CDC25 Phosphatase Inhibitor II, NSC 663284A competitive CDC25 inhibitor and cell cycle arresting compound

CDC25 Phosphatase Inhibitor II, NSC 663284 (CAS 383907-43-5)

CDC25 Phosphatase Inhibitor II, NSC 663284 | CAS 383907-43-5 is rated 5.0 out of 5 by 1.
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Synonym: 6-chloro-7-[[2-(4-morpholinyl)ethyl]amino]-5,8-quinolinedione; DA-3003-1; SPS8I1
Application: A competitive CDC25 inhibitor and cell cycle arresting compound
CAS Number: 383907-43-5
Purity: ≥98%
Molecular Weight: 321.76
Molecular Formula: C15H16ClN3O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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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 has been shown 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.


References

1. Lazo, J.S. et al. 2001. J. Med. Chem. 44(24): 4042-4049. PMID: 11708908
2. Pu, L. et al. 2002. J. Biol. Chem. 277(49): 46877-46885. PMID: 12356752
3. Chao, J.I. et al. 2004. J. Biol. Chem. 279(19): 20267-20276. PMID: 14988404
4. Han, Y. et al. 2004. J. Pharmacol. Exp. Ther. 309(1): 64-70. PMID: 14718602
5. Brisson, M. et al. 2005. Mol. Pharmacol. 68(6): 1810-1820. PMID: 16155209
6. Vogt, A. et al. 2008. Mol. Cancer Ther. 7(2): 330-340. PMID: 18245669

Physical State :
Solid
Solubility :
Soluble in DMSO (50 mM), ethanol (50 mM), DMF (~10 mg/ml), and PBS(pH 7.2) (~0.15 mg/ml). Insoluble in water.
Storage :
Store at 4° C
Boiling Point :
~478.8° C at 760 mmHg (Predicted)
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
n20D 1.63 (Predicted)
IC50 :
Cdc25B: IC50 = 0.21 µM (human); Cdc25C: IC50 = 0.25 µM (human); inhibit Cdk dephosphorylation: IC50 = 1.5 µM (NCI-60 tumor cell panel); VHR: IC50 = 4.0 µM
Ki Data :
Cdc25A: Ki= 29 nM; Cdc25C: Ki= 89 nM; Cdc25B2: Ki= 95 nM
pK Values :
pKb: 6.79 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
379077
MDL Number :
MFCD08276924
SMILES :
C1COCCN1CCNC2=C(C(=O)C3=C(C2=O)N=CC=C3)Cl

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Certificate of Analysis

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CDC25 Phosphatase Inhibitor II, NSC 663284  Product Citations

See how others have used CDC25 Phosphatase Inhibitor II, NSC 663284. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 24429874  Riemer, A. et al. 2014. Cell Cycle. 13: 919-27.

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from Guo Guo, J. et al. (PubMed 17970046) investigated the efficacy, pharmacokinetics, and metabolism of CDC25 phosphatase inhibitor, DA3003-1 (NSC 663284). DA3003-1 inhibited the growth of subcutaneous human colon HT29 xenografts in SCID mice. Following DA3003-1 treatment of tumor-bearing SCID mice, reduced glutathione concentrations in HT29 tumor was decreased to a greater extent and remained decreased for longer than the reduced glutathione concentrations in liver and kidneys. -SCBT Publication Review
Date published: 2015-07-08
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