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

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

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

EPZ020411 hydrochloride Chemical Structure

EPZ020411 hydrochloride Chemical Structure

CAS No. : 2070015-25-5

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10 mM * 1 mL in DMSO
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of EPZ020411 hydrochloride:

Top Publications Citing Use of Products

    EPZ020411 hydrochloride 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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC50 of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride 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 hydrochloride (0-20 μM; 24 h) decreases H3R2 methylation in A375 cells[1].
    EPZ020411 hydrochloride (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.

    Cell Viability Assay[2]

    Cell Line: Cultured cochleae cells
    Concentration: 20 and 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. Reduced hair cell loss caused by cisplatin treatment.
    In Vivo

    EPZ020411 hydrochloride (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 hydrochloride 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

    479.06

    Formula

    C25H39ClN4O3

    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, stored under nitrogen

    *In solvent : -80°C, 1 years; -20°C, 6 months (stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (104.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    0.1 M HCL : 50 mg/mL (104.37 mM; ultrasonic and warming and adjust pH to 2 with HCl and heat to 60°C)

    H2O : 20 mg/mL (41.75 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0874 mL 10.4371 mL 20.8742 mL
    5 mM 0.4175 mL 2.0874 mL 4.1748 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 years; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • 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 (5.22 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 (5.22 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  PBS

      Solubility: 25 mg/mL (52.19 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

    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.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation

    Purity: 98.15%

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

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO / 0.1 M HCL 1 mM 2.0874 mL 10.4371 mL 20.8742 mL 52.1855 mL
    5 mM 0.4175 mL 2.0874 mL 4.1748 mL 10.4371 mL
    10 mM 0.2087 mL 1.0437 mL 2.0874 mL 5.2186 mL
    15 mM 0.1392 mL 0.6958 mL 1.3916 mL 3.4790 mL
    20 mM 0.1044 mL 0.5219 mL 1.0437 mL 2.6093 mL
    25 mM 0.0835 mL 0.4175 mL 0.8350 mL 2.0874 mL
    30 mM 0.0696 mL 0.3479 mL 0.6958 mL 1.7395 mL
    40 mM 0.0522 mL 0.2609 mL 0.5219 mL 1.3046 mL
    DMSO / 0.1 M HCL 50 mM 0.0417 mL 0.2087 mL 0.4175 mL 1.0437 mL
    60 mM 0.0348 mL 0.1740 mL 0.3479 mL 0.8698 mL
    80 mM 0.0261 mL 0.1305 mL 0.2609 mL 0.6523 mL
    100 mM 0.0209 mL 0.1044 mL 0.2087 mL 0.5219 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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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