GSK591

Catalog No.S8111 Synonyms: EPZ015866, GSK3203591

For research use only.

GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM.

GSK591 Chemical Structure

CAS No. 1616391-87-7

Selleck's GSK591 has been cited by 6 Publications

1 Customer Review

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM.
Targets
PRMT5 [1]
(Cell-free assay)
4 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[2][3].

Assay
Methods Test Index PMID
Western blot Cyclin E1 / Cyclin D1 ; p-AKT / AKT / p-GSKβ / GSKβ ; BTG2 / p-ERK / p-c-Raf / H4R3me2s 30461193 29441724

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 76 mg/mL
(199.74 mM)
Ethanol 76 mg/mL
(199.74 mM)
Water Insoluble

Chemical Information

Molecular Weight 380.48
Formula

C22H28N4O2

CAS No. 1616391-87-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(C1)NC2=NC=CC(=C2)C(=O)NCC(CN3CCC4=CC=CC=C4C3)O

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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