| 产品描述： | GSK2656157 is a selective and ATP-competitive inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) with an IC50 of 0.9 nM. |
| 靶点： |
EIF2AK3 (PERK):0.9 nM (IC50);EIF2AK1 (HRI):460 nM (IC50);BRK:905 nM (IC50);EIF2AK2 (PKR):905 nM (IC50);MEKK3:954 nM (IC50);Aurora B:1259 nM (IC50);KHS:1764 nM (IC50);LCK:2344 nM (IC50);MLK2:2796 nM (IC50);MEKK3:2847 nM (IC50);ALK5:3020 nM (IC50);MLCK2:3039 nM (IC50);EIF2AK4(GCN2):3162 nM (IC50);c-MER:3431 nM (IC50);PI3Kγ:3802 nM (IC50);WNK3:5951 nM (IC50);LRRK2:6918 nM (IC50);ROCK1:7244 nM (IC50);MSK1:8985 nM (IC50);NEK1:9807 nM (IC50);AXL:9808 nM (IC50);JAK2:24547 nM (IC50);Apoptosis;PERK;Autophagy |
| 体内研究： |
GSK2656157 (1.5-150 mg/kg, p.o.) results in dose-dependent inhibition of phospho-PERK Thr980, with more than 80% inhibition at 50 and 150 mg/kg. GSK2656157 (50-150 mg/kg, p.o.) results in dose-dependent inhibition of tumor growth in human tumor xenograft models |
| 参考文献： |
1. Atkins C, et al. Characterization of a novel PERK kinase inhibitor with antitumor and antiangiogenic activity. Cancer Res. 2013 Mar 15;73(6):1993-2002. 2. Krishnamoorthy J, et al. Evidence for eIF2α phosphorylation-independent effects of GSK2656157, a novel catalytic inhibitor of PERK with clinical implications. Cell Cycle. 2014 Mar 1;13(5):801-6. 3. Ando T, et al. GSK2656157, a PERK inhibitor, reduced LPS-induced IL-1β production through inhibiting Caspase 1 activation in macrophage-like J774.1 cells. Immunopharmacol Immunotoxicol. 2016 Aug;38(4):298-302. 4. Zhao Q, et al. Thioredoxin-interacting protein links endoplasmic reticulum stress to inflammatory brain injury and apoptosis after subarachnoid haemorrhage. J Neuroinflammation. 2017 May 11;14(1):104. |
| 溶解性： |
1M HCl : 100 mg/mL (240.12 mM; ultrasonic and adjust pH to 1 with HCl) DMSO : 8.33 mg/mL (20.00 mM; Need ultrasonic) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.401 ml |
12.006 ml |
24.012 ml |
| 5 mM |
0.48 ml |
2.401 ml |
4.802 ml |
| 10 mM |
0.24 ml |
1.201 ml |
2.401 ml |
| 50 mM |
0.048 ml |
0.24 ml |
0.48 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京