GK921 is a transglutaminase 2 (TGase) inhibitor with an IC50 of 7.71 μM for human recombinant TGase 2.
IC50&Target
IC50: 7.71 μM (TGase)
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 GI50 of 10 to 10 M. The average GI50 is 9.05×10 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.
分子式
C21H20N4O
分子量
344.41
CAS号
1025015-40-0
运输条件
Room temperature in continental US; may vary elsewhere.