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GSK2606414

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Chemical Structure| 1337531-36-8 同义名 : -
CAS号 : 1337531-36-8
货号 : A154425
分子式 : C24H20F3N5O
纯度 : 99%+
分子量 : 451.444
MDL号 : MFCD25976926
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(232.59 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 10 mg/mL clear

PO 0.5% CMC-Na 31 mg/mL suspension

生物活性
靶点

  • PERK

    EIF2AK3 (PERK), IC50:0.4 nM
描述 UPR (unfolded protein response), dysregulation of which has been implicated in many important pathologies, is an essential pathway to cope with ER stress. PERK is one of three primary effectors of the UPR. It can be activated by the released ER chaperones caused by increase of unfolded proteins in the ER and thus phosphorylates eIF2α. GSK2606414 is a potent and selective PERK inhibitor with IC50 value of 0.4nM (measured by cytoplasmic PERK domain phosphorylation of EIF2α). Treatment with GSK2606414 at concentration ranging in 0.03-0.3μM for 2h can significantly inhibit p-PERK induced by 1μM thapsigargin with IC50 value<0.03μM in A549 cells. Oral administration of GSK2606414 at dose of 50mg/kg and 150mg/kg, b.i.d., for 21 days showed antitumor activity in a human pancreatic tumor xenograft model[1].
作用机制 The trifluoromethyl meta-substituent of GSK2606414 can occupy the PERK kinase domain.[1]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human A549 cells Function assay 2 h Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells after 2 hrs by Western blotting 22827572
human A549 cells 0.03 μM Function assay 2 h Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells at 0.03 uM after 2 hrs by Western blotting 22827572
human A549 cells Function assay 1 h Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells preincubated for 1 hr followed by thapsigargin-induction measured after 1 hr by Western blotting analysis 24900593
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.22mL

0.44mL

0.22mL

11.08mL

2.22mL

1.11mL

22.15mL

4.43mL

2.22mL
参考文献

[1]Halliday M, Radford H, et al. Partial restoration of protein synthesis rates by the small molecule ISRIB prevents neurodegeneration without pancreatic toxicity. Cell Death Dis. 2015 Mar 5;6:e1672.

[2]PERK Inhibitor I, GSK2606414