产品说明
一般描述
A cell-permeable and reversible benzimidazolo compound that acts as a potent and ATP-competitive inhibitor of Chk2 with an IC50 of 15 nM and a Ki of 37 nM. Displays ~ 1,000-fold greater selectivity over Cdk1/B and CK1 (IC50 = 12 M and 17 M, respectively) and only weakly affects the activities of a panel of 31 kinases (<25% inhibition at 10 M), including Chk1. Shown to rescue both peripheral CD4+ and CD8+ T-cells from γ-irradiation-induced apoptosis with an EC50 of 3 M and 7.6 M, respectively. Also available as a 25 mM solution in DMSO (Cat. No. 220491).
A cell-permeable, potent, reversible and ATP-competitive inhibitor of Chk2 (checkpoint kinase 2; IC50 = 15 nM; Ki = 37 nM). Displays ~1,000-fold greater selectivity for Chk2 compared to Cdk1/cyclin B and CK1 (IC50 = 12 µM and 17 µM, respectively) and only weakly affects the activities of a panel of 31 kinases (<25% inhibition at 10 µM), including Chk1. Shown to rescue both peripheral CD4+ and CD8+ T-cells from γ-irradiation-induced apoptosis with an EC50 of 3 µM and 7.6 µM, respectively.
包装
1 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Primary Target
Chk2
Ki = 37 nM inhibiting Chk2.EC50 = 3 µM and 7.6 µM in rescuing both peripheral CD4+ and CD8+ T-cells from γ-irradiation-induced apoptosis
Target Ki: 37 nM inhibiting Chk2
Reversible: yes
Cell permeable: yes
Product competes with ATP.
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Arienti, K. L., et al. 2005. J. Med. Chem.48, 1873.
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 | C20H14ClN3O2 |
分子量 | 363.80 |
产品性质
质量水平 | 100 |
测定 | ≥95% (HPLC) |
形式 | solid |
效能 | 15 nM IC50 |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
颜色 | pale yellow |
溶解性 | DMSO: 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 |
Sigma-Aldrich