中文名称:

N-[2-(2-吡啶基)-6-(1,2,4,5-四氢-3H-3-苯并氮杂卓-3-基)-4-嘧啶基]-BETA-丙氨酸

中文同义词:

N-[2-(2-吡啶基)-6-(1,2,4,5-四氢-3H-3-苯并氮杂卓-3-基)-4-嘧啶基]-BETA-丙氨酸;GSK J1(锂盐);KDM6A/KDM6B抑制剂(GSK-J1)

英文名称:

GSK J1

英文同义词:

GSK J1;GSK-J1;N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-beta-alanine;GCK J1;3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoic acid;N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyriMidinyl]-|-alanine;Histone Lysine Demethylase Inhibitor VII, GSK-J1;Histone Lysine Demethylase Inhibitor VII, GSK-J1 - CAS 1373422-53-7 - Calbiochem

CAS号:

1373422-53-7

分子式:

C22H23N5O2

分子量:

389.45

EINECS号:

200-258-5

相关类别:

抑制剂;活性分子;细胞生物学试剂;化工;API

Mol文件:

1373422-53-7.mol

沸点 

608.9±55.0 °C(Predicted)

密度 

1.292±0.06 g/cm3(Predicted)

储存条件 

2-8°C

溶解度 

DMSO: soluble15mg/mL, clear

酸度系数(pKa)

4.20±0.10(Predicted)

形态

powder

颜色

white to beige

InChIKey

AVZCPICCWKMZDT-UHFFFAOYSA-N

生物活性

GSK-J1 是 H3K27me3/me2-demethylases JMJD3/KDM6B 和 UTX/KDM6A 的抑制剂，对 KDM6B 的 IC50 值为 60 nM。

靶点

IC50: 60 nM (KDM6B)

体外研究

GSK-J1 is selective for H3K27 demethylases of the KDM6 subfamily and specifically binds to endogenous JMJD3. GSK-J1 inhibits TNF-α production by human primary macrophages in an H3K27-dependent manner. GSK-J1 inhibits the demethylase activity of KDM5C with 8.5-fold increased potency compared with that of KDM5B at 1 mM α-ketoglutarate, with IC 50 of 11 μM and 94 μM, respectively.

危险品标志 

Xi

危险类别码 

36/37/38

安全说明 

26

WGK Germany 

3