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咪唑氧吲哚 PKR 抑制剂 C16 /PKR-IN-C16 99%+

货号:A1209816 同义名: PKR Inhibitor;imoxin 产品仅供科研

PKR-IN-C16 is a specific protein kinase (PKR) inhibitor. It shows to effectively inhibit RNA-induced PKR autophosphorylation (IC50 = 210 nM) and rescue PKR-dependent translation block (IC50 = 100 nM).

PKR-IN-C16 化学结构 CAS号:608512-97-6
PKR-IN-C16 化学结构
CAS号:608512-97-6
PKR-IN-C16 3D分子结构
CAS号:608512-97-6
PKR-IN-C16 化学结构 CAS号:608512-97-6
PKR-IN-C16 3D分子结构 CAS号:608512-97-6
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PKR-IN-C16 纯度/质量文件

货号:A1209816 标准纯度:99%+
批次查询: 批次纯度:

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PKR-IN-C16 生物活性

描述 Pyruvate kinase (PK) catalyzes the last step of glycolysis and exists as four isoenzymes: PK, liver, PK, red blood cell, PK, muscle (PKM1 and PKM2). Pyruvate kinase isoenzyme type M2 (PKM2, M2-PK) plays a key role in modulating glucose metabolism to support cell proliferation. PKM2, like other PK isoforms, catalyzes the last energy-generating step in glycolysis, but is unique in its capacity to be regulated.[1]. 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. It 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[2].

PKR-IN-C16 参考文献

[1]Vibhor Gupta,et al. Pyruvate kinase M2: regulatory circuits and potential for therapeutic intervention. Curr Pharm Des. 2014. 20(15), 2595-606.

[2]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. 64, 73-83.

PKR-IN-C16 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.73mL

0.75mL

0.37mL

18.64mL

3.73mL

1.86mL

37.27mL

7.45mL

3.73mL

PKR-IN-C16 技术信息

CAS号608512-97-6
分子式C13H8N4OS
分子量268.294
别名 PKR Inhibitor;imoxin;C16, PKR Inhibitor.;Protein Kinase RNA-activated;GW 506033X;Imidazolo-oxindole PKR inhibitor C16;C16
运输蓝冰
存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 9 mg/mL(33.55 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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