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Biological Activity for NSC 663284
NSC 663284 is a potent, selective inhibitor of Cdc25 dual specificity phosphatases (Ki values are 29, 95 and 89 nM for human Cdc25A, Cdc25B2 and Cdc25C respectively); > 20- and > 450-fold selective over VHR and PTP1B phosphatases respectively. Arrests cells at both G1 and G2/M phase and blocks cdk2 and cdk1 activation. Blocks proliferation of a range of human tumor cell lines (IC50 = 0.2 - 35 μM).
Compound Libraries for NSC 663284
Technical Data for NSC 663284
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for NSC 663284
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for NSC 663284
The following data is based on the product molecular weight 321.76. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||6.22 mL||31.08 mL||62.16 mL|
|2.5 mM||1.24 mL||6.22 mL||12.43 mL|
|5 mM||0.62 mL||3.11 mL||6.22 mL|
|25 mM||0.12 mL||0.62 mL||1.24 mL|
References for NSC 663284
References are publications that support the biological activity of the product.
Brisson et al (2005) Redox regulation of cdc25B by cell-active Quinolinediones. Mol.Pharmacol. 68 1810 PMID: 16155209
Lazo et al (2001) Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25. J.Med.Chem. 44 4042 PMID: 11708908
Pu et al (2002) Dual G1 and G2 phase inhibition by a novel, selective Cdc25 inhibitor 7-chloro-6-(2-morpholin-4-ylethylamino)-quinoline-5,8-dione. J.Biol.Chem. 277 46877 PMID: 12356752
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Keywords: NSC 663284, NSC 663284 supplier, Potent, selective, Cdc25, phosphatase, inhibitors, inhibits, Cyclin-Dependent, Protein, Kinase, Cdk, Kinases, Dual-Specificity, Phosphatases, NSC663284, Phosphatase, Cyclin-dependent, CDK1, Subfamily, 1867, Tocris Bioscience
Citations for NSC 663284
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.