PKR-IN-C16

SKU: orb1219493

Description

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.PKR-IN-C16 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.

Key Properties

• CAS Number: 608512-97-6
• MW: 268.29
• Purity: >98% (HPLC)
• Formula: C₁₃H₈N₄OS
• SMILES: O=C1Nc2ccc3ncsc3c2\C1=C\c1cnc[nH]1
• Target: PKR
• Solubility: DMSO:15.67 mg/mL(58.41 mM)

Bioactivity

• 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. 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.
• 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. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

PKR