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• 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。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *