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品質等級
化驗
≥98% (HPLC)
顏色
yellow to orange-brown
溶解度
DMSO: 12 mg/mL
運輸包裝
wet ice
儲存溫度
−20°C
SMILES 字串
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 密鑰
VFBGXTUGODTSPK-BAQGIRSFSA-N
應用
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。
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
The specific protein kinase R (PKR) inhibitor C16 protects neonatal hypoxia-ischemia brain damages by inhibiting neuroinflammation in a neonatal rat model
Medical Science Monitor : International Medical Journal of Experimental and Clinical Research, 22, 5074-5074 (2016)
AIM2 inflammasome mediates Arsenic-induced secretion of IL-1 beta and IL-18
Oncoimmunology, 5(6), e1160182-e1160182 (2016)
PKR-a Kinase to Remember
Frontiers in Molecular Neuroscience, 11, 480-480 (2018)
Journal of virology, 93(19) (2019-07-12)
Leader (L) proteins encoded by cardioviruses are multifunctional proteins that contribute to innate immunity evasion. L proteins of Theiler's murine encephalomyelitis virus (TMEV), Saffold virus (SAFV), and encephalomyocarditis virus (EMCV) were reported to inhibit stress granule assembly in infected cells.
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
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