BN82002 hydrochloride is a potent, selective, and irreversible inhibitor of the CDC25 phosphatase family. It inhibits CDC25A, CDC25B2, CDC25B3, CDC25C, and 25C-cat with IC50 values of 2.4, 3.9, 6.3, 5.4, and 4.6 μM, respectively. Additionally, BN82002 hydrochloride exhibits approximately 20-fold greater selectivity over CD45 tyrosine phosphatase.

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

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 IC 50 of 7.2 μM, and the less sensitive cell line is the colon cancer HT-29 with an IC 50 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].