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

EPZ020411 

Cat. No.: HY-12970
Handling Instructions

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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Top Publications Citing Use of Products

    EPZ020411 purchased from MCE. 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.
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    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].

    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

    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.
    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Purity & Documentation
    References
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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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    Product Name:
    EPZ020411
    Cat. No.:
    HY-12970
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