PKR-IN-C16

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PKR-IN-C16 是一种特异性蛋白激酶 (PKR) 抑制剂。 PKR-IN-C16 能够抑制 PKR 的自磷酸化，并解锁原代神经元培养物中 PKR 诱导的翻译阻断。PKR-IN-C16 结合 PKR 的 ATP 结合位点并阻断自磷酸化，IC50 值为 186-210纳米。

PKR-IN-C16 is a specific protein kinase (PKR) inhibitor.?PKR-IN-C16 is able to inhibit the autophosphorylation of PKR and unlock the translation blockade induced by PKR in primary neuronal cultures.PKR-IN-C16 binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM.?PKR-IN-C16 protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress.?

PKR-IN-C16 (Compound C16) is able to unlock the translation blockade induced by PKR in primary neuronal cultures.PKR-IN-C16 (0.1 or 0.3 μM; 24 h) shows protective effect against the neuronal cell death induced by endoplasmic reticulum stress in SH-SY5Y cells.?PKR-IN-C16 (1-1000 nM; 4 h) prevents not only PKR-phosphorylation but also the activation of caspase-3 induced by Amyloid β in SH-SY5Y cells. Western Blot Analysis Cell Line:Human SH-SY5Y cells Concentration:1, 10, 20, 200, 1000 nM Incubation Time:4 h Result:Markedly reduces the level of phosphorylated PKR in the cells exposed to 20 μM Amyloid β.

PKR-IN-C16 (Compound C16) (60 or 600 μg/kg; i.p.; 3 times) prevents not only the PKR-induced neuronal loss but also the inflammatory response in the Quinolinic acid (QA) (HY-100807) induced acute excitotoxic rat model Animal Model:Normotensive male Wistar rats, excitotoxic neuroinflammatory model, inflammation was induced by unilateral striatal injection of quinolinic acid (QA)Dosage:60 or 600 μg/kg Administration: Intraperitoneal injection; 24 h, 2 h before QA injection and 24 h post-QA injectionResult:Reduced expression of the active catalytic domain of the PKR, prevented increase of IL-1β levels on the contralateral side (97% inhibition) at 600 μg/kg. Decreased by 47% the neuronal loss and by 37% the number of positive cleaved caspase-3 neurons induced by QA injection at 600 μg/kg.

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Others

Other Targets

PKR

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608512-97-6

268.29

C13H8N4OS

>98% (HPLC)

DMSO:15.67 mg/mL(58.41 mM)

O=C1Nc2ccc3ncsc3c2\C1=C\c1cnc[nH]1

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(-20℃)

With Ice Pack

≥ 2 years