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

p38 MAPK-IN-1 (Compound 4) 是 p38 MAPK 新型高效选择性抑制剂, IC50 值 68 nM。p38 MAPK-IN-1 显示持续水平，低清除率和良好的生物利用度。

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CAS No. : 1006378-90-0

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10 mM * 1 mL in DMSO ￥3850
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2 mg ￥2333
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5 mg ￥3500
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10 mg ￥5000
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Customer Review

p38 MAPK-IN-1 相关抗体

Top Publications Citing Use of Products

    p38 MAPK-IN-1 purchased from MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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.

    查看 p38 MAPK 亚型特异性产品:

    查看所有亚型
    p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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)

    体内研究
    (In Vivo)

    p38 MAPK-IN-1 (1 mg/kg 静脉注射和 10 mg/kg 口服) 具有 7.4 小时的 t1/2 和 2.7 mL/min/kg 的静脉注射 CL，雄性 wistar 大鼠中 po 的 Cmax 为 5.3 μM[1]。
    p38 MAPK-IN-1 以剂量依赖性方式抑制 TNFα 的产生，ED50 为 0.5 mg/kg[1]。

    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.
    分子量

    349.35

    Formula

    C21H15F2N2O
    CAS 号
    性状

    固体

    颜色

    Off-white to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 33.33 mg/mL (95.41 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 0.83 mg/mL (2.38 mM); 澄清溶液

      此方案可获得 ≥ 0.83 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 0.83 mg/mL (2.38 mM); 澄清溶液

      此方案可获得 ≥ 0.83 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.71%

    COA (266 KB) HNMR (274 KB) RP-HPLC (865 KB) MS (885 KB)

    产品使用指南 (1538 KB)
    参考文献

    p38 MAPK-IN-1 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 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
    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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     [Abstract]

    Customer Validation
     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.
  • 1/16

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

    Customer Validation
     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.
  • 1/16

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

    Customer Validation
     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.
  • 1/16

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

    Customer Validation
     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.
  • 1/16

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

    Customer Validation
     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.
  • 1/16

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

    Customer Validation
     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.
  • 1/16

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

    Customer Validation
     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.
  • 1/16

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

    Customer Validation
     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.
  • 1/16

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

    Customer Validation
     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.