Molecular Formula | C21H20N4O |
Molar Mass | 344.41 |
Solubility | DMSO: ≥ 30 mg/mL |
Storage Condition | -20℃ |
In vitro study | 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. |
In vivo study | A single treatment with GK921 almost completely reduces tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.904 ml | 14.518 ml | 29.035 ml |
5 mM | 0.581 ml | 2.904 ml | 5.807 ml |
10 mM | 0.29 ml | 1.452 ml | 2.904 ml |
5 mM | 0.058 ml | 0.29 ml | 0.581 ml |
biological activity | GK921 is a transglutaminase 2 (TGase 2) inhibitor with an IC50 of 8.93 μm. |
Target | Value |
TGase 2 () | 8.93 μM |