Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GK921 是一种转谷氨酰胺酶2 抑制剂,对人类重组TGase2的IC50=为7.71 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 835 | 现货 | ||
5 mg | ¥ 1,570 | 现货 | ||
10 mg | ¥ 2,268 | 现货 | ||
25 mg | ¥ 3,920 | 现货 | ||
50 mg | ¥ 5,450 | 现货 | ||
100 mg | ¥ 7,650 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,570 | 现货 |
产品描述 | GK921 is a transglutaminase 2 (TGase) inhibitor. |
靶点活性 | TGase 2:8.93 μM |
体外活性 | GK921 inhibits the TGase 2-induced polymerization of I-κBα and p53 in a dose-dependent manner. The cytotoxicity of GK921 ranged from GI50 of 10-10 to 10-4 M. The average GI50 is 9.05×10-7 M. GK921 rescues p53 levels and consequently induces apoptosis. The cleaved poly(ADP-ribose) polymerase (c-PARP) and p53 levels increase in a concentration-dependent manner[1]. |
体内活性 | A single treatment with GK921 almost completely reduces tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models which suggests the possibility of a new therapeutic approach to RCC[1]. |
激酶实验 | 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 |
细胞实验 | 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]. |
分子量 | 344.41 |
分子式 | C21H20N4O |
CAS No. | 1025015-40-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (159.69 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.9035 mL | 14.5176 mL | 29.0352 mL | 72.5879 mL |
5 mM | 0.5807 mL | 2.9035 mL | 5.807 mL | 14.5176 mL | |
10 mM | 0.2904 mL | 1.4518 mL | 2.9035 mL | 7.2588 mL | |
20 mM | 0.1452 mL | 0.7259 mL | 1.4518 mL | 3.6294 mL | |
50 mM | 0.0581 mL | 0.2904 mL | 0.5807 mL | 1.4518 mL | |
100 mM | 0.029 mL | 0.1452 mL | 0.2904 mL | 0.7259 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
GK921 1025015-40-0 Proteases/Proteasome Glutaminase GK 921 GK-921 inhibit Inhibitor inhibitor