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

中文同义词:

2,6-二氟-4-[4-[4-(4-甲基-1-哌嗪基)苯基]-3-吡啶基]苯酚;RSK抑制剂(LJH685)

英文名称:

1627710-50-2

英文同义词:

LJH685;2,6-Difluoro-4-[4-[4-(4-methyl-1-piperazinyl)phenyl]-3-pyridinyl]phenol;LJH685(LJH-685);LJH-685;LJH 685;LJH685;CS-2182;Phenol, 2,6-difluoro-4-[4-[4-(4-methyl-1-piperazinyl)phenyl]-3-pyridinyl]-

CAS号:

1627710-50-2

分子式:

C22H21F2N3O

分子量:

381.42

EINECS号:

相关类别:

细胞生物学试剂;抑制剂

Mol文件:

1627710-50-2.mol

沸点 

481.1±45.0 °C(Predicted)

密度 

1.257±0.06 g/cm3(Predicted)

酸度系数(pKa)

5.86±0.25(Predicted)

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.

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.

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.