| Description | GK921 is a transglutaminase 2 (TGase) inhibitor. |
| In vitro | 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]。 |
| In vivo | 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。 |
| Cell experiments | 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]. |
| Target activity | TGase 2:8.93 μM |
| molecular weight | 344.41 |
| Molecular formula | C21H20N4O |
| CAS | 1025015-40-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 55 mg/mL (159.69 mM) |
| References | 1. Ku BM, et al. Transglutaminase 2 inhibitor abrogates renal cell carcinoma in xenograft models. J Cancer Res Clin Oncol. 2014 May;140(5):757-67. |