2. MAPK/ERK Pathway Autophagy
  3. p38 MAPK Autophagy
  4. p38 MAPK-IN-1

p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC50 of 68 nM. p38 MAPK-IN-1 shows sustained levels, low clearance and good bioavailability.

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

CAS No. : 1006378-90-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
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10 mM * 1 mL in DMSO In-stock
Solid
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10 mg In-stock
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Customer Review

Based on 14 publication(s) in Google Scholar

p38 MAPK-IN-1 Related Antibodies

Top Publications Citing Use of Products

    p38 MAPK-IN-1 purchased from MedChemExpress. Usage Cited in: Adv Biol (Weinh). 2025 Jun 4:e00761.  [Abstract]

    Macrophages were pretreated with inhibitors of the ERK (HY‐112287; ERK1/2 inhibitor 1), JNK (HY‐12041; SP600125), p38 MAPK (HY‐12839; p38 MAPK-IN-1), and p65 NF‐kB (HY‐138537; NF-κB-IN-1) pathways prior to incubation with pyroptotic‐CM for 4 h.The MET formation by macrophages was evaluated with SYTOX Green staining and detected by flow cytometry.

    p38 MAPK-IN-1 purchased from MedChemExpress. Usage Cited in: Adv Biol (Weinh). 2025 Jun 4:e00761.  [Abstract]

    Macrophages were pretreated with inhibitors of the ERK (HY‐112287; ERK1/2 inhibitor 1), JNK (HY‐12041; SP600125), p38 MAPK (HY‐12839; p38 MAPK-IN-1), and p65 NF‐kB (HY‐138537; NF-κB-IN-1) pathways prior to incubation with pyroptotic‐CM for 4 h. The p‐p38 and p‐p65 levels in macrophages were measured by western blotting.

    p38 MAPK-IN-1 purchased from MedChemExpress. Usage Cited in: Int J Biol Macromol. 2024 Nov;281(Pt 1):136178.  [Abstract]

    S100A9 upregulated the expression of LCN2 in HK-2 cells via activating the TLR4-p38/MAPK signaling pathway. Supplementing p38 MAPK-IN-1 kept S100A9 from enhancing LCN2 expression in HK-2 cells.

    p38 MAPK-IN-1 purchased from MedChemExpress. Usage Cited in: Int J Biol Macromol. 2024 Nov;281(Pt 1):136178.  [Abstract]

    Paquinimod (HY-100442;ip; 15 mg/kg/d for seven days) and p38 MAPK-IN-1 (HY-12839; ip; 1 mg/kg/d for seven days ) both reduced the renal deposition of calcium in nephrocalcinosis mice.

    p38 MAPK-IN-1 purchased from MedChemExpress. Usage Cited in: Int J Biol Macromol. 2024 Nov;281(Pt 1):136178.  [Abstract]

    Paquinimod (HY-100442;ip; 15 mg/kg/d for seven days) and p38 MAPK-IN-1 (HY-12839; ip; 1 mg/kg/d for seven days ) both reduced the renal deposition of calcium in nephrocalcinosis mice.

    p38 MAPK-IN-1 purchased from MedChemExpress. Usage Cited in: Int J Biol Macromol. 2024 Nov;281(Pt 1):136178.  [Abstract]

    Paquinimod (HY-100442;ip; 15 mg/kg/d for seven days) and p38 MAPK-IN-1 (HY-12839; ip; 1 mg/kg/d for seven days ) both reduced the renal deposition of CaOx crystals in nephrocalcinosis mice.

    p38 MAPK-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 May 1;21(1):86.  [Abstract]

    Neutrophils were pretreated with inhibitors of the ERK (HY-112287;ERK1/2 inhibitor 1), p38 MAPK (HY-12839; p38 MAPK-IN-1), and p65 NF-кB (HY-138537; NF-κB-IN-1) pathways prior to incubation with hypoxic-CM from GC cells. The protein levels of p-ERK, p-p38, and p-p65 in neutrophils were measured by western blotting.

    p38 MAPK-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 May 1;21(1):86.  [Abstract]

    Neutrophils were pretreated with inhibitors of the ERK (HY-112287;ERK1/2 inhibitor 1), p38 MAPK (HY-12839; p38 MAPK-IN-1), and p65 NF-кB (HY-138537; NF-κB-IN-1) pathways prior to incubation with hypoxic-CM from GC cells. The NET formation by neutrophils was evaluated with MPO and citH3 staining. Magnification: 20 × . Scale bars: 50 μm.

