BN82002

396073-89-5

C19H25N3O4

DMSO : >= 150 mg/mL (417.34 mM)

Metabolic Enzyme/Protease

BN82002 is a synthetic inhibitor of CDC25 phophatases, with IC₅₀s of 2.4-6.3 uM for recombinant CDC25 phosphatases. IC50 & Target: IC50: 2.4 uM (CDC25A), 3.9 uM (CDC25B2), 6.3 uM (CDC25B3), 5.4 uM (CDC25C), 4.6 uM (CDC25C-cat)^[1]. In Vitro: 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 uM, and the less sensitive cell line is the colon cancer HT-29 with an IC₅₀ of 32.6 uM. The range of activity is very similar to the one observed with menadione (5-15 uM). It is also showed that 50 uM 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].