Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK963 是手性的选择性受体相互作用蛋白 1 酶抑制剂,其IC50值为 29 nM。它在体外强效选择性抑制小鼠和人细胞的坏死。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 315 | 现货 | ||
2 mg | ¥ 453 | 现货 | ||
5 mg | ¥ 747 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 2,490 | 现货 | ||
50 mg | ¥ 3,930 | 现货 | ||
100 mg | ¥ 5,630 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 822 | 现货 |
产品描述 | GSK963 (Racemate), a structurally distinct, potent and selective inhibitor of RIP1 kinase(IC50=29 nM). |
靶点活性 | RIP1:29 nM |
体外活性 | The increased potency of GSK 963 relative to Nec-1 in vitro also translated into increased efficacy in the TNF+zVAD-induced model of sterile shock.?At a dose of 2 mg/kg, GSK 963 was able to completely inhibit temperature loss in response to TNF+zVAD, ?the phenotype of the recently described RIP1 kinase-dead knock-in mice.?The level of inhibition of temperature loss in this acute model at different doses of GSK 963 was in line with the predictions of efficacy based on modeling of the pharamacokinetic profile and in vitro potency of GSK 963. |
体内活性 | GSK 963 efficiently blocked necroptosis in both murine and human cells with IC50 values of 1 nM and 4 nM, respectively, whereas the inactive analog GSK 962 was at least 1000-fold less potent in these assays. |
激酶实验 | GSK′963 was tested against 339 kinases using a P33-radiolabeled assay at Reaction Corp Biology. The compound was tested at a single dose in duplicate at 10?μM. Reactions were carried out at 10?μM ATP. Data are reported as % enzyme activity (relative to DMSO controls). |
别名 | GSK963 (Racemate) |
分子量 | 230.31 |
分子式 | C14H18N2O |
CAS No. | 2049868-46-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 40 mg/mL (173.67 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 4.342 mL | 21.7099 mL | 43.4197 mL | 108.5493 mL |
5 mM | 0.8684 mL | 4.342 mL | 8.6839 mL | 21.7099 mL | |
10 mM | 0.4342 mL | 2.171 mL | 4.342 mL | 10.8549 mL | |
20 mM | 0.2171 mL | 1.0855 mL | 2.171 mL | 5.4275 mL | |
50 mM | 0.0868 mL | 0.4342 mL | 0.8684 mL | 2.171 mL | |
100 mM | 0.0434 mL | 0.2171 mL | 0.4342 mL | 1.0855 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。
GSK963 2049868-46-2 Apoptosis NF-Κb RIP kinase GSK 963 Inhibitor Receptor-interacting protein kinases inhibit RIPK GSK963 (Racemate) GSK-963 Racemate inhibitor