CDC25 Phosphatase Inhibitor II, NSC 663284

A cell-permable, potent, irreversible, and competitive inhibitor of the Cdc25 phosphatase family (K_i = 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 (K_i = 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.

Cell permeable: yes

Primary Target
CD25A

Product does not compete with ATP.

Reversible: no

Target K_i: 29 nM, 95 nM and 89 nM for CDC25A, CDC25B2 and CDC25C, respectively; 210 nM for CDC25B2

Packaged under inert gas

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.

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.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Carcinogenic / Teratogenic (D)