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

PD98059 是一種有效的選擇性的 MEK 抑制劑，IC50 為 5 μM。PD98059 與 MEK 的無活性形式結(jié)合，從而阻止上游激酶激活 MEK1 (IC50 為 2-7 μM) 和 MEK2 (IC50 為 50 μM)。PD98059 是一種 ERK1/2 信號的抑制劑。PD98059 是一種芳烴受體 (AHR) 的配體，可抑制細胞中 TCDD 結(jié)合 (IC50 為 4 μM) 和 AHR 轉(zhuǎn)化 (IC50 為 1 μM)。PD98059 還可抑制 Mycobacterium bovis Bacillus CalmetteGuerin (BCG) 誘導(dǎo)的細胞自噬 (autophagy)。

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PD98059 Chemical Structure

PD98059 Chemical Structure

CAS No. : 167869-21-8

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規(guī)格 價格 是否有貨 數(shù)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 現(xiàn)貨 詢價
1 g   詢價  
5 g   詢價  

* Please select Quantity before adding items.

Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 326 篇科研文獻

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    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 亞型特異性產(chǎn)品:

    查看 ERK 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    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

     

    細胞效力
    (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]
    體外研究
    (In Vitro)

    PD98059 (20 μM；24 小時) 導(dǎo)致 OCI-AML-3 細胞 G1 期細胞周期停滯[4]。
    PD98059 (10 μM；22 小時) 導(dǎo)致濃度依賴性ERK1 和 ERK2 雙磷酸化形式的減少[1]。
    PD98059 既可防止 ERK 激活，又可阻斷 TDP-43 和 HuR 陽性 SGs 的形成[7]。

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

    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.
    體內(nèi)研究
    (In Vivo)

    PD98059 (10 mg/kg；腹腔注射；在酵母聚糖后 1 和 6 小時) 顯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 號
    性狀

    固體

    顏色

    Light yellow to yellow

    運輸條件

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

    4°C, protect from light

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

    溶解性數(shù)據(jù)
    細胞實驗： 

    DMSO 中的溶解度 : 33.33 mg/mL (124.70 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

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

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (protect from light)。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (7.78 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.08 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

    以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請依序添加每種溶劑： 50% PEG300    50% Saline

      Solubility: 10 mg/mL (37.41 mM); 懸濁液; 超聲助溶

    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

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

    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.96%

    參考文獻

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (protect from light)。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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.

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    產(chǎn)品名稱：
    PD98059
    目錄號：
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