2. Apoptosis
  3. Apoptosis
  4. PKR-IN-C16

PKR-IN-C16 (Compound C16) is a specific double-stranded RNA-dependent protein kinase (PKR) inhibitor. PKR-IN-C16 shows promising neuroprotective properties and can rescue acute brain lesions.

For research use only. We do not sell to patients.

CAS No. : 608512-97-6

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10 mM * 1 mL in DMSO
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Customer Review

Based on 7 publication(s) in Google Scholar

PKR-IN-C16 Related Antibodies

Top Publications Citing Use of Products

    PKR-IN-C16 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jan 25;15(1):739.  [Abstract]

    Compound C16, a PKR inhibitor, was included as a positive control group. Significantly, co-delivery of FLuc-SEC induced a 1.48-fold, 1.54-fold, and 1.17-fold higher luminescence signal than FLuc-saRNA, FLuc-mRNA, and FLuc-saRNA/C16 group on day 1, respectively.

    PKR-IN-C16 purchased from MedChemExpress. Usage Cited in: Auburn University. 2024 May.

    WI-38 cells were treated with PKR-inhibitor PKR-INC16 (C16, 1-5 µM) for 30 min prior to infection with RSV with multiplicity of infection (MOI) of 3 or incubated with medium (n.i.) for 72 h. Expression of peIF2α, pPKR and PKR were assessed by Western blotting with GAPDH as endogenous control.

    PKR-IN-C16 purchased from MedChemExpress. Usage Cited in: Auburn University. 2024 May.

    WI-38 cells were treated with PKR-inhibitor PKR-INC16 (C16, 1-5 µM) for 30 min prior to infection with RSV with multiplicity of infection (MOI) of 3 or incubated with medium (n.i.) for 72 h. CHOP mRNA normalized against GAPDH (endogenous control) and is presented as fold change relative to non-infected DMSO "C16 5 µM".

    PKR-IN-C16 purchased from MedChemExpress. Usage Cited in: Auburn University. 2024 May.

    WI-38 cells were treated with PKR-inhibitor PKR-INC16 (C16, 1-5 µM) for 30 min prior to infection with RSV with multiplicity of infection (MOI) of 3 or incubated with medium (n.i.) for 72 h. XPB1swas normalized against GAPDH (endogenous control) and is presented as fold change relative to non-infected DMSO "C16 5 µM".

    PKR-IN-C16 purchased from MedChemExpress. Usage Cited in: Brain Behav. 2022 Aug;12(8):e2722.  [Abstract]

    By constructing a rat SAH model and giving PKR-IN-C16 (C16) treatment, the rats were scored for cerebral floor hemorrhage and neurological function 48 h after modeling. The scoring results are shown in Figure.

    PKR-IN-C16 purchased from MedChemExpress. Usage Cited in: Brain Behav. 2022 Aug;12(8):e2722.  [Abstract]

    Treatment of rats with the PKR inhibitor PKR-IN-C16 (C16) significantly alleviated the accumulation of MDA and iron ions and the reduction of GPX4 activities induced by SAH.

    PKR-IN-C16 purchased from MedChemExpress. Usage Cited in: Brain Behav. 2022 Aug;12(8):e2722.  [Abstract]

    Shows the reciprocal network of differentially expressed mRNA target proteins in the SAH group and the SAH‐PKR-IN-C16 (C16) group.

    • Biological Activity

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    Description

    PKR-IN-C16 (Compound C16) is a specific double-stranded RNA-dependent protein kinase (PKR) inhibitor. PKR-IN-C16 shows promising neuroprotective properties and can rescue acute brain lesions[1].

    IC50 & Target

    PKR[1]
    In Vitro

    PKR-IN-C16 (Compound C16) is able to unlock the translation blockade induced by PKR in primary neuronal cultures[1].
    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[1].
    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[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    PKR-IN-C16 Related Antibodies

    Western Blot Analysis[2]

    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.
    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.html" class="link-product" target="_blank">Quinolinic acid (QA) (HY-100807) induced acute excitotoxic rat model[1]

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Normotensive male Wistar rats, excitotoxic neuroinflammatory model, inflammation was induced by unilateral striatal injection of quinolinic acid (QA)[1]
    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.
    Molecular Weight

    268.29

    Formula

    C13H8N4OS
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1/C(C2=C(SC=N3)C3=CC=C2N1)=C\C4=CN=CN4
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 10 mg/mL (37.27 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.7273 mL 18.6365 mL 37.2731 mL
    5 mM 0.7455 mL 3.7273 mL 7.4546 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1 mg/mL (3.73 mM); Clear solution

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 1 mg/mL (3.73 mM); Clear solution

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 20 mg/mL (74.55 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  15% Cremophor EL    85% Saline

      Solubility: 10 mg/mL (37.27 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.70%

    SDS (393 KB)

    COA (255 KB) HNMR (142 KB) RP-HPLC (169 KB) LCMS (234 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.7273 mL 18.6365 mL 37.2731 mL 93.1827 mL
    5 mM 0.7455 mL 3.7273 mL 7.4546 mL 18.6365 mL
    10 mM 0.3727 mL 1.8637 mL 3.7273 mL 9.3183 mL
    15 mM 0.2485 mL 1.2424 mL 2.4849 mL 6.2122 mL
    20 mM 0.1864 mL 0.9318 mL 1.8637 mL 4.6591 mL
    25 mM 0.1491 mL 0.7455 mL 1.4909 mL 3.7273 mL
    30 mM 0.1242 mL 0.6212 mL 1.2424 mL 3.1061 mL
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    PKR-IN-C16 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    PKR-IN-C16608512-97-6Apoptosisacute brain lesionsdouble-stranded RNA-dependent protein kinasePKRSH-SY5YInhibitorinhibitorinhibit

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