1. Epigenetics
  2. Histone Methyltransferase
  3. GSK591

GSK591  (Synonyms: EPZ015866; GSK3203591)

Cat. No.: HY-100235 Purity: 99.87%
COA Handling Instructions

GSK591 (EPZ015866) 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.

GSK591 Chemical Structure

GSK591 Chemical Structure

CAS No. : 1616391-87-7

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 145 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 145 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
25 mg USD 444 In-stock
Estimated Time of Arrival: December 31
50 mg USD 744 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1140 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 8 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GSK591 purchased from MCE. 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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GSK591 (EPZ015866) 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]

    In Vitro

    GSK591 (5 μM; MCF7, T47D, and MCF10A cells) treatment suppresses breast cancer stem cells (BCSCs) proliferation and self-renewal. GSK591 reduces BCSCs numbers in vitro[2].

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

    Cell Proliferation Assay[2]

    Cell Line: MCF7, T47D, and MCF10A cells
    Concentration: 5 μM
    Incubation Time:
    Result: Suppressed BCSCs proliferation and self-renewal.
    Molecular Weight

    380.48

    Formula

    C22H28N4O2

    CAS No.
    SMILES

    O=C(C1=CC(NC2CCC2)=NC=C1)NC[[email protected]](O)CN3CC4=C(C=CC=C4)CC3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (262.83 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6283 mL 13.1413 mL 26.2826 mL
    5 mM 0.5257 mL 2.6283 mL 5.2565 mL
    10 mM 0.2628 mL 1.3141 mL 2.6283 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.25 mg/mL (5.91 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.25 mg/mL (5.91 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.25 mg/mL (5.91 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.87%

    References
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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.

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

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    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

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    × = ×
    C1   V1   C2   V2

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    Inquiry Information

    Product Name:
    GSK591
    Cat. No.:
    HY-100235
    Quantity:
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