6-Chloro-7-(2-morpholin-4-yl-ethylamino)quinoline-5,8-dione
DA3003-1 Red solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. 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. CAS 383907-43-5. Ref.: 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. |
