GK921

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GK921 是一种转谷氨酰胺酶 2 (TGase) 抑制剂。

GK921 is a transglutaminase 2 (TGase 2) inhibitor. GK921 showed cytotoxicity to RCC (average GI50 in eight RCC cell lines: 0.905 μM). A single treatment with GK921 almost completely reduced tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models. TGase 2 inhibitor GK921 abrogates RCC growth in xenograft tumor models, suggesting the possibility of a new therapeutic approach to RCC.

GK921 inhibits the TGase 2-induced polymerization of I-κBα and p53 in a dose-dependent manner. The cytotoxicity of GK921 ranged from GI50 of 10-10 to 10-4 M. The average GI50 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.

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

GK921 | GK-921 | GK 921

Others

Other Targets

TGase

Cancer

——

1025015-40-0

344.42

C21H20N4O

>98% (HPLC)

DMSO : ≥ 30 mg/mL 87.11 mM

C1CCN(C1)CCOc1c(nc2c(n1)cccn2)C#Cc1ccccc1

3-(phenylethynyl)-2-(2-(pyrrolidin-1-yl)ethoxy)pyrido[2,3-b]pyrazine

(-20℃)

With Ice Pack

≥ 2 years