1. MAPK/ERK Pathway Stem Cell/Wnt Epigenetics
  2. ERK Epigenetic Reader Domain
  3. XMD8-92

XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with Kds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with Kds of 190, 600 and 890 nM, respectively. Anti-cancer activity.

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

XMD8-92 Chemical Structure

XMD8-92 Chemical Structure

CAS No. : 1234480-50-2

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 65 In-stock
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Customer Review

Based on 13 publication(s) in Google Scholar

Top Publications Citing Use of Products

    XMD8-92 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.

    XMD8-92 purchased from MedChemExpress. Usage Cited in: PLoS One. 2015 Apr 17;10(4):e0125054.  [Abstract]

    The induction of c-Fos is blocked by inhibition of the ERK5 pathway. 4B12 cells (2.5 × 104) are pretreated with or without BIX02189 or XMD8-92 for 6 hrs and then cultured in the presence of M-CSF (10 ng/mL) for 24 hrs. The expression of c-Fos is measured by Western blot analysis.

    XMD8-92 purchased from MedChemExpress. Usage Cited in: Sci Signal. 2014 Oct 28;7(349):ra102.  [Abstract]

    Activation of ERK5 in neuroblastoma cell lines expressing activated ALK. (A to C) Immunoblotting for the indicated proteins in neuroblastoma cells CLB-BAR (A), CLB-GE (B), and IMR32 (C) cultured on six-well plates in complete growth medium and treated with inhibitors as indicated for 6 hours alone (A and B) or before (C) stimulation with mAb46 for 30 min.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with Kds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with Kds of 190, 600 and 890 nM, respectively. Anti-cancer activity[1][2].

    IC50 & Target[1]

    BMK1

    80 nM (Kd)

    BRD4

    190 nM (Kd)

    In Vitro

    XMD8-92 (0-5 Μm; 48 hours) inhibits the proliferation of HMEC and cancer cells[1].
    XMD8-92 effectively inhibits BMK1 activation as well as induces PML’s (promyelocytic leukemia protein) downstream effector, p21. XMD8-92 significantly inhibits basic fibroblast growth factor (bFGF) induced angiogenesis in Matrigel plugs. XMD8-92 significantly induces p21 expression in HeLa and A549 cells[1].

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

    Cell Viability Assay[1]

    Cell Line: HMEC, A549 and HeLa cells
    Concentration: 0.16, 0.32, 0.63, 1.25, 2.5 or 5 μM
    Incubation Time: 48 hours
    Result: Inhibited the proliferation of HMEC and cancer cells.
    In Vivo

    XMD8-92 (i.p.; twice a day for 28 days) significantly inhibits the growth of the xenografted human tumors[1].

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

    Animal Model: HeLa Xenograft Model (6-week-old Nod/Scid mice)[1]
    Dosage: 50 mg/kg
    Administration: I.p.; twice a day for 28 days
    Result: Significantly inhibited the growth of the xenografted human tumors.
    Molecular Weight

    474.55

    Formula

    C26H30N6O3

    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    CN(C1=O)C2=CN=C(N=C2N(C3=C1C=CC=C3)C)NC4=C(C=C(C=C4)N5CCC(CC5)O)OCC

    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 : 50 mg/mL (105.36 mM; Need ultrasonic; 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 2.1073 mL 10.5363 mL 21.0726 mL
    5 mM 0.4215 mL 2.1073 mL 4.2145 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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 (5.27 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 (5.27 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

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    Dosing volume
    (per animal)

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    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: 99.67%

    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 2.1073 mL 10.5363 mL 21.0726 mL 52.6815 mL
    5 mM 0.4215 mL 2.1073 mL 4.2145 mL 10.5363 mL
    10 mM 0.2107 mL 1.0536 mL 2.1073 mL 5.2681 mL
    15 mM 0.1405 mL 0.7024 mL 1.4048 mL 3.5121 mL
    20 mM 0.1054 mL 0.5268 mL 1.0536 mL 2.6341 mL
    25 mM 0.0843 mL 0.4215 mL 0.8429 mL 2.1073 mL
    30 mM 0.0702 mL 0.3512 mL 0.7024 mL 1.7560 mL
    40 mM 0.0527 mL 0.2634 mL 0.5268 mL 1.3170 mL
    50 mM 0.0421 mL 0.2107 mL 0.4215 mL 1.0536 mL
    60 mM 0.0351 mL 0.1756 mL 0.3512 mL 0.8780 mL
    80 mM 0.0263 mL 0.1317 mL 0.2634 mL 0.6585 mL
    100 mM 0.0211 mL 0.1054 mL 0.2107 mL 0.5268 mL
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    • 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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    Product Name:
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    Cat. No.:
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