PKR-IN-C16

For research use only. Not for use in humans.

目录号:S9668 别名: imoxin, C16, Imidazolo-oxindole PKR inhibitor C16

PKR-IN-C16 Chemical Structure

CAS No. 608512-97-6

PKR-IN-C16 (C16, Imidazolo-oxindole PKR inhibitor C16) 是一种RNA-dependent protein kinase (PKR, Protein Kinase R, EIF2AK2)的特异性抑制剂。PKR-IN-C16 可在具有神经炎症成分的急性兴奋性毒性大鼠模型中阻止凋亡和 IL-1β 的产生。

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客户使用Selleck生产的PKR-IN-C16发表文献2篇:

产品安全说明书

PKR抑制剂选择性比较

生物活性

产品描述 PKR-IN-C16 (C16, Imidazolo-oxindole PKR inhibitor C16) 是一种RNA-dependent protein kinase (PKR, Protein Kinase R, EIF2AK2)的特异性抑制剂。PKR-IN-C16 可在具有神经炎症成分的急性兴奋性毒性大鼠模型中阻止凋亡和 IL-1β 的产生。
靶点
PKR [1]
()
IL-1β [1]
()
体外研究

PKR-IN-C16 suppresses proliferation of HCC cells in a dose-dependent manner in vitro. Transcript levels of vascular endothelial growth factor-A and factor-B, platelet-derived growth factor-A and factor-B, fibroblast growth factor-2, epidermal growth factor, and hepatocyte growth factor, which are angiogenesis-related growth factors, are significantly decreased by PKR-IN-C16 in vitro. PKR-IN-C16 blockes tumor cell growth and angiogenesis via a decrease in mRNA levels of several growth factors.[2]

体内研究

Inflammation is induced by unilateral striatal injection of quinolinic acid (QA) in 10-week-old normotensive rats. The highest dose of C16 (600 μg/kg; C16-2) in QA rats reduces expression of the active catalytic domain of the PKR vs. that in vehicle-injected QA rats. A robust increase of IL-1b levels on the contralateral side of QA rats is prevented by C16-2 (97% inhibition). Macroscopic and microscopic observation of cerebral tissue revealed that tissue integrity is more preserved with C16-2 treatment than its vehicle in QA rats. Furthermore, C16-2 treatment decreases by 47% the neuronal loss and by 37% the number of positive cleaved caspase-3 neurons induced by QA injection. In conclusion, C16 prevents not only the PKR-induced neuronal loss but also the inflammatory response in this acute excitotoxic in vivo model, highlighting its promising neuroprotective properties to rescue acute brain lesions.[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[2]

- 合并
  • Cell lines: Huh7 cells
  • Concentrations: 500–3000 nM
  • Incubation Time: 120 min
  • Method:

    In vitro cell viability is quantified with the MTS assay. Huh7 cells treated with several concentrations (500–3000  nM) of the PKR inhibitor are seeded in 96-well plates at 2 × 103 cells per well. At each time point, cells are treated with MTS reagent and incubated for 120 min. Absorbance at 450 nm is recorded. Cells treated with DMSO are used as controls. The wells are photographed under the microscope.


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: 10-week-old male normotensive male Wistar rats
  • Dosages: 60 μg/kg, 600 μg/kg
  • Administration: IP
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 13 mg/mL (48.45 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 268.29
化学式

C13H8N4OS

CAS号 608512-97-6
储存条件 粉状
溶于溶剂
别名 imoxin, C16, Imidazolo-oxindole PKR inhibitor C16

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04716452 Not yet recruiting Drug: Ceramide NanoLiposome (Ceraxa) Acute Myeloid Leukemia in Relapse|Acute Myeloid Leukemia Refractory Keystone Nano Inc|University of Virginia|Memorial Sloan Kettering Cancer Center|Milton S. Hershey Medical Center February 15 2021 Phase 1
NCT04832217 Completed Other: Pyrenees´ Beef diet Body Weight Changes|Habits Diet|Habit Food|Life Change Events Universidad de Zaragoza January 20 2019 Not Applicable
NCT03691402 Active not recruiting Behavioral: MCT-Silver|Behavioral: Cognitive Remediation Depression Universitätsklinikum Hamburg-Eppendorf November 18 2018 Not Applicable
NCT03937115 Unknown status Device: Active tDCS|Device: Sham tDCS Healthy Volunteers|High-level Sportsman Centre Hospitalier Universitaire de Besancon November 21 2018 Not Applicable
NCT03327402 Completed Drug: SHP465 Attention Deficit Hyperactivity Disorder (ADHD) Shire|Takeda March 13 2018 Phase 1
NCT03196219 Completed Drug: C16G2|Other: Placebo Dental Caries Armata Pharmaceuticals Inc. July 7 2017 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID