| 规格 | 价格 | 库存 | 数量 | 操作 |
|---|---|---|---|---|
| 1mg | ¥585.00 | 现货 | 1 | |
| 2mg | ¥900.00 | 现货 | 1 | |
| 5mg | ¥1,710.00 | 现货 | 1 | |
| 10mg | ¥2,520.00 | 现货 | 1 | |
| 50mg | ¥6,300.00 | 现货 | 1 | |
| 100mg | ¥10,800.00 | 现货 | 1 | |
| 10mM (in 1mL DMSO) | ¥1,705.00 | 现货 | 1 |
GK921 is an inhibitor of transglutaminase 2 (TG2; IC50 = 7.71 ?M).1 It is cytotoxic against a panel of eight renal cell carcinoma (RCC) cell lines (mean GI50 = 0.905 ?M). GK921 (8 mg/kg) suppresses tumor growth in ACHN and Caki-1 RCC mouse xenograft models.
1.Ku, B.M., Kim, S.-J., Kim, N., et al.Transglutaminase 2 inhibitor abrogates renal cell carcinoma in xenograft modelsJ. Cancer Res. Clin. Oncol.140(5)757-767(2014)
Kinase experiment: | 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 |
Cell experiment: | 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]. |
Animal experiment: | Mice: GK921 is dissolved in DMSO. Vehicle alone and GK921 (8 mg/kg) are administered orally once per day, 5 days/week, for 64 days. The size of the primary tumors is measured every 2-3 days using calipers. Tumor volume is calculated[1]. |
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. |
