中文名称:

TCS PIM-1 1

中文同义词:

3-氰基-4-苯基-6-(3-溴-6-羟基苯基)-2(1H)-吡啶酮;PIM-1激酶抑制剂(TCS PIM-1 1);6-(5-溴-2-羟基苯)-2-氧代-4-苯基-1,2-二氢吡啶-3-腈

英文名称:

3-Cyano-4-phenyl-6-(3-bromo-6-hydroxy)phenyl-2(1H)-pyridone

英文同义词:

3-Cyano-4-phenyl-6-(3-bromo-6-hydroxy)phenyl-2(1H)-pyridone;TCS PIM-1 1;SC 204330;6-(5-Bromo-2-hydroxyphenyl)-1,2-dihydro-2-oxo-4-phenyl-3-pyridinecarbonitrile;TCS PIM-1;TCS PIM-1 1, >=98%;SC 204330; TCS PIM 1-1;CS-1482

CAS号:

491871-58-0

分子式:

C18H11BrN2O2

分子量:

367.2

EINECS号:

相关类别:

细胞生物学试剂;小分子抑制剂;小分子抑制剂，天然产物;抑制剂;Inhibitors

Mol文件:

491871-58-0.mol

沸点 

592.6±50.0 °C(Predicted)

密度 

1.63±0.1 g/cm3(Predicted)

储存条件 

Store at +4°C

酸度系数(pKa)

6.93±0.10(Predicted)

生物活性

TCS PIM-1 1 (SC 204330)是一种有效的、选择性的 ATP-competitive Pim-1 kianse 抑制剂，其IC50值为50 nM，对 Pim-2 和 MEK1/MEK2 具有良好的选择性（IC50> 20000 nM）。

靶点

Target Value Pim1 (Cell-free assay) 50 nM

Target

Value

Pim1 (Cell-free assay)

50 nM

体外研究

TCS PIM-1 1 (compound 1), a substituted pyridone scaffold, binds convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggests that TCS PIM-1 1 lacked in vitro inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2. Hence, small molecules similar to TCS PIM-1 1 may serve as useful starting scaffolds for the development of other improved yet selective Pim-1 inhibitors. TCS PIM-1 1 serves both as a starting point for SAR chemical syntheses and was used for co-crystallization with Pim-1 protein.