BN82002 hydrochloride |
| Catalog No.GC63788 |
El clorhidrato de BN82002 es un inhibidor potente, selectivo e irreversible de la familia de fosfatasa CDC25. El clorhidrato de BN82002 inhibe CDC25A, CDC25B2, CDC25B3, CDC25C CDC25A y 25C-cat con valores IC50 de 2,4, 3,9, 6,3, 5,4 y 4,6 μM, respectivamente. El clorhidrato de BN82002 muestra una selectividad ~20 veces mayor que la tirosina fosfatasa CD45.
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Cas No.: 1049740-43-3
Sample solution is provided at 25 µL, 10mM.
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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].
[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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