GSK591

For research use only.

Catalog No.S8111 Synonyms: EPZ015866, GSK3203591

5 publications

GSK591 Chemical Structure

CAS No. 1616391-87-7

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

Selleck's GSK591 has been cited by 5 publications

1 Customer Review

  • Treatment of HCC cells with 500 nmol/L GSK591 for 4 days led to significant loss of PRMT5-catalyzed methylarginine on H4 (H4R3me2s), the upregulation of BTG2, and the phosphorylation of ERK. Inhibition of ERK phosphorylation by PD184352 treatment reversed these effects. H4R3me2s was used to detect the PRMT5 activity. Histone 3 was used as nuclear loading control.

    Cancer Med, 2018, 7(3):869-882. GSK591 purchased from Selleck.

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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 ; 

PubMed: 30461193     


A549 and H1299 cells were treated with PRMT5 inhibitor GSK591 (1 μmol/L) or vehicle and the cyclin E1 and cyclin D1 protein expression level was detected by Western blotting.

p-AKT / AKT / p-GSKβ / GSKβ ; 

PubMed: 30461193     


A549 and H1299 were treated with PRMT5 inhibitor GSK591 (1 μmol/L) or vehicle for 4 days and indicated proteins were detected by Western blotting. 

BTG2 / p-ERK / p-c-Raf / H4R3me2s ; 

PubMed: 29441724     


Treatment of HCC cells with 500 nmol/L GSK591 for 4 days led to significant loss of PRMT5‐catalyzed methylarginine on H4 (H4R3me2s), the upregulation of BTG2, and the phosphorylation of ERK. Inhibition of ERK phosphorylation by PD184352 treatment reversed these effects. H4R3me2s was used to detect the PRMT5 activity. Histone 3 was used as nuclear loading control

30461193 29441724

Protocol

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 380.48
Formula

C22H28N4O2

CAS No. 1616391-87-7
Storage powder
in solvent
Synonyms EPZ015866, GSK3203591
Smiles C1CC(C1)NC2=NC=CC(=C2)C(=O)NCC(CN3CCC4=CC=CC=C4C3)O

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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.

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Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID