GK921 is a specific, orally active Transglutaminase 2 (TGase 2, TG2) inhibitor with IC50 of 7.71 uM against recombinant hTGase 2.
GK921 inhibits the TGase 2-induced polymerization of I-κBα and p53 in vitro in a dose-dependent manner, induces cell death of eight RCC lines with average GI50 of 0.9 uM.
GK921 almost completely reduces tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models.
GK921 blocks MES transdifferentiation and showed significant therapeutic efficacy in mouse models of glioma stem cells (GSC)
