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

PD 169316 

目录号: HY-10578 纯度: 98.33%
产品使用指南

PD 169316 是一种高效,细胞透过的,有选择性的 p38 MAP kinase 抑制剂,IC50 值为 89 nM。PD169316 选择性地抑制磷酸化 p38 的激酶活性,但不阻碍上游激酶磷酸化 p38。PD169316 显示对 Enterovirus71 有抗病毒活性。

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PD 169316 Chemical Structure

PD 169316 Chemical Structure

CAS No. : 152121-53-4

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Size Price Stock Quantity
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1392 In-stock
10 mg ¥1265 In-stock
50 mg ¥4185 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Top Publications Citing Use of Products

    PD 169316 purchased from MCE. 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.

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

    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 MCE. Usage Cited in: Oncol Rep. 2017 Dec;38(6):3668-3676.

    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 MCE. Usage Cited in: Int J Med Sci. 2016 Jul 18;13(8):611-9.

    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.
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    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].

    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].

    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.

    152121-53-4

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 12.5 mg/mL (34.69 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    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
    10 mM 0.2775 mL 1.3876 mL 2.7752 mL
    * 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,并请注意储备液的保存方式和期限。
    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案,配制前请先配制澄清的储备液,再依次添加助溶剂 (为保证实验结果的可靠性,体内实验的工作
    液,建议您现用现配,当天使用;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分比是指该溶剂在您配制终溶液中的体积占比):

    • 1.

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

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

    • 2.

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

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

    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 1.25 mg/mL (3.47 mM); Clear solution

    *以上所有助溶剂都可在 MCE 网站选购。
    References
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    × = ×
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    产品名称:
    PD 169316
    目录号:
    HY-10578
    需求量:

    PD 169316

    Cat. No.: HY-10578