CDC25 Phosphatase Inhibitor I; BN82002

Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Target IC₅₀: 2.4, 3.9, 6.3, 5.4, and 4.6 µM for CDC25 phosphatase family 25A, 25B2, 25B3, 25C, and 25C-cat, respectively

Primary TargetCDC25A

Cell permeable: yes

General description

A cell-permeable ortho-hydroxybenzylamino compound that displays anti-tumor properties. Acts as a potent, selective, and irreversible inhibitor of CDC25 phosphatase family (IC₅₀ = 2.4, 3.9, 6.3, 5.4, and 4.6 µM for 25A, 25B2, 25B3, 25C, and 25C-cat, respectively). Displays ~20-fold greater selectivity for CDC25 phosphatases compared to CD45 tyrosine phosphatase. Shown to delay cell cycle progression in vitro (IC₅₀ in the range of 7.2-32.6 µM), and reduces tumor growth in athymic mice xenografted with the human pancreatic cell MIA PaCa-2 (15 mg/kg, i.p. route).

A cell-permeable ortho-hydroxybenzylamino compound that displays antitumor properties. Acts as a potent, selective and irreversible inhibitor of CDC25 phosphatase family (IC₅₀ = 2.4, 3.9, 6.3, 5.4, and 4.6 µM for 25A, 25B2, 25B3, 25C, and 25C-cat, respectively). Displays ~20-fold greater selectivity for CDC25 phosphatases over CD45 tyrosine phosphatase. Shown to delay cell cycle progression in vitro (IC₅₀ = ~7.2-32.6 µM), and reduces tumor growth in athymic mice xenografted with the human pancreatic cells MIA PaCa-2 (15 mg/kg, i.p. route).

Legal Information

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

Other Notes

Brezak, M.C., et al. 2004. Cancer Res.64, 3320.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Unstable in aqueous solution.

Warning

Toxicity: Standard Handling (A)