    p38 MAPK-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 May 1;21(1):86.  [Abstract]

    NETs accelerate tumour growth in vivo via angiogenesis. Subcutaneous AGS tumour growth was increased in the presence of NET-producing neutrophils from LPS-treated mice in vivo (n = 5 each group). LPS (10 μg/mouse) was intraperitoneally injected to induce systemic inflammation in BALB/c nude mice. Deoxyribonuclease I (DNase I, 100 U/mouse) or a p38 MAPK signalling pathway inhibitor (HY-12839; p38 MAPK-IN-1; 1 mg/kg) was injected intraperitoneally 24 h before injection of LPS as the NET inhibitor.

    p38 MAPK-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 May 1;21(1):86.  [Abstract]

    NETs accelerate tumour growth in vivo via angiogenesis. LPS (10 μg/mouse) was intraperitoneally injected to induce systemic inflammation in BALB/c nude mice. Deoxyribonuclease I (DNase I, 100 U/mouse) or a p38 MAPK signalling pathway inhibitor (HY-12839; p38 MAPK-IN-1; 1 mg/kg) was injected intraperitoneally 24 h before injection of LPS as the NET inhibitor. Increased angiogenesis in tumours of LPS-treated mice compared to control mice. Representative images of CD31 staining are shown. Magnification: 20 × . Scale bars: 50 μm. All values are the means ± SDs. *P < 0.05, **P < 0.01.

    View All p38 MAPK Isoform Specific Products:

    View All Isoforms
    p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC50 of 68 nM. p38 MAPK-IN-1 shows sustained levels, low clearance and good bioavailability.

    IC50 & Target[1]

    p38 MAPK

    68 nM (IC50)

    In Vivo

    p38 MAPK-IN-1 (Compound 4; 1 mg/kg for iv and 10 mg/kg for po) has a t1/2 of 7.4 hours and CL of 2.7 mL/min/kg for iv, and a Cmax of 5.3 μM for po in male wistar rats[1].
    p38 MAPK-IN-1 dose-dependently inhibits TNFα production with an ED50 of 0.5 mg/kg[1].

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

    Animal Model: Male wistar rats[1]
    Dosage: 10 mg/kg for po and 1 mg/kg for iv (Pharmacokinetic Analysis)
    Administration: Po and iv
    Result: Had a t1/2 of 7.4 hours and CL of 2.7 mL/min/kg for iv, and a Cmax of 5.3 μM for po.
    Molecular Weight

    349.35

    Formula

    C21H15F2N2O
    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    FC1=CC(F)=C(C2=CC=NC(C2=CC=[NH+]3[O-])=C3C4=C(C)C=CC=C4)C=C1
    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 : 33.33 mg/mL (95.41 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 2.8625 mL 14.3123 mL 28.6246 mL
    5 mM 0.5725 mL 2.8625 mL 5.7249 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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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: ≥ 0.83 mg/mL (2.38 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (2.38 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
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    %
    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

    Purity: 99.71%

    SDS (393 KB)

    COA (250 KB) HNMR (274 KB) RP-HPLC (865 KB) MS (885 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, 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 2.8625 mL 14.3123 mL 28.6246 mL 71.5615 mL
    5 mM 0.5725 mL 2.8625 mL 5.7249 mL 14.3123 mL
    10 mM 0.2862 mL 1.4312 mL 2.8625 mL 7.1561 mL
    15 mM 0.1908 mL 0.9542 mL 1.9083 mL 4.7708 mL
    20 mM 0.1431 mL 0.7156 mL 1.4312 mL 3.5781 mL
    25 mM 0.1145 mL 0.5725 mL 1.1450 mL 2.8625 mL
    30 mM 0.0954 mL 0.4771 mL 0.9542 mL 2.3854 mL
    40 mM 0.0716 mL 0.3578 mL 0.7156 mL 1.7890 mL
    50 mM 0.0572 mL 0.2862 mL 0.5725 mL 1.4312 mL
    60 mM 0.0477 mL 0.2385 mL 0.4771 mL 1.1927 mL
    80 mM 0.0358 mL 0.1789 mL 0.3578 mL 0.8945 mL
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    p38 MAPK-IN-1 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:

    p38 MAPK-IN-11006378-90-0p38 MAPKAutophagysustainedlevelslowclearancebioavailabilityInhibitorinhibitorinhibit

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