| Identification | Back Directory | [Name]
NSC 663284 | [CAS]
383907-43-5 | [Synonyms]
CDC25 Phosphatase Inhibitor II, NSC 663284
5,8-Quinolinedione, 6-chloro-7-[[2-(4-morpholinyl)ethyl]amino]-
CDC25 Phosphatase Inhibitor II, NSC 663284 - CAS 383907-43-5 - Calbiochem | [Molecular Formula]
C15H16ClN3O3 | [MDL Number]
MFCD08276924 | [MOL File]
383907-43-5.mol | [Molecular Weight]
321.76 |
| Chemical Properties | Back Directory | [Boiling point ]
478.8±45.0 °C(Predicted) | [density ]
1.41±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 16 mg/mL
| [form ]
solid
| [pka]
6.79±0.10(Predicted) | [color ]
red
| [Sensitive ]
Light Sensitive | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month. |
| Hazard Information | Back Directory | [Description]
NSC663284 (383907-43-5) is a potent, selective and irreversible inhibitor of CDC25 phosphatases, Ki=29, 95 and 89 nM for human CDC25A, B2 and C respectively and >20- and >450-fold selective over VHR and PTP1B.1?Arrests cells at G1 and G2/M and inhibits cdk1 and 2 activation.2 Inhibits the growth of a variety of human tumor cell lines.3 NSC663284 acts via irreversible oxidation of the catalytic cysteine of CDC25.4 | [Uses]
CDC25 Phosphatase Inhibitor II, NSC 663284 is a competitive CDC25 inhibitor and cell cycle arresting compound. | [Definition]
ChEBI: 6-chloro-7-[2-(4-morpholinyl)ethylamino]quinoline-5,8-dione is a quinolone. | [General Description]
A cell-permable, potent, irreversible, and competitive inhibitor of the Cdc25 phosphatase family (Ki = 29 nM, 95 nM, and 89 nM for Cdc25A, Cdc25B2, and Cdc25C, respectively) with anti-proliferative properties. Displays nearly 20- and 450-fold greater selectivity over VHR and PTP1B (IC50 = 4.0 μM and >100 μM, respectively). Reported to arrest cell cycle progression, inhibit Cdk dephosphorylation, and delay tumor growth (mean IC50 = 1.5 μM in NCI-60 tumor cell panel). Also shown to block ERK dephosphorylation caused by ectopic Cdc25A expression. | [Biological Activity]
Potent, selective inhibitor of Cdc25 dual specificity phosphatases (K i values are 29, 95 and 89 nM for human Cdc25A, Cdc25B 2 and Cdc25C respectively); > 20- and > 450-fold selective over VHR and PTP1B phosphatases respectively. Arrests cells at both G 1 and G 2 /M phase and blocks cdk2 and cdk1 activation. Blocks proliferation of a range of human tumor cell lines (IC 50 = 0.2-35 μ M). | [Biochem/physiol Actions]
Cell permeable: yes | [storage]
Store at -20°C | [References]
1) Lazo et al. (2001), Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatases Cdc25; J. Med. Chem., 44 4042
2) Pu et al. (2002), Dual G1 and G2 phase inhibition by a novel, selective Cdc25 inhibitor 6-chloro-7-(2-morpholin-4-ylethylamino)-quinoline-3,8-dione; J. Biol. Chem., 277 46877
3) Han et al. (2004), NAD(P)H:quinone oxidoreductase-1-dependent and independent cytotoxicity of potent quinone Cdc25 phosphatase inhibitors; J. Pharmacol. Exp. Ther., 309 64
4) Brisson et al. (2005), Redox regulation of Cdc25B by cell-active quinolonediones; Mol. Pharmacol., 68 1810 |
|
| Company Name: |
Sigma-Aldrich
|
| Tel: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
| Company Name: |
Twochem Co.Ltd.
|
| Tel: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
| Company Name: |
DC Chemicals
|
| Tel: |
021-58447131 13564518121 |
| Website: |
http://www.is0513.com/ShowSupplierProductsList927327/0.htm |
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