Figure 2: GK921 inhibits TGase 2 in vitro and in cancer cells. (A) GK921 was tested for specific TGase 2 inhibition in vitro. The GK921 IC50 was 7.71μM using human recombinantTGase 2 and putrescine as a substrate, which resulted in about 2-fold increase of efficacy to compare to GK13 (IC50: 16.4μM). (B) Competition assay showing inhibition of TGase 2-mediated I-κBα polymerization by GK921. (C) Competition assay showing inhibition of TGase 2-mediated p53 polymerization by GK921. Data represent three independent experiments.