Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK2656157 是一种ATP 竞争性的PERK 选择性抑制剂,IC50值为 0.9 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 278 | 现货 | ||
2 mg | ¥ 393 | 现货 | ||
5 mg | ¥ 659 | 现货 | ||
10 mg | ¥ 967 | 现货 | ||
25 mg | ¥ 1,560 | 现货 | ||
50 mg | ¥ 2,120 | 现货 | ||
100 mg | ¥ 3,870 | 现货 | ||
200 mg | ¥ 5,490 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 795 | 现货 |
产品描述 | GSK2656157 is a highly specific and ATP-competitive PERK inhibitor (IC50: 0.9 nM) in a cell-free assay. The selectivty is 500-fold higher against a panel of 300 kinases. |
靶点活性 | PERK:0.9 nM |
体外活性 | GSK2656157可抑制小鼠体内多种人移植瘤生长.GSK2656157(50 mg/kg,p.o.)处理8 h后,完全抑制phospho-PERK Thr980. GSK2656157(50/150 mg/kg,2次/天)剂量依赖性地抑制小鼠体内四种肿瘤模型生长,150 mg/kg可抑制54-114%肿瘤生长. |
体内活性 | GSK2656157(1 mM)可进行UPR诱导,并抑制de novo蛋白合成。GSK2656157下调6%的UPR相关基因(PPP1R15A,HERPUD1,DDIT3,C/EBP-β和ERN1),且有超过4倍的下调。GSK2656157预处理细胞可抑制PERK活化,且可使下游底物、phospho-eIF2a、ATF4和 CHOP减少(IC50:10-30 nM)。在无外源UPR诱导剂时,GSK2656157则不影响这些细胞的生长(IC50:6-25 mM)。 |
激酶实验 | Kinase assay: Inhibitory potency of GSK2656157 is measured using recombinant GST-PERK (536–1116 amino acids) with 6-His-full-length human eIF2a as a substrate. Kinase selectivity is evaluated using 27 kinases at GSK as well as a panel of 300 kinases. |
细胞实验 | Antiproliferative activity of GSK2656157 against multiple human tumor cell lines as well as primary human microvascular endothelial cells is evaluated in a 3-day proliferation assay using standard culture medium. In the absence of exogeneous UPR inducers, GSK2656157 has no significant effect on the growth of any of these cells with IC50 range of 6–25 mM. (Only for Reference) |
分子量 | 416.45 |
分子式 | C23H21FN6O |
CAS No. | 1337532-29-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 30 mg/mL (72 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4012 mL | 12.0062 mL | 24.0125 mL | 60.0312 mL |
5 mM | 0.4802 mL | 2.4012 mL | 4.8025 mL | 12.0062 mL | |
10 mM | 0.2401 mL | 1.2006 mL | 2.4012 mL | 6.0031 mL | |
20 mM | 0.1201 mL | 0.6003 mL | 1.2006 mL | 3.0016 mL | |
50 mM | 0.048 mL | 0.2401 mL | 0.4802 mL | 1.2006 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。
GSK2656157 1337532-29-2 Apoptosis Autophagy PERK PKR-like endoplasmic reticulum kinase GSK 2656157 Protein kinase R-like endoplasmic reticulum kinase Inhibitor GSK-2656157 inhibit inhibitor