2. Epigenetics
  3. Histone Methyltransferase
  4. GSK591 hydrochloride

GSK591 hydrochloride  (Synonyms: EPZ015866 hydrochloride; GSK3203591 hydrochloride)

Cat. No.: HY-100235A
Handling Instructions Technical Support

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

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of GSK591 hydrochloride:

Other Forms of GSK591 hydrochloride:

GSK591 hydrochloride Related Antibodies

Top Publications Citing Use of Products

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

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

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

    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.

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

    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.

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

    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.

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

    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.

    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

    • Biological Activity

    • Purity & Documentation

    • Customer Review

    Description

    GSK591 (EPZ015866) hydrochloride is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 4 nM[1].

    IC50 & Target

    IC50: 4 nM (PRMT5)[1]
    Molecular Weight

    453.41

    Formula

    C22H30Cl2N4O2
    CAS No.
    SMILES

    O=C(C1=CC(NC2CCC2)=NC=C1)NC[C@H](O)CN3CC4=C(C=CC=C4)CC3.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
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    GSK591 hydrochloride Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2
    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:

    GSK5912320953-89-5EPZ015866GSK3203591GSK 591GSK-591EPZ 015866EPZ-015866GSK 3203591GSK-3203591Histone MethyltransferaseInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    GSK591 hydrochloride
    Cat. No.:
    HY-100235A
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.