CDC25 Phosphatase Inhibitor I

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BN82002 是 CDC25 磷酸酶的合成抑制剂。

BN-82002, also known as CDC25 Phosphatase Inhibitor I, is a cell-permeable ortho-hydroxybenzylamino compound that displays anti-tumor properties. BN-82002 acts as a potent, selective, and irreversible inhibitor of CDC25 phosphatase family (IC50 = 2.4, 3.9, 6.3, 5.4, and 4.6 μM for 25A, 25B2, 25B3, 25C, and 25C-cat, respectively). BN82002 inhibits the phosphatase activity of recombinant human CDC25A, B, and C in vitro. It impairs the proliferation of tumoral cell lines and increases cyclin-dependent kinase 1 inhibitory tyrosine phosphorylation. In synchronized HeLa cells, BN82002 delays cell cycle progression at G1-S, in S phase and at the G2-M transition.

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.

——

BN-82002 | CDC25 Phosphatase Inhibitor I | PTP Inhibitor XX |

Metabolic Enzyme/Protease

Phosphatase

CDC25A|CDC25B2|CDC25B3|CDC25C|CDC25C-cat

——

——

396073-89-5

359.42

C19H25N3O4

>98% (HPLC)

DMSO : ≥ 150 mg/mL; 417.34 mM

Oc1c(cc(cc1OC)N(C)C)CN(C)CCc2ccc(cc2)[N+]([O-])=O

Phenol, 4-(dimethylamino)-2-methoxy-6-((methyl(2-(4-nitrophenyl)ethyl)amino)methyl)-

(-20℃)

With Ice Pack

≥ 2 years