GK921 is a transglutaminase 2 (TGase) inhibitor.

TGase 2:8.93 μM

GK921以剂量依赖的方式抑制TGase 2诱导的I-κBα和p53的聚合作用。GK921的细胞毒性范围，GI50为10^-10至10^-4 M，平均GI50为9.05×10^-7 M。GK921通过恢复p53水平从而诱导细胞凋亡。随着浓度的增加，裂解的多(ADP-核糖)聚合酶（c-PARP）和p53水平呈浓度依赖性上升[1]。

单次使用GK921通过稳定ACHN和CAKI-1预临床异种移植肿瘤模型中的p53几乎完全抑制了肿瘤生长，这表明了一种对抗RCC[1]的新治疗方法的可能性。

TGase 2 from guinea pig liver is preincubated for 10 min with various concentrations of GK13 or GK921 in 0.1 mL of reaction buffer, with or without 10 mM CaCl2, followed by the addition of 0.4 mL of substrate solution containing 2

Cells are transfected with a BAX promoter luciferase reporter construct. After exposure to GK921 (0, 0.5, 1, 2.5, 5 μM), firefly and Renilla luciferase activities are measured using a dual luciferase assay kit and pRL-CMV as an internal control[1].