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GSK591 hydrochloride

(Synonyms: EPZ015866 hydrochloride; GSK3203591 hydrochloride)
15 Cited Publications
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Based on 15 publication(s) in Google Scholar

GSK591 (EPZ015866) hydrochloride is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 4 nM.

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

  • CAS No.: 2320953-89-5
  • Formula: C22H30Cl2N4O2
  • Molecular Weight:453.41
  • Storage:

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

  • GSK591 hydrochloride Chemical Structure
    GSK591 hydrochloride Chemical Structure
  • Experimental Validation Results for GSK591 hydrochloride
  • Experimental Validation Results for GSK591 hydrochloride
  • Experimental Validation Results for GSK591 hydrochloride
  • Experimental Validation Results for GSK591 hydrochloride
  • Experimental Validation Results for GSK591 hydrochloride
CAS No.: 2320953-89-5
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Publications Citing Use of MedChemExpress (MCE) GSK591 hydrochloride

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Cell Proliferation/Viability AssayWBIn Vivo Efficacy StudyIP
  • Cell Proliferation/Viability Assay
  • Cell Proliferation/Viability Assay
  • WB
  • In Vivo Efficacy Study
  • IP

All Histone Methyltransferase Isoforms

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  • GSK591 hydrochloride Chemical Structure
    GSK591 hydrochloride Chemical Structure
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    GSK591 hydrochloride purchased from MedChemExpress. Usage Cited in: Exp Cell Res. 2022 Nov 16;422(1):113413. [Abstract]

    Customer Validation
     GSK591 (PRMT5i; 200-1000 nM) in combination with EPZ020411 (PRMT6i; 200-1000 nM) exhibits a synergistic anti-proliferative effect on HCT116 and SW620 cells.

  • 1/16

    GSK591 hydrochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Jan 27;11(8):3742-3759. [Abstract]

    Customer Validation
     The compound dose-response matrix for proliferation inhibition of HCT116 and SW480 cells treated with PRMT5i (GSK591) (10-100 μM; 7 days) and EZH2i (GSK126). Color gradation indicates percentage viability at the indicated dose combination. Combination index (CI) plots for 100 nM PRMT5i (GSK591) (top) or EZH2i (GSK126) (bottom) with graded doses of EZH2i (GSK126) or PRMT5i (GSK591) in HCT116 and SW480 cells.

  • 1/16

    GSK591 hydrochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Jan 27;11(8):3742-3759. [Abstract]

    Customer Validation
     Immunoblots of PRMT5, EZH2 and CDKN2B (p15INK4b) protein levels in HCT116 and SW480 cells following treatment with PRMT5i (GSK591; 100 nM), EZH2i (GSK126; 100 nM), or PRMT5i (GSK591; 100 nM) + EZH2i (GSK126; 100 nM). GAPDH was used as a loading control. Western blot analysis clearly showed that the selected combination of PRMT5i (GSK591) and EZH2i (GSK126) robustly activated the protein expression of CDKN2B.

  • 1/16

    GSK591 hydrochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Jan 27;11(8):3742-3759. [Abstract]

    Customer Validation
     Representative images of xenograft tumors excised from mice. Control, PRMT5i (GSK591) (100 mg/kg; i.p.; every other day for a month), EZH2i (GSK126) (100 mg/kg; i.p.; every other day for a month), or PRMT5i (GSK591) + EZH2i (GSK126)-treated HCT116 cells were subcutaneously injected into the flank of nude mice.

  • 1/16

    GSK591 hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 21;10(1):3761. [Abstract]

    Customer Validation
     ChIP assay analysis of the enrichment of H3R2me1 and H3R2me2s on the promoter of SLC7A11 in the indicated cells treated with PRMT5 inhibitor GSK591 (5 μM, 1 h). ChIP-qPCR of Histone 3 served as the control. The results showed that inhibiting PRMT5 activity using the PRMT5 inhibitor GSK591 significantly reduced the levels of H3R2me1 and H3R2me2s on the SLC7A11 promoter in CPT-treated cells.

  • GSK591 hydrochloride