Description 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. A cell-permeable 7-substituted quinolinedione compound that displays antiproliferative properties. Acts as a potent, irreversible and mixed competitive inhibitor of the CDC25 phosphatase family (Ki = 29 nM, 95 nM and 89 nM for CDC25A, CDC25B2 and CDC25C, respectively; IC50 = 210 nM for CDC25B2) and displays nearly 20- and 450-fold greater selectivity for the CDC252 phosphatases 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 (IC50 = ~1.5 µM in NCI-60 tumor cell panel). Shown to modify CDC25A catalytic domain and to block cellular ERK dephosphorylation in HeLa-CDC25A cells. Packaging 5 mg in Plastic ampoule Biochem/physiol Actions Cell permeable: yes Primary Target CD25A Product does not compete with ATP. Reversible: no Target Ki: 29 nM, 95 nM and 89 nM for CDC25A, CDC25B2 and CDC25C, respectively; 210 nM for CDC25B2 Packaging Packaged under inert gas Warning Toxicity: Carcinogenic / Teratogenic (D) Reconstitution Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 1 month at -20°C. Ethanol stock solutions are stable for up to 6 months at -20°C. Other Notes Chao, J. I., et al. 2004. J. Biol. Chem.279, 20267. Han, Y., et al. 2004. J. Pharmacol. Exp. Ther.309, 64. Pu, L., et al. 2002. J. Biol. Chem.277, 46877. Lazo, J.S., et al. 2001. J. Med. Chem.44, 4042.