2. MAPK/ERK Pathway Stem Cell/Wnt
  3. ERK
  4. XMD17-109

XMD17-109 is a novel, specific ERK-5 inhibitor, with an IC50 of 162 nM.

For research use only. We do not sell to patients.

XMD17-109 Chemical Structure

XMD17-109 Chemical Structure

CAS No. : 1435488-37-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 138 In-stock
Solution
10 mM * 1 mL in DMSO USD 138 In-stock
Solid
1 mg USD 46 In-stock
5 mg USD 98 In-stock
10 mg USD 180 In-stock
50 mg USD 460 In-stock
100 mg USD 695 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 6 publication(s) in Google Scholar

XMD17-109 Related Antibodies

Top Publications Citing Use of Products

    XMD17-109 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Jun 7;7(23):34322-40.  [Abstract]

    HCT116 parental cells are treated for up to 48 h with increasing doses of 5-FU in combination with 4 μM XMD8-92 or 2 μM XMD17-109, two highly-selective ERK5 pharmacological inhibitors.

    View All ERK Isoform Specific Products:

    View All Isoforms
    ERK ERK1 ERK2 ERK5 ERK8

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    XMD17-109 is a novel, specific ERK-5 inhibitor, with an IC50 of 162 nM.

    IC50 & Target[1]

    ERK5

    162 nM (IC50)

    LRRK2[G2019S]

    339 nM (IC50)

    In Vitro

    XMD17-109 (Compound 26) inhibits ERK5 biochemically with an IC50 of 0.162 ± 0.006 μM, and blocks pidermal growth factor induced ERK5 autophosphorylation with an EC50 of 0.09 ± 0.03 μM in cells. XMD17-109 also inhibits LRRK2[G2019S] with an IC50 of 339 nM[1]. XMD17-109 demonstrats low nanomolar cellular activity judged by the significant dose-dependent reduction of mobility shifted phosphorylated ERK5 bands from sorbitol stimulated cells. XMD17-109 completely inhibits the ERK5-mediated AP1 transcriptional activity at 30 μM and has an EC50 of 4.2 μM[2].

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

    XMD17-109 Related Antibodies
    Molecular Weight

    638.80

    Formula

    C36H46N8O3
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1C2=C(C=CC=C2)N(C3CCCC3)C4=NC(NC5=C(OCC)C=C(C(N6CCC(N7CCN(C)CC7)CC6)=O)C=C5)=NC=C4N1C
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (156.54 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5654 mL 7.8272 mL 15.6544 mL
    5 mM 0.3131 mL 1.5654 mL 3.1309 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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 (3.91 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 (3.91 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
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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.
    Purity & Documentation

    Purity: 99.20%

    COA (260 KB) LCMS (92 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    HeLa cells are maintained in DMEM supplemented with 10% FBS, 2 mM l-glutamine, 50 U/mL penicillin G, and 50 μg/mL streptomycin. Before use HeLa cells are serum starved for 16 h in DMEM supplemented with 2 mM l-glutamine, 50 U/mL penicillin G, and 50 μg/mL streptomycin. HeLa cells are then incubated with ERK5-IN-1 at the indicated concentrations for 1 h prior to stimulation with 0.5mol/Lsorbitol for 30 min. Cells are lysed in Triton lysis buffer (50 mM Tris-HCl, pH 7.5, 1 mM EGTA, 1 mM EDTA, 1 mM sodium orthovanadate, 50 mM sodium fluoride, 1 mM sodium pyrophosphate, 0.27mol/Lsucrose, 1 μM microcystin-LR, 1% (v/v) Triton X-100, 0.1% (v/v) 2-mercaptoethanol) and 20 μg of protein loaded per well. Samples are run on 8% polyacrylamide gels using standard methods. Proteins are transferred onto nitrocellulose membranes and specific proteins detected by immunoblotting.

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

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.5654 mL 7.8272 mL 15.6544 mL 39.1359 mL
    5 mM 0.3131 mL 1.5654 mL 3.1309 mL 7.8272 mL
    10 mM 0.1565 mL 0.7827 mL 1.5654 mL 3.9136 mL
    15 mM 0.1044 mL 0.5218 mL 1.0436 mL 2.6091 mL
    20 mM 0.0783 mL 0.3914 mL 0.7827 mL 1.9568 mL
    25 mM 0.0626 mL 0.3131 mL 0.6262 mL 1.5654 mL
    30 mM 0.0522 mL 0.2609 mL 0.5218 mL 1.3045 mL
    40 mM 0.0391 mL 0.1957 mL 0.3914 mL 0.9784 mL
    50 mM 0.0313 mL 0.1565 mL 0.3131 mL 0.7827 mL
    60 mM 0.0261 mL 0.1305 mL 0.2609 mL 0.6523 mL
    80 mM 0.0196 mL 0.0978 mL 0.1957 mL 0.4892 mL
    100 mM 0.0157 mL 0.0783 mL 0.1565 mL 0.3914 mL
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    XMD17-109 Related Classifications

    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:

    XMD17-1091435488-37-1ERKExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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