1. MAPK/ERK Pathway Autophagy Anti-infection
  2. p38 MAPK Autophagy Enterovirus
  3. PD 169316

PD 169316 is a potent, cell-permeable and selective p38 MAP kinase inhibitor, with IC50 of 89 nM. PD169316 selectively inhibits the kinase activity of the phosphorylated p38 without hindering upstream kinases to phosphorylate p38. PD169316 shows antiviral activity against Enterovirus71. PD169316 shows antiviral activity against Enterovirus71.

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

PD 169316 Chemical Structure

PD 169316 Chemical Structure

CAS No. : 152121-53-4

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 109 In-stock
Solution
10 mM * 1 mL in DMSO USD 109 In-stock
Solid
5 mg USD 63 In-stock
10 mg USD 99 In-stock
50 mg USD 275 In-stock
100 mg USD 495 In-stock
500 mg USD 1595 In-stock
1 g   Get quote  
5 g   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 17 publication(s) in Google Scholar

Top Publications Citing Use of Products

    PD 169316 purchased from MedChemExpress. Usage Cited in: Oncol Lett. 2018 Jan;15(1):235-242.  [Abstract]

    Cells are treated with 15 and 20 μM Lapatinib for 24 h, the expression of p AKT, AKT, p p38 MAPK, p38 MAPK, p JNK, and JNK are measured by western blotting. Quantification analysis of western blotting, β actin is served as a control. D: 1 DMSO; 2 PD169316; 3 15 μM Lapatinib; 4 PD169316+15 μM Lapatinib).

    PD 169316 purchased from MedChemExpress. Usage Cited in: Oncol Rep. 2017 Dec;38(6):3668-3676.  [Abstract]

    Western blot analysis evaluated p-p38, p38, LC3 and quantification of LC3-II in untreated (control), treated with the p38 inhibitor PD169316, cisplatin, and both these agents in MDA-MB-231 cells.

    PD 169316 purchased from MedChemExpress. Usage Cited in: Int J Med Sci. 2016 Jul 18;13(8):611-9.  [Abstract]

    PD169316 (10 μM) inhibits the effects of all-trans retinoic acid(ATRA) on nuclear localization signal retinoic acid receptor alpha (NLS-RARα)-overexpressed NB4 cells incluing an increase of the expressions of p-p38α, C/EBPβ and CD11b.

    PD 169316 purchased from MedChemExpress. Usage Cited in: Chinese Journal of Cell Biology. 2016, 38(7): 770–776

    The protein levels of Bax and Bcl-2 detected by Western blot. PD169316 decreases EGCG-mediated increases in Bax protein expression.

    View All p38 MAPK Isoform Specific Products:

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PD 169316 is a potent, cell-permeable and selective p38 MAP kinase inhibitor, with IC50 of 89 nM. PD169316 selectively inhibits the kinase activity of the phosphorylated p38 without hindering upstream kinases to phosphorylate p38. PD169316 shows antiviral activity against Enterovirus71. PD169316 shows antiviral activity against Enterovirus71.

    IC50 & Target

    IC50: 89 nM (p38 MAPK)[5]

    In Vitro

    PD169316 (10 μM) inhibits TGFβ and Activin A, but not BMP4 signaling in CaOV3 cells. PD169316 (0.2-20 μM) inhibits TGFβ-induced Smad2 nuclear translocation, Smad7 mRNA induction, and reporter gene activity in CaOV3 cells[1]. PD169316 (10 μM) shows a significantly increased rate of proliferation in Nestin knockdown cells, and can rescue the effect of Nestin knockdown on cell viability in the absence of EGF[2]. PD169316 significantly inhibits p38 MAP kinase activity with no significant change in ERK activity in PC12 cells. PD169316 (10 μM) blocks apoptosis induced by trophic factor withdrawal in differentiated PC12 cells[3].PD169316 (10 μM, 30 min) selectively inhibits the kinase activity of the phosphorylated p38 without hindering upstream kinases to phosphorylate p38. Increased phospho p-38 levels in the presence of PD169316 are most likely due to blockade of negative feedback loop of dephosphorylation of p38 MAPK by MAPK phosphatases[4].

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

    Western Blot Analysis[1]

    Cell Line: Ishikawa PRB or PRA cells.
    Concentration: 10 μM.
    Incubation Time: 30 min.
    Result: Did not inhibit MEKK1-induced p38 phosphorylation.
    In Vivo

    PD169316 (1 mg/kg, intramuscular injection every day for 14 consecutive days) shows antiviral activity in a suckling mouse model[5].

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

    Animal Model: EV71-challenged suckling mouse model (7-day-old Kunming mice)[5].
    Dosage: 1 mg/kg.
    Administration: Intramuscular injection every day for 14 consecutive days.
    Result: Showed antiviral activity.
    Molecular Weight

    360.34

    Formula

    C20H13FN4O2

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    FC(C=C1)=CC=C1C2=C(C3=CC=NC=C3)NC(C4=CC=C([N+]([O-])=O)C=C4)=N2

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 12.5 mg/mL (34.69 mM; Need ultrasonic; 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 2.7752 mL 13.8758 mL 27.7516 mL
    5 mM 0.5550 mL 2.7752 mL 5.5503 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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: 1.25 mg/mL (3.47 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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% (20% SBE-β-CD in Saline)

      Solubility: 1.25 mg/mL (3.47 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    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:  50% PEG300    50% Saline

      Solubility: 5 mg/mL (13.88 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    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
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7752 mL 13.8758 mL 27.7516 mL 69.3789 mL
    5 mM 0.5550 mL 2.7752 mL 5.5503 mL 13.8758 mL
    10 mM 0.2775 mL 1.3876 mL 2.7752 mL 6.9379 mL
    15 mM 0.1850 mL 0.9251 mL 1.8501 mL 4.6253 mL
    20 mM 0.1388 mL 0.6938 mL 1.3876 mL 3.4689 mL
    25 mM 0.1110 mL 0.5550 mL 1.1101 mL 2.7752 mL
    30 mM 0.0925 mL 0.4625 mL 0.9251 mL 2.3126 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    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.

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Salutation

    Applicant Name *

     

    Email Address *

    Phone Number *

     

    Organization Name *

    Department *

     

    Requested quantity *

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    PD 169316
    Cat. No.:
    HY-10578
    Quantity:
    MCE Japan Authorized Agent: