中文名称:

STAT5 Inhibitor

中文同义词:

STAT5抑制剂(STAT5-IN-1);STAT5抑制剂;化合物STAT5 INHIBITOR

英文名称:

STAT5 Inhibitor

英文同义词:

STAT5 Inhibitor;CS-2509;STAT5-IN-1;N-[(4-oxo-4H-chromen-3-yl)methylene]nicotinohydrazide;STAT5 Inhibitor 1;(E)-N-((4-oxo-4H-chromen-3-yl)methylene)nicotinohydrazide;MDK6314;3-Pyridinecarboxylic acid, 2-[(4-oxo-4H-1-benzopyran-3-yl)methylene]hydrazide

CAS号:

285986-31-4

分子式:

C16H11N3O3

分子量:

293.28

EINECS号:

604-604-1

相关类别:

细胞生物学试剂

Mol文件:

285986-31-4.mol

熔点 

214-216 °C

密度 

1.33±0.1 g/cm3(Predicted)

储存条件 

Keep in dark place,Sealed in dry,2-8°C

酸度系数(pKa)

10.44±0.46(Predicted)

生物活性

STAT5-IN-1 是一种有效的选择性 STAT5 抑制剂，其对于STAT5β亚型的IC50值为47 μM。

靶点

Target Value STAT5β (Cell-free assay) 47 μM

Target

Value

STAT5β (Cell-free assay)

47 μM

体外研究

The signal transducer and activator of transcription 5 (STAT5) is a member of the STAT family of proteins, implicated in cell growth and differentiation. STAT5-IN-1 inhibits STAT5 by binding to the SH2 domain. The functions of the SH2 domains of STAT3, STAT1, and of the tyrosine kinase Lck are inhibited to a lesser extent (IC50>500 µM). STAT5-IN-1 block STAT5/STAT5 DNA binding in K562 nuclear extracts. Substitution of the hydrogen at C6 of the chromone ring by an ethyl group does not affect activity of STAT5-IN-1 against STAT5β, but leads to complete loss of selectivity against other STAT family members.