2. MAPK/ERK Pathway Stem Cell/Wnt Immunology/Inflammation Autophagy
  3. MEK ERK Aryl Hydrocarbon Receptor Autophagy
  4. PD98059

PD98059 是一种有效的选择性的 MEK 抑制剂，IC50 为 5 μM。PD98059 与 MEK 的无活性形式结合，从而阻止上游激酶激活 MEK1 (IC50 为 2-7 μM) 和 MEK2 (IC50 为 50 μM)。PD98059 是一种 ERK1/2 信号的抑制剂。PD98059 是一种芳烃受体 (AHR) 的配体，可抑制细胞中 TCDD 结合 (IC50 为 4 μM) 和 AHR 转化 (IC50 为 1 μM)。PD98059 还可抑制 Mycobacterium bovis Bacillus CalmetteGuerin (BCG) 诱导的细胞自噬 (autophagy)。

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PD98059 Chemical Structure

PD98059 Chemical Structure

CAS No. : 167869-21-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥979
In-stock
1 mg ￥333
In-stock
5 mg ￥750
In-stock
10 mg ￥1083
In-stock
25 mg ￥2025
In-stock
50 mg ￥3100
In-stock
100 mg ￥4100
In-stock
200 mg ￥5330
In-stock
500 mg 现货 询价
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Customer Review

PD98059 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 311 篇科研文献

WB
IF

    PD98059 purchased from MCE. Usage Cited in: Int Immunopharmacol. 2023 Feb 1;116:109763.  [Abstract]

    PD98059 (0,10,30 μM; 24 h) inhibits the expression of p-ERK, Nrf2, Hif-1α, and IL-17D in NCM460 cells.

    PD98059 purchased from MCE. Usage Cited in: Redox Biol. 2019 Apr;22:101133.  [Abstract]

    The effects of inhibitor PD98059 on the phosphorylated-ERK1/2, total ERK1/2, Thr181-phosphorylated tau, Thr205-phosphorylated tau, total tau and ROS production in different groups with or without Aβ25-35/FGF21.

    PD98059 purchased from MCE. Usage Cited in: Mol Cell. 2018 Feb 1;69(3):480-492.e7.  [Abstract]

    ERK is important for Nur77 phosphorylation. MV3 cells are pretreated with different kinase inhibitors (PD98059, 40 μM; SB202190, 20 μM; SP600125, 25 μM) before 3 hr of glucose starvation.

    PD98059 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2018 Mar;75(6):1117-1132.  [Abstract]

    Sertoli cells (SC) are pretreated with the PD98059 for 1 h followed by a 24-h treatment with MC-LR. Expression levels of MMP-8, c-Jun, c-Fos, p-ERK, ERK, p-JNK, and JNK are determined by western blotting.

    PD98059 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2018 Jul;75(14):2627-2641.  [Abstract]

    RAW264.7 macrophages are pre-treated with the inhibitor of ERK, JNK, P38, P65, and AKT signal pathway.Western blot analyzes the non- and phosphorylation of ERK, JNK, P38, P65, and AKT.

    PD98059 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Feb;98:36-44.  [Abstract]

    Resveratrol (RES) inhibits epithelial-mesenchymal transition (EMT) and extracellular matrix (ECM) remodeling of renal cell carcinoma (RCC) cells via the Akt and ERK1/2 signaling pathway. RCC cell lines are treated with RES (0, 50, 100 μM) and 50 μM PD98059 for 24 h. Levels of Akt, p-Akt, ERK1/2, p-ERK1/2 proteins are examined by Western blot.

    PD98059 purchased from MCE. Usage Cited in: Mol Oncol. 2018 Mar;12(3):305-321.  [Abstract]

    Western blot analysis of the expression level of EGFR, Sp1, total and phosphorylated Erk1/2 proteins in cell lysates from two breast cancer cells pretreated with PD98059 and then stimulated with TGF-β for the indicated times

    PD98059 purchased from MCE. Usage Cited in: J Agric Food Chem. 2018 Jun 27;66(25):6317-6325.  [Abstract]

    HepG2 cells are pre-incubated with 20 µM SB203580, SP600125 and PD98059 for 1 h and then treated with tangeretin(20µM) for 24 h.

