1. Epigenetics
  2. Histone Methyltransferase
  3. GSK591

GSK591 (Synonyms: EPZ015866; GSK3203591)

Cat. No.: HY-100235 Purity: 99.98%
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
10 mM * 1 mL in DMSO USD 145 In-stock
Estimated Time of Arrival: December 31
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 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

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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].

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.

1616391-87-7

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 : ≥ 135 mg/mL (354.81 mM)

*"≥" means soluble, but saturation unknown.

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 provided by MCE.
References

Purity: 99.98%

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KeyWords:

GSK591 | EPZ015866 | GSK3203591 | GSK 591 | GSK-591 | EPZ 015866 | EPZ-015866 | GSK 3203591 | GSK-3203591 | Histone Methyltransferase | Inhibitor | inhibitor | inhibit

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Product name:
GSK591
Cat. No.:
HY-100235
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