108477-18-5

中文名称:

108477-18-5

中文同义词:

半胱天冬酶和细胞凋亡激活剂(UBIQUITIN ISOPEPTIDASE INHIBITOR I, G5)

英文名称:

4H-Thiopyran-4-one,tetrahydro-3,5-bis[(4-nitrophenyl)methylene]-1,1-dioxide

英文同义词:

4H-Thiopyran-4-one,tetrahydro-3,5-bis[(4-nitrophenyl)methylene]-1,1-dioxide;NSC-144303;Ubiquitin Isopeptidase Inhibitor I;Ubiquitin Isopeptidase Inhibitor I, G5;G5, Ubiquitin Isopeptidase Inhibitor I;Ubiquitin Isopeptidase-IN-G5;Ubiquitin Isopeptidase Inhibitor I, G5 (NSC144303)

CAS号:

108477-18-5

分子式:

C19H14N2O7S

分子量:

414.39

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

108477-18-5.mol

熔点 

233.5-234.5 °C

沸点 

693.0±55.0 °C(Predicted)

密度 

1.541±0.06 g/cm3(Predicted)

生物活性

Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303)是凋亡不依赖的半胱天冬酶和细胞凋亡的激活剂，对E1A和E1A/C9DN细胞的IC50值分别为1.76和1.6 μM。

靶点

IC50: 1.76 μM (E1A cells), 1.6 μM (E1A/C9DN cells)

体外研究

G5 is capable of activating an apoptosome-independent apoptotic pathway. It targets the ubiquitinproteasome system by inhibiting the ubiquitin isopeptidases. G5 induces a rather unique apoptotic pathway, which includes a Bcl-2-dependent but apoptosome-independent mitochondrial pathway with upregulation of the BH3-only protein Noxa, stabilization of the inhibitor of apoptosis antagonist Smac, but also the involvement of the death receptor pathway. G5 is a potent apoptotic inducer showing IC 50 s of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively.