2. Epigenetics
  3. Histone Methyltransferase
  4. GSK3368715 hydrochloride

GSK3368715 hydrochloride  (Synonyms: EPZ019997 hydrochloride)

Cat. No.: HY-128717C
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GSK3368715 (EPZ019997) hydrochloride is an orally active, reversible, SAM-noncompetitive type I protein arginine methyltransferase (PRMT) inhibitor with IC50 values of 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), and 1.7 nM (PRMT8). GSK3368715 hydrochloride induces a shift in arginine methylation states, alters exon usage, and exhibits potent anticancer activity.

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

CAS No. : 2227587-25-7

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GSK3368715 hydrochloride Related Antibodies

Top Publications Citing Use of Products

    GSK3368715 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 (EPZ019997) hydrochloride is an orally active, reversible, SAM-noncompetitive type I protein arginine methyltransferase (PRMT) inhibitor with IC50 values of 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), and 1.7 nM (PRMT8). GSK3368715 hydrochloride induces a shift in arginine methylation states, alters exon usage, and exhibits potent anticancer activity[1].

    Molecular Weight

    403.00

    Formula

    C20H39ClN4O2
    CAS No.
    SMILES

    CNCCN(CC1=CNN=C1C2CCC(COCC)(COCC)CC2)C.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 hydrochloride 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:

    GSK33687152227587-25-7EPZ019997GSK 3368715GSK-3368715EPZ 019997EPZ-019997Histone MethyltransferaseInhibitorinhibitorinhibit

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