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PKR Inhibitor

双链RNA激活蛋白激酶（PKR）抑制剂,PKR-IN-C16 是特异性蛋白激酶 (PKR) 抑制剂。PKR-IN-C16 能够抑制 PKR 的自磷酸化，PKR 在原代神经元细胞培养中诱导的翻译阻断可被 PKR-IN-C16 解除。

目录号: PC16184 纯度: ≥98%

CAS No. :608512-97-6

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中文名称

PKR Inhibitor

中文别名

甲萘威;西维因

英文名称

8-(1H-IMIDAZOL-4-YLMETHYLENE)-6,8-DIHYDRO-THIAZOLO[5,4-E]INDOL-7-ONE

英文别名

8-(1H-IMIDAZOL-4-YLMETHYLENE)-6,8-DIHYDRO-THIAZOLO[5,4-E]INDOL-7-ONE;PKR Inhibitor;C16;Imidazolo-oxindole PKR inhibitor C16;6,8-Dihydro-8-(1H-imidazol-5-ylmethylene)-7H-pyrrolo[2,3-g]benzothiazol-7-one;PKR-IN-C16

Cas No.

608512-97-6

分子式

C₁₃H₈N₄Os

分子量

268.29

包装储存

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

PKR-IN-C16 (Compound C16) is a specific double-stranded RNA-dependent protein kinase (PKR) inhibitor. PKR-IN-C16 shows promising neuroprotective properties and can rescue acute brain lesions.

性状

Solid

IC50 & Target[1][2]

PKR

体外研究(In Vitro)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究(In Vivo)

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

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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 injection
Result:	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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Tronel C, et al. The specific PKR inhibitor C16 prevents apoptosis and IL-1β production in an acute excitotoxic rat model with a neuroinflammatory component. Neurochem Int. 2014 Jan;64:73-83. [Information]

[2]. Page G, et al. Activated double-stranded RNA-dependent protein kinase and neuronal death in models of Alzheimers disease. Neuroscience. 2006;139(4):1343-54. [Information]

溶解度数据

体外研究:

DMSO : 7.35 mg/mL (27.40 mM; ultrasonic and warming and heat to 60°C)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.7273 mL	18.6365 mL	37.2731 mL
5 mM	0.7455 mL	3.7273 mL	7.4546 mL
10 mM	0.3727 mL	1.8637 mL	3.7273 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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