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GSK591

Name: GSK591
Brand: TargetMol
SKU: T6853
Price: 40 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T6853Cas No. 1616391-87-7

Alias GSK3203591, EPZ015866

GSK591 (GSK3203591), Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM).

GSK591

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Purity: 99.59%

Catalog No. T6853Alias GSK3203591, EPZ015866Cas No. 1616391-87-7

GSK591 (GSK3203591), Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$40	In Stock	In Stock
2 mg	$56	In Stock	In Stock
5 mg	$102	In Stock	In Stock
10 mg	$147	In Stock	In Stock
25 mg	$297	In Stock	In Stock
50 mg	$448	In Stock	In Stock
100 mg	$629	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$108	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.59%

Appearance:Solid

Color:White

Resource Download

COA HNMR HPLC

Product Introduction

Bioactivity

Description	GSK591 (GSK3203591), Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM).
Targets&IC50	PRMT5:11 nM
In vitro	In an in vitro biochemical assay, GSK591 potently inhibits the PRMT5/MEP50 complex from methylating (histone) H4 with IC50 = 11 nM. In Z-138 cells, GSK591 inhibits the symmetric arginine methylation of SmD3 with EC50 = 56 nM. Further, GSK591 is selective for PRMT5 (up to 50 micromolar) relative to a panel of methyltransferases[1][2].
Kinase Assay	Selectivity profiling experiments: The lysates (5 mg of total protein each) are preincubated with 0 (DMSO control), 2.5 nM, 25 nM, 250 nM, 2.5 μM or 25 μM free compound (GSK690693 or GSK2141795) on an end-over-end shaker for 45 min at 4 °C. Subsequently, lysates are incubated with beads (coupled Akt probe or kinobeads) for 1 h at 4 °C, for both qualitative and quantitative experiments. The beads are washed with 1× CP buffer and collected by centrifugation. Bound proteins are eluted with 2× NuPAGE LDS sample buffer, and eluates are reduced and alkylated by 50 mM dithiothreitol and 55 mM iodoacetamide.
Synonyms	GSK3203591, EPZ015866

Chemical Properties

Molecular Weight	380.48
Formula	C₂₂H₂₈N₄O₂
Cas No.	1616391-87-7
Smiles	O[C@@H](CNC(=O)c1ccnc(NC2CCC2)c1)CN1CCc2ccccc2C1
Relative Density.	1.252 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (657.06 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.26 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6283 mL	13.1413 mL	26.2826 mL	131.4130 mL
5 mM	0.5257 mL	2.6283 mL	5.2565 mL	26.2826 mL
10 mM	0.2628 mL	1.3141 mL	2.6283 mL	13.1413 mL
20 mM	0.1314 mL	0.6571 mL	1.3141 mL	6.5706 mL
50 mM	0.0526 mL	0.2628 mL	0.5257 mL	2.6283 mL
100 mM	0.0263 mL	0.1314 mL	0.2628 mL	1.3141 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc