BN82002

BN82002 is a synthetic inhibitor of CDC25 phophatases, with IC50s of 2.4-6.3 μM for recombinant CDC25 phosphatases.

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphatase

Research Areas >> Cancer

IC50: 2.4 μM (CDC25A), 3.9 μM (CDC25B2), 6.3 μM (CDC25B3), 5.4 μM (CDC25C), 4.6 μM (CDC25C-cat)[1].

The effect of BN82002 on cell proliferation is evaluated in vitro on several human tumor cell lines. Menadione, which has been reported to inhibit cell proliferation, is used as a control. All of the examined cell lines are sensitive to BN82002 and Menadione in a concentration-dependent manner in the low micromolar range. The most sensitive is the pancreatic cancer cell line MIA PaCa-2 with an IC50 of 7.2 μM, and the less sensitive cell line is the colon cancer HT-29 with an IC50 of 32.6 μM. The range of activity is very similar to the one observed with menadione (5-15 μM). It is also showed that 50 μM BN82002 is a concentration that fully inhibits cell proliferation, the cell cycle distribution is only modestly affected with a slight decrease in S phase and an increase in cells containing both a G1 and a G2 DNA content, suggesting that the cells treated with BN82002 are arrested at various stages of the cell cycle[1].

[1]. Brezak MC, et al. A novel synthetic inhibitor of CDC25 phosphatases: BN82002. Cancer Res. 2004 May 1;64(9):3320-5.

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