1. MAPK/ERK Pathway
    Autophagy
  2. p38 MAPK
    Autophagy
  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。

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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.

    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].

    In Vivo

    PD169316 (30 ng/5 μL) or in combination with U0126 improves spatial learning in MWM in Aβ-injected rats, 20 days after Aβ-injection. Pretreatment with U0126 and PD169316 decreases the levels of phosphorylated form of ERK and p38 to about 77.7 and 64.2%, respectively, and causes a significant increase in c-fos, p-CREB, NRF-1 and TFAM protein levels, compared to the Aβ-injected group[4].

    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。
    In Vivo:
    • 1.

      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

    • 2.

      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

    • 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
    Kinase Assay
    [3]

    Sixteen hours after the removal of serum from Rat-1 fibroblasts or NGF from differentiated PC12 cells, the cells are incubated in the absence or presence of insulin (50 ng/mL) for 15 min at 37°C. After washing with 2 mL of ice-cold PBS, the cells are solubilized in 400 μL of ice-cold immunoprecipitation buffer containing 10 mM Tris, pH 7.4, 1% Triton X-100, 0.5% Nonidet P-40, 150 mM NaCl, 1 mM EDTA, 1 mM EGTA, 0.2 mM sodium orthovanadate, and 0.2 mM phenylmethylsulfonyl fluoride. The cell lysates are centrifuged to remove insoluble material, and 200 μg of the supernatant protein (400 μL, total volume) are incubated with 1 μg of anti-p38 antibodies for 1 h at 4°C followed by incubation with 30 μL of Protein G Plus/Protein A-agarose for an additional hour. The immunocomplexes are pelleted and washed twice in immunoprecipitation buffer and then once in kinase ish buffer (50 mM β-glycerolphosphate, 1 mM EGTA, 20 mM MgCl2, 100 μM sodium orthovanadate). The protein kinase assay is initiated by the addition of 20 μL of 2× reaction buffer (50 mMβ-glycerolphosphate, 1 mM EGTA, 20 mM MgCl2, 100 μM sodium orthovanadate, 0.1 mg/mL ATF-2 (N-terminal half), 50 μg/mL IP20, a peptide inhibitor of c-AMP dependent protein kinase, 200 μM ATP, and 0.9 mCi/mL [32P]ATP) to 20 μL of immune complex. The reaction is allowed to proceed for 10 min at 30°C and then terminated by the addition of 2× LaemmLi sample buffer and analyzed by SDS-polyacrylamide gel electrophoresis using 12% acrylamide gels. After electrophoresis, the gels are dried and subjected to phosphoimaging.

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

    Animal Administration
    [4]

    Adult male albino Wistar rats weighing 210-280 g are used in these experiments. Animals are divided into six groups: (A) Aβ-injected group, which receives bilateral intra-CA1 injection of Aβ (30 ng/3 μL PBS per side), 4 h after unilateral i.c.v. administration of DMSO (5 μL/rat), without receiving any treatment; (B) vehicle group, which only receives carrier, DMSO in lateral ventricle and PBS (3 μL/side) in both CA1 regions; (C) ERK inhibitor group, which receives i.c.v. infusion of U0126 (30 μg/5 μL 1% DMSO in PBS) with PBS injection (3 μL/side in CA1); (D) p38 inhibitor group, which receives i.c.v. infusion of PD169316 (30 μg/5 μL 1% DMSO in PBS) with PBS injection (3 μL/side in CA1); and (E) treatment group which receives i.c.v. administration of U0126 (30 μg/5 μL 1% DMSO in PBS), 4 h prior to intra-hippocampal A (30 ng/3 μL PBS per side) injection; (F) treatment group which receives i.c.v. administration of PD169316 (30 μg/5 μL 1% DMSO in PBS), 4 h prior to intra-hippocampal A (30 ng/3 μL PBS per side) injection. The aforementioned groups enter two experimental protocols: behavioral experiments and molecular studies. All the groups of animals in molecular study are considered as 7 and 20-day experimental groups.

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

    References
    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

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    产品名称:
    PD 169316
    目录号:
    HY-10578
    需求量:

    PD 169316

    Cat. No.: HY-10578