1982372-88-2

生物活性靶点体外研究 1982372-88-2 试剂级价格

1982372-88-2

CAS号:1982372-88-2
英文名:A-196
中文名:1982372-88-2
CBNumber:CB43051065
分子式:C18H16Cl2N4
分子量:359.25
MOL File:1982372-88-2.mol

1982372-88-2化学性质

沸点 :584.6±45.0 °C(Predicted)
密度 :1.399±0.06 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :Soluble in DMSO (up to 5 mg/ml)
酸度系数(pKa) :3.96±0.30(Predicted)
形态 :powder
颜色 :white to light brown
稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months.

安全信息

危险品运输编号 :UN 2811 6.1 / PGIII

1982372-88-2性质、用途与生产工艺

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.