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PKR Inhibitor
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
PKR Inhibitor图片
CAS NO:608512-97-6
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍

化学性质

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt268.3
Cas No.608512-97-6
FormulaC13H8N4OS
SynonymsC16,GW 506033X,Protein Kinase RNA-activated
Solubility≤2.5mg/ml in DMSO;0.5mg/ml in dimethyl formamide
Chemical Name6,8-dihydro-8-(1H-imidazol-5-ylmethylene)-7H-pyrrolo[2,3-g]benzothiazol-7-one
Canonical SMILESO=C1NC2=CC=C3C(SC=N3)=C2/C1=C/C4=CNC=N4
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

IC50: 186-210 nM

PKR Inhibitor is a double-stranded RNA-activated protein kinase (PKR) inhibitor.

Initiation of protein synthesis is reported to be regulated by kinase-dependent phosphorylation reactions. Double-stranded RNA-dependent protein kinase (PKR) is identified as one of these important kinases controlling the initiation step.

In vitro: PKR Inhibitor was identified as a small molecule able to inhibit the autophosphorylation of PKR and to rescue the translation blockade induced by PKR. It was found that PKR Inhibitor prevented not only PKR phosphorylation but also the activation of caspase 3 induced by Ab in SH-SY5Y cells. In addition, the protective effect of PKR Inhibitor on the neuronal cell death induced by endoplasmic reticulum-stress in SH-SY5Y cells has been reported [1].

In vivo: A previous animal study used an in-vivo model of 7-day-old rat exhibiting a high activation of brain PKR to investigate the effects of PKR Inhibitor. Results showed for the first time that acute systemic injection of PKR Inhibitor could specifically inhibit the apoptotic PKR/eIF2a signaling pathway without stimulating the proliferative mTOR/p70S6K signaling mechanism [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Ingrand, S. ,Barrier, L.,Lafay-Chebassier, C., et al. The oxindole/imidazole derivative C16 reduces in vivo brain PKR activation. FEBS Letters 581(23), 4473-4478 (2007).