BN82002 hydrochloride

• CAT Number: I045605
• CAS Number: 1049740-43-3
• Molecular Formula: C19H26ClN3O4
• Molecular Weight: 395.88
• Purity: ≥95%
• Synonyms: 4-(dimethylamino)-2-methoxy-6-[[methyl-[2-(4-nitrophenyl)ethyl]amino]methyl]phenol;hydrochloride
• InChI: InChI=1S/C19H25N3O4.ClH/c1-20(2)17-11-15(19(23)18(12-17)26-4)13-21(3)10-9-14-5-7-16(8-6-14)22(24)25;/h5-8,11-12,23H,9-10,13H2,1-4H3;1H
• InChIKey: FGPZRTQNJSSCAQ-UHFFFAOYSA-N
• SMILES: CN(C)C1=CC(=C(C(=C1)OC)O)CN(C)CCC2=CC=C(C=C2)[N+](=O)[O-].Cl

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

Reference

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