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Cdc25 dual-specific protein tyrosine phosphatases are important for cell cycle progression and often overexpressed in cancers. Through the removal of inhibitory phosphates, they function to catalyze the activation of cyclin-Cdk complexes. DA-3003-2 is a Cdc25 phosphatase inhibitor (IC50 = 0.82 µM for human recombinant Cdc25B) that demonstrates antiproliferative activity.1,2,3 At 20 µM, it has been shown to arrest asynchronous PC-3 prostate cancer cells in G2/M phase.3
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1. Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25. J. Med. Chem. 44(24), 4042-4049 (2001).
2. Modeling of Cdc25B dual specifity protein phosphatase inhibitors: Docking of ligands and enzymatic inhibition mechanism. ChemMedChem 1(5), 540-550 (2006).
3. G2/M accumulation in prostate cancer cell line PC-