2. MAPK/ERK Pathway Stem Cell/Wnt
  3. MEK ERK
  4. BIX02189

BIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM.

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CAS 番号 : 1265916-41-3

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 108 在庫あり
Solution
10 mM * 1 mL in DMSO USD 108 在庫あり
Solid
5 mg $99 在庫あり
10 mg $154 在庫あり
25 mg $310 在庫あり
50 mg $495 在庫あり
100 mg $740 在庫あり
200 mg   お問い合わせ  
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カスタマーレビュー

Based on 10 publication(s) in Google Scholar

Other Forms of BIX02189:

BIX02189 関連抗体

Top Publications Citing Use of Products

    BIX02189 purchased from MedChemExpress. Usage Cited in: Stem Cell Reports. 2018 Oct 9;11(4):929-943.  [Abstract]

    Immunoblotting of total cell lysates of CML cell lines; tubulin is a loading control; representative images from four independent experiments.

    MEK アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    MEK1 MEK2 MEK5 MEK MAP2K4/MEK4 MAP2K7/MEK7

    ERK アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    ERK ERK1 ERK2 ERK5 ERK8

    • 生物活性

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    • 純度とドキュメンテーション

    • 参考文献

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    製品説明

    BIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM.

    IC50 & Target[1]

    MEK5

    1.5 nM (IC50)

    ERK5

    59 nM (IC50)

    CSF1R (FMS)

    46 nM (IC50)

    LCK

    250 nM (IC50)

    JAK3

    440 nM (IC50)

    TGFβR1

    580 nM (IC50)

    RPS6KA6 (RSK4)

    990 nM (IC50)

    RPS6KA3 (RSK2)

    2.1 μM (IC50)

    FGFR1

    1 μM (IC50)

    KIT

    1.1 μM (IC50)

    ABL1

    2.4 μM (IC50)

    MAPK14 (p38 alpha)

    3.7 μM (IC50)

    SRC

    7.6 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    HeLa IC50
    59 nM
    Compound: BIX02189
    Inhibition of ERK5 phosphorylation in sorbitol-stimulated human HeLa cells
    Inhibition of ERK5 phosphorylation in sorbitol-stimulated human HeLa cells
    		[PMID: 23656407]
    体外実験

    BIX02189 blocks phosphorylation of ERK5, without affecting phosphorylation of ERK1/2 in sorbitol-stimulated HeLa cells. BIX02189 inhibits ERK5 phosphorylation in a dose dependent manner[1]. Fluvastatin reduces advanced glycation endproduct (AGE)-induced vascular smooth muscle cells (VSMCs) proliferation. To confirm this effect, VSMCs are treated with AGEs in the presence or absence of Fluvastatin and then subject to MTT assay. AGEs are found to dose-dependently induce cell proliferation, and this is significantly suppressed by Fluvastatin. In addition to MTT assay, the similar results are got with cell counting. This suppressive effect of Fluvastatin is prevented when VSMCs are pretreated with BIX02189. Whether ERK5 activation can reduce proliferation is also examined by using Ad-CA-MEK5α encoding a constitutively active mutant form of MEK5α (an upstream kinase of ERK5). AGE-induced proliferation determined by both MTT assay and cell counting is significantly diminished in the presence of Ad-CA-MEK5α, and Nrf2 depletion using siRNA restored AGE-induced proliferation[2].

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

    BIX02189 関連抗体
    体内実験

    Mice are treated with either 10 mg/kg of BIX02189 (in 25% DMSO) or vehicle control (same volume of 25% DMSO) by intraperitoneal injection. The nuclear localization of Nrf2 is inhibited in aortic endothelial cells from mice treated with BIX02189[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    440.55

    分子式

    C27H28N4O2
    CAS 番号
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C(N(C)C)C1=CC(NC2=O)=C(/C2=C(C3=CC=CC=C3)/NC4=CC=CC(CN(C)C)=C4)C=C1
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 49.4 mg/mL (112.13 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2699 mL 11.3494 mL 22.6989 mL
    5 mM 0.4540 mL 2.2699 mL 4.5398 mL
    10 mM 0.2270 mL 1.1349 mL 2.2699 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    体積 （開始）

    V1

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    濃度 （終了）

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.72%

    COA (254 KB) HNMR (212 KB) RP-HPLC (259 KB) MS (72 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [2]

    AGE-induced proliferation is quantified using the MTT assay. Briefly, VSMCs are cultured on 24-well plates and when ~80% confluent, medium is replaced with serum free DMEM. Cells are then pretreated with BIX02189 (2 μM) and stimulated with Fluvastatin (5 μM) for 24 h. MTT reagents are added for 4 h at 37°C the removed by washing with PBS, and eluted with DMSO. Proliferation is measured using a microplate reader at 570 nm[2].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [3]

    Mice[3]
    C57BL/6-specific pathogen-free mice are used. To determine the role of ERK5 on laminar flow-dependent Nrf2 nuclear translocation in vivo, 6-week-old male C57BL/6 mice are intraperitoneally treated with BIX02189 (10 mg/kg of body weight in 25% DMSO) or vehicle control. Following euthanization, vascular perfusion is performed with saline for 5 min followed by fixation with 4% paraformaldehyde for 5 min. Isolated aorta is incubated with 0.1% PBS with Tween, and then fat is removed. 5% goat serum is used for blocking and antibody diluents. Aortic endothelial cells are stained with anti-vascular endothelial-cadherin antibody and Topro3 for endothelial cell junction and nuclear, respectively. Cellular localization of Nrf2 is determined by immunofluorescence staining with anti-Nrf2 antibody under the Confocal microscope[3].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2699 mL 11.3494 mL 22.6989 mL 56.7472 mL
    5 mM 0.4540 mL 2.2699 mL 4.5398 mL 11.3494 mL
    10 mM 0.2270 mL 1.1349 mL 2.2699 mL 5.6747 mL
    15 mM 0.1513 mL 0.7566 mL 1.5133 mL 3.7831 mL
    20 mM 0.1135 mL 0.5675 mL 1.1349 mL 2.8374 mL
    25 mM 0.0908 mL 0.4540 mL 0.9080 mL 2.2699 mL
    30 mM 0.0757 mL 0.3783 mL 0.7566 mL 1.8916 mL
    40 mM 0.0567 mL 0.2837 mL 0.5675 mL 1.4187 mL
    50 mM 0.0454 mL 0.2270 mL 0.4540 mL 1.1349 mL
    60 mM 0.0378 mL 0.1892 mL 0.3783 mL 0.9458 mL
    80 mM 0.0284 mL 0.1419 mL 0.2837 mL 0.7093 mL
    100 mM 0.0227 mL 0.1135 mL 0.2270 mL 0.5675 mL
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    BIX02189 Related Classifications

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    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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:

    BIX021891265916-41-3BIX 02189BIX-02189MEKERKMitogen-activated protein kinase kinaseMAPKKMAP2KExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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    製品名:
    BIX02189
    製品番号:
    HY-12056
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