CDC25 Phosphatase Inhibitor II, NSC 663284 CAS: 383907-43-5
MF: C15H16ClN3O3
MW: 321.76
A competitive CDC25 inhibitor and cell cycle arresting compound.

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

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Nombres Alternativos: 6-chloro-7-[[2-(4-morpholinyl)ethyl]amino]-5,8-quinolinedione; DA-3003-1; SPS8I1
Solicitud: CDC25 Phosphatase Inhibitor II, NSC 663284 is a competitive CDC25 inhibitor and cell cycle arresting compound
Número de CAS: 383907-43-5
Pureza: ≥98%
Peso Molecular: 321.76
Fórmula Molecular: C15H16ClN3O3
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
* En el Certificado de Análisis específico de lote, puede encontrar información específica (como el contenido en agua).
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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

Estado de Materia :
Solid
Solubilidad :
Soluble in DMSO (50 mM), ethanol (50 mM), DMF (~10 mg/ml), and PBS(pH 7.2) (~0.15 mg/ml). Insoluble in water.
ALMACENAMIENTO :
Store at 4° C
Punto de ebullición :
~478.8° C at 760 mmHg (Predicted)
Densidad :
~1.4 g/cm3 (Predicted)
Indice de Refracción :
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
Datos Ki :
Cdc25A: Ki= 29 nM; Cdc25C: Ki= 89 nM; Cdc25B2: Ki= 95 nM
Valores de pK :
pKb: 6.79 (Predicted)
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
WGK Alemania :
3
PubChem CID :
Número MDL :
MFCD08276924
SMILES :
C1COCCN1CCNC2=C(C(=O)C3=C(C2=O)N=CC=C3)Cl

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PMID: # 31130988  Rodríguez, A.|Naveja, JJ.|Torres, L.|García de Teresa, B.|Juárez-Figueroa, U.|Ayala-Zambrano, C.|Azpeitia, E.|Mendoza, L.|Frías, S.| et al. 2019. Front Genet. 10: 411.

PMID: # 30097580  Wu, C. et al. 2018. Nat Commun. 9: 3212.

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

PMID: # 27619510  Sci Rep. 6: 33272.

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