1. Epigenetics
  2. Histone Methyltransferase
  3. Tazemetostat trihydrochloride

Tazemetostat trihydrochloride (Synonyms: EPZ-6438 trihydrochloride; E-7438 trihydrochloride)

Cat. No.: HY-13803A
Handling Instructions

Tazemetostat trihydrochloride (EPZ-6438 trihydrochloride) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat trihydrochloride inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki of 2.5 nM. Tazemetostat trihydrochloride inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat trihydrochloride inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM.

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Tazemetostat trihydrochloride Chemical Structure

Tazemetostat trihydrochloride Chemical Structure

CAS No. : 1403255-00-4

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Top Publications Citing Use of Products

    Tazemetostat trihydrochloride purchased from MCE. Usage Cited in: Toxins (Basel). 2017 May 16;9(5). pii: E162.

    Cells are treated with LeTx in the presence or absence of GSK-J4 or EPZ-6438 for 48 h. H3K27me3 level is analyzed by Western blotting.

    Tazemetostat trihydrochloride purchased from MCE. Usage Cited in: J Clin Invest. 2018 Jan 2;128(1):483-499.

    Immunoblotting for N1-ICD (n=3) in mouse podocytes exposed to 10 μM EPZ-6438 for 48 hours.

    Tazemetostat trihydrochloride purchased from MCE. Usage Cited in: Nat Struct Mol Biol. 2018 Mar;25(3):225-232.

    Western blots of extracts from E14 mESCs treated with 10 μM. EPZ6438 EZH2 inhibitor for 7 d and sampled at time points following inhibitor washout. Blots are probed with the indicated antibodies.
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    Description

    Tazemetostat trihydrochloride (EPZ-6438 trihydrochloride) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat trihydrochloride inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki of 2.5 nM. Tazemetostat trihydrochloride inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat trihydrochloride inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM[1].

    IC50 & Target[1]

    EZH2 WT

    2.5 nM (Ki)

    EZH2

    11 nM (IC50, in peptide assay)

    EZH2

    16 nM (IC50, in nucleosome assay)

    Rat EZH2

    4 nM (IC50)

    EZH1

    392 nM (IC50)

    In Vitro

    Tazemetostat (EPZ-6438) inhibits multi wild-type and mutant lymphoma cell lines proliferation with IC50s of 0.49 nM-7.6 μM[1].

    Cell Proliferation Assay[1]

    Cell Line: Wild-type and mutant lymphoma cell lines: DOHH-2 cell (EZH2 wild-type), Farage cell (EZH2 wild-type), OCI-LY19 cell (EZH2 wild-type), Toledo cell (EZH2 wild-type), KARPAS-422 (EZH2 Y646N), Pfeiffer (EZH2 A682G), RL cell line (EZH2 Y646N), SU-DHL-10 (EZH2 Y646F), SU-DHL-6 (EZH2 Y646N), WSU-DLCL2 (EZH2 Y646F)
    Concentration: 0.49 nM-7.6 μM
    Incubation Time: 11 days
    Result: Inhibited DOHH-2 cell (EZH2 wild-type; IC50=1.7 μM), Farage cell (EZH2 wild-type; IC50=99 nM), OCI-LY19 cell (EZH2 wild-type; IC50=6.2 μM), Toledo cell (EZH2 wild-type; IC50=7.6 μM), KARPAS-422 (EZH2 Y646N; IC50=1.8 nM), Pfeiffer (EZH2 A682G; IC50=0.49 nM), RL cell line (EZH2 Y646N; IC50=5.8 μM), SU-DHL-10 (EZH2 Y646F; IC50=5.8 nM), SU-DHL-6 (EZH2 Y646N; IC50=4.7 nM), WSU-DLCL2 (EZH2 Y646F; IC50=8.6 nM) proliferation.
    In Vivo

    Tazemetostat (EPZ-6438; 250 or 500 mg/kg twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors[1].

    Animal Model: SCID mice bearing s.c. G401 xenografts[1]
    Dosage: 125 mg/kg, 250 mg/kg, 500 mg/kg
    Administration: Oral; twice daily; 28 days
    Result: Practically eliminated the fast-growing G401 tumors at 250 or 500 mg/kg.
    Clinical Trial
    Molecular Weight

    682.12

    Formula

    C₃₄H₄₇Cl₃N₄O₄

    CAS No.

    1403255-00-4

    SMILES

    O=C(C1=CC(C2=CC=C(CN3CCOCC3)C=C2)=CC(N(CC)C4CCOCC4)=C1C)NCC5=C(C)C=C(C)NC5=O.[H]Cl.[H]Cl.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

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

    References
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    Keywords:

    Tazemetostat trihydrochlorideEPZ-6438 trihydrochlorideE-7438 trihydrochlorideHistone MethyltransferaseEZH2PRC2EZH1epigeneticcancerInhibitorinhibitorinhibit

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