3-[(2,7-二甲氧基吖啶-9-基)硫基]丙胺

中文名称:

3-[(2,7-二甲氧基吖啶-9-基)硫基]丙胺

中文同义词:

3-[(2,7-二甲氧基吖啶-9-基)硫基]丙胺;HASPIN抑制剂(LDN-192960);3-[(2,7-二甲氧基吖啶-9-基)硫基]丙-1-胺;3-(2,7-二甲氧基AC啶-9-基硫基)丙-1-胺

英文名称:

LDN-192960

英文同义词:

LDN-192960;LDN-192960 3-(2,7-diMethoxyacridin-9-ylthio)propan-1-aMine;3-[(2,7-Dimethoxy-9-acridinyl)thio]-1-propanamine dihydrochloride;CS-613;3-[(2,7-Dimethoxyacridin-9-yl)thio]propan-1-amine dihydrochloride;LDN-192960 dihydrochloride;1-Propanamine, 3-[(2,7-dimethoxy-9-acridinyl)thio]-;LDN-192960 2HCl

CAS号:

184582-62-5

分子式:

C18H20N2O2S

分子量:

328.43

EINECS号:

相关类别:

细胞生物学试剂;其它

Mol文件:

184582-62-5.mol

沸点 

536.1±40.0 °C(Predicted)

密度 

1.25±0.1 g/cm3(Predicted)

储存条件 

2-8°C

溶解度 

DMSO: soluble20mg/mL, clear

形态

powder

酸度系数(pKa)

9.33±0.10(Predicted)

颜色

white to light brown

生物活性

LDN-192960 是 Haspin 和 DYRK2 的双重抑制剂，IC50 值分别为 10 nM 和 48 nM。

靶点

IC50: 10 nM (Haspin); 48 nM (DYRK2)

体外研究

LDN-192960 (10 μM) is selective and inhibits ten of the other kinases by ≥90%, with only five being potently inhibited (IC 50 <1 μM), including CLK1 (IC 50 =0.21 μM), DYRK1A (IC 50 = 0.10 μM), DYRK2 (IC 50 =2 nM), DYRK3 (IC 50 =19 nM) and PIM1 (IC 50 =0.72 μM).LDN-0192960 (0-5 μM; 2 hours) demonstrates that the classical Haspin inhibition phenotype by reducing levels of p-Thr3H3 in HeLa cells overexpressing Haspin with an EC 50 of 1.17 μM.LDN-0192960 (0-1 μM; 1 hour incubation in the presence of nocodazole and MG132) demonstrates the classical Haspin inhibition phenotype by reducing levels of p-Thr3H3 in HeLa cells synchronized in mitosis with an EC 50 of 0.02 μM.

危险品标志 

Xi

危险类别码 

36/37/38

安全说明 

26

WGK Germany 

3