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CAS No.: 608512-97-6

PKR-IN-C16/咪唑氧吲哚 PKR 抑制剂 C16 Catalog No. CSN26210

Synonyms: imoxin;C16;Imidazolo-oxindole PKR inhibitor C16

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).

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技术信息

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].
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.7273 mL
- 18.6363 mL
- 37.2726 mL
- 5 mM
- 0.7455 mL
- 3.7273 mL
- 7.4545 mL
- 10 mM
- 0.3727 mL
- 1.8636 mL
- 3.7273 mL

技术信息

CAS号

608512-97-6

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H8N4OS

运输

蓝冰

分子量

268.29

别名

imoxin;C16;Imidazolo-oxindole PKR inhibitor C16;Protein Kinase RNA-activated;GW-506033X

溶解度

DMSO	13.0 mg/mL (48.5 mM)
Water	Insoluble
Ethanol	Insoluble

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PKR-IN-C16/咪唑氧吲哚 PKR 抑制剂 C16 Catalog No. CSN26210

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