1627710-50-2
中文名称
2,6-二氟-4-[4-[4-(4-甲基-1-哌嗪基)苯基]-3-吡啶基]苯酚
英文名称
1627710-50-2
CAS
1627710-50-2
分子式
C22H21F2N3O
分子量
381.42
MOL 文件
1627710-50-2.mol
更新日期
2024/07/04 11:32:52
1627710-50-2 结构式
基本信息
中文别名
RSK抑制剂(LJH685)2,6-二氟-4-[4-[4-(4-甲基-1-哌嗪基)苯基]-3-吡啶基]苯酚
英文别名
LJH685CS-2182
LJH685(LJH-685)
LJH-685
LJH 685
LJH685
2,6-Difluoro-4-[4-[4-(4-methyl-1-piperazinyl)phenyl]-3-pyridinyl]phenol
Phenol, 2,6-difluoro-4-[4-[4-(4-methyl-1-piperazinyl)phenyl]-3-pyridinyl]-
所属类别
生物化工：激动剂抑制剂物理化学性质
沸点481.1±45.0 °C(Predicted)
密度1.257±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度溶于二甲基亚砜
酸度系数(pKa)5.86±0.25(Predicted)
形态结晶固体
颜色White to off-white
常见问题列表
生物活性
LJH685 是一种有效的选择性，ATP-竞争性的 RSK 抑制剂, 抑制 RSK1/2/3 生物活性, IC50 为 6、5、4 nM。靶点
IC50: 6 nM (RSK1), 5 nM (RSK1), 4 nM (RSK1)
体外研究
LJH685 (0.01-100 μM; 72 hours) efficiently inhibits the growth of MDA-MB-231 and H358 cells in soft agar with EC 50 s of 0.73 and 0.79 μM, respectively. LJH685 (0.1-10 μM; 4 hours) efficiently reduces phosphorylation of YB1 at submicromolar concentrations and causes nearly complete inhibition at higher concentrations.
Cell Proliferation Assay
| Cell Line: | MDA-MB-231, H358 cells |
| Concentration: | 0.01, 0.1, 1, 10, 100 μM |
| Incubation Time: | 72 hours |
| Result: | The growth in soft agar was efficiently inhibited with EC 50 values of 0.73 and 0.79 μM in MDA-MB-231 and H358, respectively. |
Western Blot Analysis
| Cell Line: | MDA-MB-231, H358 cells |
| Concentration: | 0.1, 0.3, 1, 3, 10 μM |
| Incubation Time: | 4 hours |
| Result: | Efficiently reduced phosphorylation of YB1 at submicromolar concentrations and caused nearly complete inhibition at higher concentrations. |