CSN-B

中文名称:

CSN-B

中文同义词:

NUR77激动剂(CYTOSPORONE B);化合物CYTOSPORONE B

英文名称:

Csn-B

英文同义词:

3,5-Dihydroxy-2-(1-oxooctyl)benzeneacetic acid ethyl ester;3,5-Dihydroxy-2-(1-oxooctyl)-benzeneacetic acid, ethyl ester;Csn-B;Cytosporone B;ethyl 2-(3,5-dihydroxy-2-octanoylphenyl)acetate;Benzeneacetic acid, 3,5-dihydroxy-2-(1-oxooctyl)-, ethyl ester;N-{2-[(3-CYANO-5,7-DIMETHYL-2-QUINOLINYL)AMINO]ETHYL}-3-METHOXYBENZAMIDE;Ethyl 3,5-dihydroxy-2-(1-oxooctyl)-benzeneacetate

CAS号:

321661-62-5

分子式:

C18H26O5

分子量:

322.4

EINECS号:

相关类别:

细胞生物学试剂;对照品;抑制剂

Mol文件:

321661-62-5.mol

沸点 

471.6±24.0 °C(Predicted)

密度 

1.126±0.06 g/cm3(Predicted)

储存条件 

-20°C

溶解度 

DMSO: >20mg/mL

酸度系数(pKa)

7.54±0.40(Predicted)

颜色

white to off-white

生物活性

Cytosporone B是天然存在的核孤儿受体Nur77(NR4A1) 激动剂，EC50为0.278 nM。

靶点

Target Value Nur77 (Cell-free assay) 0.278 nM(EC50)

Target

Value

Nur77 (Cell-free assay)

0.278 nM(EC50)

体外研究

Cytosporone B targets the ligand binding domain of Nur77, which selectively stimulates the transactivational activity of Nur77. Cytosporone B induces luciferase activity in cells that are cotransfected with GAL4- Nur77 or GAL4-LBD. The EC 50 of cytosporone B for Nur77 is 0.278 nM. Cytosporone B displays robust pro-apoptotic activity in gastric cancer cells BGC-823. 63.5% of the cells are apoptotic when treated with cytosporone B for 48 h. Cytosporone B shows selective effect on cancerous cells. Cytosporone B inhibits proliferation of human gastric cancer BGC-823 cells and human colon cancer SW620 cells by 470%, but it has a modest effect on human lung cancer H1299 cells and human hepatoma HepG2 cells.

体内研究

In the hepatocytes of wild-type mice, the transcriptional activity of the reporter is induced five-fold with cytosporone B treatment. In wild-type mice, cytosporone B treatment significantly increases glucose levels from 3.2 to 11.4 mM within the first 30 min, and thereafter blood glucose gradually decreased before reaching the initial level after 300 min.

危险品标志 

Xn

危险类别码 

22

WGK Germany 

3