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Merck
CN

I9785

Sigma-Aldrich

咪唑氧吲哚 PKR 抑制剂 C16

≥98% (HPLC)

别名:

6,8-二氢-8-(1H-咪唑-5-基亚甲基)-7H-吡咯并 [2,3-g] 苯并噻唑-7-酮

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About This Item

经验公式(希尔记法):
C13H8N4OS
分子量:
268.29
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

质量水平

检测方案

≥98% (HPLC)

颜色

yellow to orange-brown

溶解性

DMSO: 12 mg/mL

运输

wet ice

储存温度

−20°C

SMILES字符串

O=C1NC2=CC=C3C(SC=N3)=C2/C1=C/C4=CNC=N4

InChI

1S/C13H8N4OS/c18-13-8(3-7-4-14-5-15-7)11-9(17-13)1-2-10-12(11)19-6-16-10/h1-6H,(H,14,15)(H,17,18)/b8-3-

InChI key

VFBGXTUGODTSPK-BAQGIRSFSA-N

应用

咪唑-氧化吲哚 PKR 抑制剂 C16 已被用于:
  • 挽救小鼠恐惧记忆缺陷和恢复长时程增强 (LTP) 损伤
  • 在HeLa-S3细胞中质粒转染后抑制干扰素刺激基因(ISG)的强烈诱导
  • 增强真核翻译起始因子 2 (eIF2) 的活性。

生化/生理作用

C16在成人脑损伤中表现出神经保护作用。
咪唑并 - 羟吲哚PKR抑制剂C16是RNA依赖性蛋白激酶(PKR,Eif2ak2)的选择性抑制剂。C16 是第一个被报道的有效的选择性 PKR 抑制剂。其对 PKR 的抑制作用是通过 ATP 结合位点介导的。C16特异性地抑制凋亡PKR / eIF2a信号传导途径而不刺激增殖性mTOR / p70S6K信号传导机制。

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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访问文档库

The specific protein kinase R (PKR) inhibitor C16 protects neonatal hypoxia-ischemia brain damages by inhibiting neuroinflammation in a neonatal rat model
Xiao J, et al.
Medical Science Monitor : International Medical Journal of Experimental and Clinical Research, 22, 5074-5074 (2016)
PKR-a Kinase to Remember
Gal-Ben-Ari S, et al.
Frontiers in Molecular Neuroscience, 11, 480-480 (2018)
Jiahui Tang et al.
Antioxidants (Basel, Switzerland), 11(10) (2022-10-28)
Retinal ganglion cells (RGCs), the projection neurons of the eye, are irreversibly lost once the optic nerve is injured, which is a critical mechanism of glaucoma. Mobile zinc (Zn2+) levels rapidly increase in retinal interneuron amacrine cells and Zn2+ is
Mohamad A Zaini et al.
Scientific reports, 7, 42603-42603 (2017-02-16)
An important part of the beneficial effects of calorie restriction (CR) on healthspan and lifespan is mediated through regulation of protein synthesis that is under control of the mechanistic target of rapamycin complex 1 (mTORC1). As one of its activities
AIM2 inflammasome mediates Arsenic-induced secretion of IL-1 beta and IL-18
Zhang MF, et al.
Oncoimmunology, 5(6), e1160182-e1160182 (2016)

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