1. Epigenetics Apoptosis
  2. Histone Methyltransferase Apoptosis
  3. EPZ020411

EPZ020411 is a selective inhibitor of PRMT6 with an IC50 of 10 nM, has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 can be used for the research of cancer.

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

EPZ020411 Chemical Structure

EPZ020411 Chemical Structure

CAS No. : 1700663-41-7

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5 mg USD 165 In-stock
10 mg USD 275 In-stock
50 mg USD 715 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of EPZ020411:

Top Publications Citing Use of Products

    EPZ020411 purchased from MedChemExpress. Usage Cited in: Exp Cell Res. 2022 Nov 16;422(1):113413.  [Abstract]

    EPZ020411(PRMT6i; 200-1000 nM) in combination with GSK591(PRMT5i; 200-1000 nM) exhibits a synergistic anti-proliferative effect on HCT116 and SW620 cells.

    View All Histone Methyltransferase Isoform Specific Products:

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    EPZ020411 is a selective inhibitor of PRMT6 with an IC50 of 10 nM, has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 can be used for the research of cancer[1][2].

    IC50 & Target

    PRMT6

    0.01 μM (IC50)

    PRMT1

    0.119 μM (IC50)

    PRMT8

    0.223 μM (IC50)

    In Vitro

    EPZ020411 (0-20 μM; 24 h) decreases H3R2 methylation in A375 cells[1].
    EPZ020411 (20-40 μM; 6 h) reduces neomycin- and cisplatin-induced cell apoptosis and increases hair cell survival[2].

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

    Western Blot Analysis[1]

    Cell Line: A375 cells
    Concentration: 0-20 μM
    Incubation Time: 24 hours
    Result: Dose-dependently decreased H3R2 methylation in A375 cells with an IC50 of 0.634 μM.

    Apoptosis Analysis[2]

    Cell Line: Cultured cochleae cells
    Concentration: 20-40 μM
    Incubation Time: 6 hours
    Result: Suppressed the apoptotic cascade induced by aminoglycosides and also inhibited cisplatin-induced apoptosis in the hair cells of the cochlear explants after pretreatment deposed. Also reduced hair cell loss caused by cisplatin treatment.
    In Vivo

    EPZ020411 (10 mg/kg; i.p. once) reduces neomycin- and cisplatin-induced hearing loss in C57BL/6J wild-type mice with acute ototoxicity model[2].
    1.19 Pharmacokinetic Parameters of EPZ020411 in rats[1].

    Rats
    IV 1 mg/kg
    Rats
    SC 5 mg/kg
    CL (mL/min/kg) 19.7±1.0
    Vss (L/kg) 11.1±1.6
    t1/2 (h) 8.54±1.43 9.19±1.60
    tmax (h) 0.444
    Cmax (ng/mL) 844±306
    AUC0-τ (h·ng/mL) 745±34 2456±135
    AUC0-inf (h·ng/mL) 846±45 2775±181
    F (%) 65.6±4.3

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

    Animal Model: C57BL/6J wild-type mice at P28 with acute ototoxicity model[2]
    Dosage: 10 mg/kg
    Administration: Intraperitoneal injection; 10 mg/kg once
    Result: Significantly reduced neomycin- and cisplatin-induced HC loss and showed no effect without neomycin injection with mice.
    Molecular Weight

    442.59

    Formula

    C25H38N4O3

    CAS No.
    Appearance

    Oil

    Color

    Off-white to yellow

    SMILES

    CNCCN(C)CC1=CNN=C1C2=CC=C(O[C@H]3C[C@H](OCCC4CCOCC4)C3)C=C2

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (225.94 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 2.2594 mL 11.2971 mL 22.5943 mL
    5 mM 0.4519 mL 2.2594 mL 4.5189 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    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 (5.65 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 (5.65 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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    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: 98.06%

    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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2594 mL 11.2971 mL 22.5943 mL 56.4857 mL
    5 mM 0.4519 mL 2.2594 mL 4.5189 mL 11.2971 mL
    10 mM 0.2259 mL 1.1297 mL 2.2594 mL 5.6486 mL
    15 mM 0.1506 mL 0.7531 mL 1.5063 mL 3.7657 mL
    20 mM 0.1130 mL 0.5649 mL 1.1297 mL 2.8243 mL
    25 mM 0.0904 mL 0.4519 mL 0.9038 mL 2.2594 mL
    30 mM 0.0753 mL 0.3766 mL 0.7531 mL 1.8829 mL
    40 mM 0.0565 mL 0.2824 mL 0.5649 mL 1.4121 mL
    50 mM 0.0452 mL 0.2259 mL 0.4519 mL 1.1297 mL
    60 mM 0.0377 mL 0.1883 mL 0.3766 mL 0.9414 mL
    80 mM 0.0282 mL 0.1412 mL 0.2824 mL 0.7061 mL
    100 mM 0.0226 mL 0.1130 mL 0.2259 mL 0.5649 mL
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    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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    Cat. No.:
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