DA-3003-2

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. Lazo, J.S., Aslan, D.C., Southwick, E.C., et al. 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. Lavecchia, A., Cosconati, S., Limongelli, V., et al. Modeling of Cdc25B dual specifity protein phosphatase inhibitors: Docking of ligands and enzymatic inhibition mechanism. ChemMedChem 1(5), 540-550 (2006).

3. Nemoto, K. G₂/M accumulation in prostate cancer cell line PC-3 is induced by Cdc25 inhibitor 7-chloro-6-(2-morpholin-4-ylethylamino) quinoline-5, 8-dione (DA 3003-2). Exp. Ther. Med. 1(4), 647-650 (2010).