GSK591

Catalog No.S8111 Synonyms: EPZ015866, GSK3203591

GSK591 Chemical Structure

Molecular Weight(MW): 380.48

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

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Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description GSK591 (EPZ015866,GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 11 nM.
Targets
PRMT5 [2]
(Cell-free assay)
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].

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
Synonyms EPZ015866, GSK3203591

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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

Tel: +1-832-582-8158 Ext:3

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Related Antibodies

Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID