产品说明
一般描述
A cell-permable, potent, irreversible, and competitive inhibitor of the Cdc25 phosphatase family (Ki = 29 nM, 95 nM, and 89 nM for Cdc25A, Cdc25B2, and Cdc25C, respectively) with anti-proliferative properties. Displays nearly 20- and 450-fold greater selectivity over VHR and PTP1B (IC50 = 4.0 µM and >100 µM, respectively). Reported to arrest cell cycle progression, inhibit Cdk dephosphorylation, and delay tumor growth (mean IC50 = 1.5 µM in NCI-60 tumor cell panel). Also shown to block ERK dephosphorylation caused by ectopic Cdc25A expression.
A cell-permeable 7-substituted quinolinedione compound that displays antiproliferative properties. Acts as a potent, irreversible and mixed competitive inhibitor of the CDC25 phosphatase family (Ki = 29 nM, 95 nM and 89 nM for CDC25A, CDC25B2 and CDC25C, respectively; IC50 = 210 nM for CDC25B2) and displays nearly 20- and 450-fold greater selectivity for the CDC252 phosphatases over VHR and PTP1B (IC50 = 4.0 µM and >100 µM, respectively). Reported to arrest cell cycle progression, inhibit Cdk dephosphorylation and delay tumor growth (IC50 = ~1.5 µM in NCI-60 tumor cell panel). Shown to modify CDC25A catalytic domain and to block cellular ERK dephosphorylation in HeLa-CDC25A cells.
包装
5 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Primary Target
CD25A
Product does not compete with ATP.
Reversible: no
Target Ki: 29 nM, 95 nM and 89 nM for CDC25A, CDC25B2 and CDC25C, respectively; 210 nM for CDC25B2
警告
Toxicity: Carcinogenic / Teratogenic (D)
重悬
Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 1 month at -20°C. Ethanol stock solutions are stable for up to 6 months at -20°C.
其他说明
Chao, J. I., et al. 2004. J. Biol. Chem.279, 20267.
Han, Y., et al. 2004. J. Pharmacol. Exp. Ther.309, 64.
Pu, L., et al. 2002. J. Biol. Chem.277, 46877.
Lazo, J.S., et al. 2001. J. Med. Chem.44, 4042.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C15H16ClN3O3 |
分子量 | 321.76 |
MDL编号 | MFCD08276924 |
产品性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
颜色 | red |
溶解性 | DMSO: 5 mg/mL (Use only fresh, anhydrous DMSO.) ethanol: 5 mg/mL |
运输 | ambient |
储存温度 | 2-8℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
闪点(F) | 470.1 °F |
闪点(C) | 243.4 ℃ |
Sigma-Aldrich