中文名称:

1025015-40-0

中文同义词:

转谷氨酰胺酶2(TGASE2)抑制剂(GK921);化合物GK921

英文名称:

GK921

英文同义词:

GK921;3-(phenylethynyl)-2-(2-(pyrrolidin-1-yl)ethoxy)pyrido[3,2-b]pyrazine;GK-921;GK 921;GK921, >98%;Pyrido[2,3-b]pyrazine, 3-(2-phenylethynyl)-2-[2-(1-pyrrolidinyl)ethoxy]-;3-(2-Phenylethynyl)-2-[2-(1-pyrrolidinyl)ethoxy]pyrido[2,3-b]pyrazine

CAS号:

1025015-40-0

分子式:

C21H20N4O

分子量:

344.41

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

1025015-40-0.mol

生物活性

GK921是transglutaminase 2 (TGase 2)抑制剂，IC50为8.93 μM。

靶点

Target Value TGase 2 () 8.93 μM

Target

Value

TGase 2 ()

8.93 μM

体外研究

GK921 inhibits the TGase 2-induced polymerization of I-κBα and p53 in a dose-dependent manner. The cytotoxicity of GK921 ranged from GI 50 of 10 -10 to 10 -4 M. The average GI 50 is 9.05×10 -7 M. GK921 rescues p53 levels and consequently induces apoptosis; a concentration-dependent increase in cleaved poly(ADP-ribose) polymerase (c-PARP) and p53 levels is observed.

体内研究

A single treatment with GK921 almost completely reduces tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models.