半岛bd体育手机客户端 说明
一般描述
A cell-permeable isothiazolopyridine based compound that acts as a high-affinity binding, reversible and ATP-competitive inhibitor of cyclin G associated kinase (GAK;Kd= 8.3 nM). Displays moderate to excellent selectivity over Kit, PDGFRβ, Flt3, Mek5 & PDGFRα (Kd= 29, 70, 110, 150 & 220 nM, respectively) in a 456-kinase profiling. Shown to dose-dependently disrupt both HCV entry & assembly and efficiently arrest HCV infection (EC50= 2.55 & 3.6 ?M in HCVcc- & HCVpp-infected Huh-7.5 cells, respectively; CC50= 23.27 ?M in HCVcc-infected Huh-7.5 cells). Significantly inhibits intracellular & extracellular infectivity (EC50= 1.64 & 2.13 ?M, respectively) and AP2M1 phosphorylation. Exerts no effect on HCV RNA replication.
生化/生理作用
Cell permeable: yes
Secondary Target
Kit, PDGFRβ, Flt3, Mek5 & PDGFRα
Primary Target
GAK
Reversible: yes
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Kovackova, S., et al. 2015.J. Med. Chem.58,3393.
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 | C19H21N3O4S |
分子量 | 387.45 |
半岛bd体育手机客户端 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 | yellow |
溶解性 | DMSO: 50 mg/mL |
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) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich