is a potent, irreversible, mixed competitive inhibitor of the CDC25 phosphatase family (Ki = 29 nM, 95 nM and 89 nM for CDC25A, CDC25B and CDC25C, respectively, IC50 = 210 nM for CDC25B). CDC25 dual-specificity phosphatases coordinate cell cycle progression and cellular signaling. CDC25 Phosphatase Inhibitor II may act to arrest synchronized cells at both G1 and G2/M phases, and block dephosphorylation and activation of Cdk1 and Cdk2. This product was 20-fold more selective against CDC25B as compared to VHR phosphatase and 450-fold more selective as compared to PTP1B phosphatase, and also blocked cellular Erk dephosphorylation. Recent research shows that CDC25 Phosphatase Inhibitor II induces reactive oxygen species in mammalian cells, but does not inhibit MKP-1 and MKP-3.
CDC25 Phosphatase Inhibitor II, NSC 663284 (CAS 383907-43-5) References
- Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25. | Lazo, JS., et al. 2001. J Med Chem. 44: 4042-9. PMID: 11708908
- Dual G1 and G2 phase inhibition by a novel, selective Cdc25 inhibitor 6-chloro-7-[corrected](2-morpholin-4-ylethylamino)-quinoline-5,8-dione. | Pu, L., et al. 2002. J Biol Chem. 277: 46877-85. PMID: 12356752
- Small molecule regulation of phosphatase-dependent cell signaling pathways. | Lazo, JS. and Wipf, P. 2003. Oncol Res. 13: 347-52. PMID: 12725524
- NAD(P)H:quinone oxidoreductase-1-dependent and -independent cytotoxicity of potent quinone Cdc25 phosphatase inhibitors. | Han, Y., et al. 2004. J Pharmacol Exp Ther. 309: 64-70. PMID: 14718602
- Down-regulation of survivin in nitric oxide-induced cell growth inhibition and apoptosis of the human lung carcinoma cells. | Chao, JI., et al. 2004. J Biol Chem. 279: 20267-76. PMID: 14988404
- Chemical complementation: a definitive phenotypic strategy for identifying small molecule inhibitors of elusive cellular targets. | Vogt, A. and Lazo, JS. 2005. Pharmacol Ther. 107: 212-21. PMID: 15925410
- Redox regulation of Cdc25B by cell-active quinolinediones. | Brisson, M., et al. 2005. Mol Pharmacol. 68: 1810-20. PMID: 16155209
- Pharmacology and antitumor activity of a quinolinedione Cdc25 phosphatase inhibitor DA3003-1 (NSC 663284). | Guo, J., et al. 2007. Anticancer Res. 27: 3067-73. PMID: 17970046
- A cell-active inhibitor of mitogen-activated protein kinase phosphatases restores paclitaxel-induced apoptosis in dexamethasone-protected cancer cells. | Vogt, A., et al. 2008. Mol Cancer Ther. 7: 330-40. PMID: 18245669
- Small-molecule inhibitors of SETD8 with cellular activity. | Blum, G., et al. 2014. ACS Chem Biol. 9: 2471-8. PMID: 25137013
- Next-Generation Cell-Active Inhibitors of the Undrugged Oncogenic PTP4A3 Phosphatase. | Lazo, JS., et al. 2019. J Pharmacol Exp Ther. 371: 652-662. PMID: 31601683
- High-throughput screening of the ReFRAME, Pandemic Box, and COVID Box drug repurposing libraries against SARS-CoV-2 nsp15 endoribonuclease to identify small-molecule inhibitors of viral activity. | Choi, R., et al. 2021. PLoS One. 16: e0250019. PMID: 33886614
- Addressing Compound Reactivity and Aggregation Assay Interferences: Case Studies of Biochemical High-Throughput Screening Campaigns Benefiting from the National Institutes of Health Assay Guidance Manual Guidelines. | Coussens, NP., et al. 2021. SLAS Discov. 26: 1280-1290. PMID: 34218710
Inhibitor of:
6330545A04Rik, Cdc25, Cdc25A, Cdc25B, Cdc25C, D4Wsu53e, DDX42, DDX52, E74 like ETS transcription factor (ELF), EG244495, HSZFP36, IPP-1, IQSEC3, Ribosomal Protein L11, Ribosome (RPL; 40S; 60S), USP9X, ZIP7, and ZSCAN5.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
CDC25 Phosphatase Inhibitor II, NSC 663284, 1 mg | sc-202987A | 1 mg | $51.00 | |||
CDC25 Phosphatase Inhibitor II, NSC 663284, 5 mg | sc-202987 | 5 mg | $241.00 | |||
CDC25 Phosphatase Inhibitor II, NSC 663284, 10 mg | sc-202987B | 10 mg | $357.00 | |||
CDC25 Phosphatase Inhibitor II, NSC 663284, 25 mg | sc-202987C | 25 mg | $663.00 |