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

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

The in vitro impact of BN82002 on the proliferation of various human tumor cell lines was assessed, employing Menadione, a known proliferation inhibitor, as a benchmark. BN82002 and Menadione were observed to inhibit proliferation across all tested cell lines in a concentration-dependent fashion within the low micromolar range. Particularly, the pancreatic cancer cell line MIA PaCa-2 demonstrated the highest sensitivity to BN82002 with an IC 50 of 7.2 μM, while the colon cancer cell line HT-29 exhibited the least sensitivity with an IC 50 of 32.6 μM. This sensitivity pattern closely mirrors that seen with Menadione (5-15 μM). Additionally, it was found that a 50 μM concentration of BN82002 effectively halted cell proliferation. However, this arrest saw only a slight shift in the cell cycle, characterized by a minor decrease in the S phase and a rise in cells at both G1 and G2 DNA content stages, indicating BN82002-induced arrest occurs at various cell cycle phases[1].