    PD98059 purchased from MCE. Usage Cited in: Sci Rep. 2018 Feb 12;8(1):2848.  [Abstract]

    The expression of EGFR, p-EGFR, ERK, p-ERK and FOS in four groups (from left to right: 50 μM PD98059, 30 min; control; pretreatment with 50 μM PD98059, 30 min, then intervened with 0.1 mg/L BER 15 min; 0.1 mg/L BER for 15 min) are examined using western blot.

    PD98059 purchased from MCE. Usage Cited in: Toxicology. 2018 Dec 1;410:222-230.  [Abstract]

    SH-SY5Y cells are pretreated with MEK inhibitor PD98059 (10 μM) for 1 h, then incubated with NaF (60 mg/L) for 24 h. Representative images of western blotting for BDNF, TrkB and p-ERK1/2 in SH-SY5Y cells.

    PD98059 purchased from MCE. Usage Cited in: Mol Cell Biochem. 2018 Feb;439(1-2):117-129.  [Abstract]

    Protein expression levels of E-cadherin N-cadherin, p-ERK, ERK, TGF-β1, p-Smad2, and p-Smad3 in each group are analyzed by western blotting.

    PD98059 purchased from MCE. Usage Cited in: World J Gastroenterol. 2018 Feb 21;24(7):819-832.  [Abstract]

    HSCs are pretreated with AICAR (500 μM), LY294002 (20 μM), PD98059 (10 μM), or Rapamycin (100 nM) for 2 h and then incubated with or without CoCl2 (150 μM) for 12 h. Expression levels of HIF-1α and VEGF are measured by Western blot analysis;

    PD98059 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Jan 1;495(1):781-786.  [Abstract]

    Representative images of migrated cells. HUVECs are pretreated with PD98059 (10 μM), SCH772984 (500 nM) or mock control for 2 h, and seeded in upper chambers of transwell inserts. VEGF (100 ng/ml), Scg3 (1 μg/ml) or PBS in medium with reduced FBS is added to bottom chambers in the presence or absence of the inhibitor. After culturing for 4 or 20 h, cells migrated to the lower surface of transwell membrane are stained with DAPI.

    PD98059 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Dec 9;507(1-4):253-259.  [Abstract]

    The expression of p-ERK1/2, ERK1/2, AGCAN and COL2 detected by Western blot in degenerated NP cells treated with or without rhLIF (100 ng/ml) and PD98059 (0 μM, 25 μM, 50 μM) for 48 h.

    PD98059 purchased from MCE. Usage Cited in: Mol Immunol. 2017 Jul;87:161-170.  [Abstract]

    Effect of TLR2 on autophagy activation via ERK1/2 signaling pathway activation in MG-infected RAW264.7 cells. RAW264.7 cells transfected with TLR2 siRNA/control siRNA is then infected with MG for 30 min prior to PD98059. The expression levels of Beclin1, LC3-II/I, p-JNK, p-ERK1/2 and p-p38 are examined by Western blot.

    PD98059 purchased from MCE. Usage Cited in: Hum Mol Genet. 2017 Sep 15;26(18):3553-3563.  [Abstract]

    Immunofluorescence analysis for expression of the I-cell marker ΔNP63 on proximal sections of ureters explanted from E12.5 wildtype (control) embryos and cultured for 6 d in the presence of solvent (DMSO) (A), the AKT inhibitor (AKT-i) MK2206 (B), the P38 inhibitor (P38-i) SB203580 (C), the ERK1/2 inhibitor (ERK1/2-i) PD98059 (D) or combinations as indicated (E and F).

    PD98059 purchased from MCE. Usage Cited in: Exp Ther Med. 2017 Apr;13(4):1353-1359.  [Abstract]

    Hippocampal neuron lysates are subjected to western blotting to evaluate Nrf2 levels and the phosphorylation of ERK in the presence and absence of PD98059.

    PD98059 purchased from MCE. Usage Cited in: Biomed Res. 2017; 28 (8): 3383-3386

    Effects of various protease inhibitors on HO-1 and P-gp protein expressions.

    查看 MEK 亚型特异性产品:

    查看所有亚型
    MEK1 MEK2 MEK5 MEK

    查看 ERK 亚型特异性产品:

    查看所有亚型
    ERK ERK1 ERK2 ERK5 ERK8

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy[1][2][3].

