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PKR-IN-C16

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Chemical Structure| 608512-97-6 同义名 : PKR Inhibitor;imoxin;C16, PKR Inhibitor.;Protein Kinase RNA-activated;GW 506033X;Imidazolo-oxindole PKR inhibitor C16;C16
CAS号 : 608512-97-6
货号 : A1209816
分子式 : C13H8N4OS
纯度 : 99%+
分子量 : 268.294
MDL号 : MFCD28046009
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：
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].
实验方案
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
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.