2. Epigenetics
  3. Histone Methyltransferase
  4. GSK3368715 trihydrochloride

GSK3368715 trihydrochloride  (Synonyms: EPZ019997 trihydrochloride)

Cat. No.: HY-128717B
Handling Instructions Technical Support

GSK3368715 trihydrochloride (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 trihydrochloride (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.

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

CAS No. : 2227587-26-8

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GSK3368715 trihydrochloride Related Antibodies

Top Publications Citing Use of Products

    GSK3368715 trihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2024 Dec;20(12):1566-1576.  [Abstract]

    Immunoblot analysis and quantification of GSK3β-SNAP in MrTAC-treated HEK293T cells (10 μM; 3 h) in the presence of GSK368715 (10 μM).

    GSK3368715 trihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 23;14(1):1011.  [Abstract]

    PRMT1 inhibitor GSK3368715 (2 μM) markedly reduced the growth of HCC cells in vitro.

    GSK3368715 trihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 23;14(1):1011.  [Abstract]

    Images, weight, and volume of Huh7 tumor xenografts from BALB/c nude mice fed with a -SG diet and treated with or without GSK3368715 (100 mg/kg; p.o.; every other day).

    GSK3368715 trihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 23;14(1):1011.  [Abstract]

    GSK3368715 (2 μM; 6 h) blocked the binding of nonmethylated peptide with PRMT1 in Huh7 and PLC/PRF/5 cells.

    GSK3368715 trihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 23;14(1):1011.  [Abstract]

    Endogenous PHGDH was immunoprecipitated in Huh7 and PLC/PRF/5 cells treated with or without the PRMT1 inhibitor GSK3368715 (2 μM).

    View All Histone Methyltransferase Isoform Specific Products:

    View All Isoforms
    EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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    Description

    GSK3368715 trihydrochloride (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 trihydrochloride (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity[1].

    IC50 & Target[1]

    PRMT4

    1148 nM (IC50)

    PRMT3

    48 nM (IC50)

    PRMT1

    3.1 nM (IC50)

    PRMT6

    5.8 nM (IC50)

    PRMT8

    1.7 nM (IC50)

    In Vitro

    GSK3368715 trihydrochloride (EPZ019997) shows 50% or more growth inhibition relative to DMSO-treated cells in the majority of 249 cancer cell lines, representing 12 tumor types[1].

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

    GSK3368715 trihydrochloride Related Antibodies
    In Vivo

    GSK3368715 trihydrochloride (EPZ019997) significantly effects on the growth of BxPC3 xenografts at all doses tested, reducing tumor growth by 78% and 97% in the 150- and 300-mg/kg dose groups, respectively[1].

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

    475.92

    Formula

    C20H41Cl3N4O2
    CAS No.
    SMILES

    CNCCN(CC1=CNN=C1C2CCC(COCC)(COCC)CC2)C.Cl.Cl.Cl
    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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    GSK3368715 trihydrochloride Related Classifications

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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.

    Keywords:

    GSK3368715 trihydrochloride2227587-26-8EPZ019997 trihydrochlorideHistone MethyltransferaseInhibitorinhibitorinhibit

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