    IC50 & Target[1][3]

    MEK1

    2-7 μM (IC50)

    MEK2

    50 μM (IC50)

    ERK1

     

    ERK2

     

    Autophagy

     

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    C6 IC50
    4.2 μM
    Compound: PD98059
    Inhibition of MEK1/2 in rat IEC6 cells assessed as reduction in ERK1/2 loop phosphorylation dosed 30 mins before to stimulation with 10% serum for 5 mins by immunoblotting method
    Inhibition of MEK1/2 in rat IEC6 cells assessed as reduction in ERK1/2 loop phosphorylation dosed 30 mins before to stimulation with 10% serum for 5 mins by immunoblotting method
    		[PMID: 25078316]
    HT-29 IC50
    4 μM
    Compound: PD98059
    Antiproliferative activity against human HT-29 cells after 5 days by WST1 assay
    Antiproliferative activity against human HT-29 cells after 5 days by WST1 assay
    		[PMID: 25078316]
    体外研究
    (In Vitro)

    PD98059 (20 μM；24 小时) 导致 OCI-AML-3 细胞 G1 期细胞周期停滞[4]。
    PD98059 (10 μM；22 小时) 导致浓度依赖性ERK1 和 ERK2 双磷酸化形式的减少[1]。
    PD98059 既可防止 ERK 激活，又可阻断 TDP-43 和 HuR 阳性 SGs 的形成[7]。

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

    PD98059 相关抗体:

    Cell Cycle Analysis[4]

    Cell Line: OCI-AML-3 cells
    Concentration: 20 μM
    Incubation Time: 24 hours
    Result: Caused G1-phase cell cycle arrest.

    Western Blot Analysis[1]

    Cell Line: MCF10A-Neo, MCF10ANeoT cells
    Concentration: 10 μM
    Incubation Time: 22 hours
    Result: Phosphorylated ERK forms were almost completely eliminated in both cell lines.
    体内研究
    (In Vivo)

    PD98059 (10 mg/kg；腹腔注射；在酵母聚糖后 1 和 6 小时) 显著降低注射酵母聚糖的小鼠中的 p-ERK1/2 水平[3]。

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

    Animal Model: Male CD mice[3]
    Dosage: 10 mg/kg
    Administration: Intraperitoneal injection; 1 and 6 hours after Zymosan
    Result: Significantly reduced the level of p-ERK1/2.
    分子量

    267.28

    Formula

    C16H13NO3
    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, protect from light

    *In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 33.33 mg/mL (124.70 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.7414 mL 18.7070 mL 37.4139 mL
    5 mM 0.7483 mL 3.7414 mL 7.4828 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, 1 year; -20°C, 6 months (protect from light)。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    • 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    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (7.78 mM); 悬浊液; 超声助溶

      此方案可获得 2.08 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例，取 100 μL 20.8 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。

    以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 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： 50% PEG300    50% Saline

      Solubility: 10 mg/mL (37.41 mM); 悬浊液; 超声助溶

    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）。

    *In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

    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: 99.96%

    COA (286 KB) LCMS (92 KB)

    产品使用指南 (1538 KB)
    参考文献

    PD98059 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, 1 year; -20°C, 6 months (protect from light)。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.7414 mL 18.7070 mL 37.4139 mL 93.5349 mL
    5 mM 0.7483 mL 3.7414 mL 7.4828 mL 18.7070 mL
    10 mM 0.3741 mL 1.8707 mL 3.7414 mL 9.3535 mL
    15 mM 0.2494 mL 1.2471 mL 2.4943 mL 6.2357 mL
    20 mM 0.1871 mL 0.9353 mL 1.8707 mL 4.6767 mL
    25 mM 0.1497 mL 0.7483 mL 1.4966 mL 3.7414 mL
    30 mM 0.1247 mL 0.6236 mL 1.2471 mL 3.1178 mL
    40 mM 0.0935 mL 0.4677 mL 0.9353 mL 2.3384 mL
    50 mM 0.0748 mL 0.3741 mL 0.7483 mL 1.8707 mL
    60 mM 0.0624 mL 0.3118 mL 0.6236 mL 1.5589 mL
    80 mM 0.0468 mL 0.2338 mL 0.4677 mL 1.1692 mL
    100 mM 0.0374 mL 0.1871 mL 0.3741 mL 0.9353 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:

    PD98059167869-21-8PD 98059PD-98059MEKERKAryl Hydrocarbon ReceptorAutophagyMitogen-activated protein kinase kinaseMAPKKMAP2KExtracellular signal regulated kinasesAhRInhibitorinhibitorinhibit

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