中文名称:

1982372-88-2

中文同义词:

SUV420H1和SUV420H2化学抑制剂(A-196);A-196游离态;化合物A196

英文名称:

A-196

英文同义词:

A-196;A-196;A 196;A196;A-196 (A196;6,7-Dichloro-N-cyclopentyl-4-(4-pyridinyl)-1-phthalazinamine;1-Phthalazinamine, 6,7-dichloro-N-cyclopentyl-4-(4-pyridinyl)-;SGC A-196

CAS号:

1982372-88-2

分子式:

C18H16Cl2N4

分子量:

359.25

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

1982372-88-2.mol

沸点 

584.6±45.0 °C(Predicted)

密度 

1.399±0.06 g/cm3(Predicted)

储存条件 

2-8°C

形态

powder

酸度系数(pKa)

3.96±0.30(Predicted)

颜色

white to light brown

生物活性

A-196 是一种有效的选择性的 SUV420H1 和 SUV420H2 抑制剂，其 IC50 值分别为 25 nM 和 144 nM。A-196 以底物竞争性方式抑制 SUV4-20，也是一种 SUV4-20 的化学探针，用于研究组蛋白甲基转移酶在基因组完整性中的作用。

靶点

IC50: 25 nM (SUV420H1) and 144 nM (SUV420H2).

体外研究

A-196 (0-5 μM; 48 hours; U2OS cells) treatment results in an increase in H4K20me1 ( EC 50 value of 735 nM) and a decrease in both H4K20me2 and H4K20me3 ( EC 50 values of 262 and 370 nM, respectively). A-196 (10 μM; 72 hours; Wild-type, Suv4-20h double knockout and inhibitortreated mouse embryonic fibroblast cells) inhibits both SUV4-20 enzymes in cells in multiple tissue types without overt toxicity. Western Blot Analysis Cell Line: U2OS cells Concentration: 0 μM, 0.075 μM, 0.15 μM, 0.3 μM, 0.6 μM, 1.25 μM, 2.5 μM, 5 μM Incubation Time: 48 hours Result: Increased in H4K20me1 and decreased in both H4K20me2 and H4K20me3.

Cell Line:

U2OS cells

Concentration:

0 μM, 0.075 μM, 0.15 μM, 0.3 μM, 0.6 μM, 1.25 μM, 2.5 μM, 5 μM

Incubation Time:

48 hours

Result:

Increased in H4K20me1 and decreased in both H4K20me2 and H4K20me3.

危险品运输编号 

UN 2811 6.1 / PGIII