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    InvivoChem Cat #: V0387
    CAS #: 1346572-63-1Purity ≥98%

    Description: GSK503 (GSK-503) is a novel, potent and specific inhibitor of Enhancer of zeste homolog 2 (EZH2) methyltransferase inhibitor with potential antitumor activity. It inhibits EZH2 with Kiapp of 3 to 27 nM. GSK503 demostrates excellent antiproliferative activity and high in vivo antitumor efficacy in a melanoma mouse model.

    References: Cancer Cell. 2013 May 13;23(5):677-92; Nat Commun. 2015 Jan 22;6:6051. 

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    Molecular Weight (MW)526.67
    CAS No.1346572-63-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (189.8 mM)
    Water: <1 mg/mL
    Ethanol: 26 mg/mL warmed (49.4 mM)

    GSK 503; GSK503; GSK-503

    Chemical Name: N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide


    InChi Code: InChI=1S/C31H38N6O2/c1-19(2)37-18-21(4)29-25(30(38)33-17-26-20(3)13-22(5)34-31(26)39)14-24(15-27(29)37)23-7-8-28(32-16-23)36-11-9-35(6)10-12-36/h7-8,13-16,18-19H,9-12,17H2,1-6H3,(H,33,38)(H,34,39)

    SMILES Code: O=C(C1=CC(C2=CC=C(N3CCN(C)CC3)N=C2)=CC4=C1C(C)=CN4C(C)C)NCC5=C(C)C=C(C)NC5=O 

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    In Vitro

    In vitro activity: GSK503 inhibits the methyltransferase activity of WT and mutant EZH2 with similar potency. In a panel of seven DLBCL cell lines, GSK503 causes growth inhibition and the effects are enhanced by ABT737 or Obatoclax.

    Kinase Assay: GSK503 is profiled to assess inhibition against a panel of histone acetylases. GSK503 is dissolved in DMSO and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM, with a final DMSO concentration of 2%. Anacardic Acid is used as positive control for CBP, GCN5, and pCAF and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM. Curcumin is used as positive control for KAT5, MYST2/KAT7, MYST4/KAT6B, and p300, and tested in 10-dose IC50 mode with 3-fold serial dilution starting at 100 μM. Reactions are carried out at 3.08 μM Acetyl-CoA. For CBP, GCN5, MYST2/KAT7, pCAF, and p300, the substrate used is histone H3. For KAT5 and MYST4/KAT6B the substrates used are histone H2A and histone H4, respectively.

    In VivoIn C57BL6 mice immunized with SRBC, GSK503 (150 mg/kg, i.p.) reduced the level of H3K27me3 in splenocytes. In male SCID mice bearing SUDHL4 and SUDHL6 tumors, GSK503 (150 mg/kg, i.p.) inhibits tumor growth. In C57Bl/6 mice bearing murine B16-F10 tumors, GSK503 (150 mg/kg, i.p.) significantly reduces global H3K27me3 levels, inhibits tumor growth and virtually abolishes metastases formation.
    Animal modelMale SCID mice bearing SUDHL4 and SUDHL6 tumors
    Formulation & DosageDissolved in 20% captisol;  150 mg/kg; i.p. injection
    ReferencesCancer Cell. 2013 May 13;23(5):677-92; Nat Commun. 2015 Jan 22;6:6051. 

    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Mutant EZH2 Induces Germinal Center Hyperplasia. Cancer Cell. 2013 May 13; 23(5): 677–692.


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