Catalog No.S8111 Synonyms: EPZ015866, GSK3203591
Molecular Weight(MW): 380.48
GSK591 (EPZ015866,GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM.
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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Choose Selective Histone Methyltransferase Inhibitors
|Description||GSK591 (EPZ015866,GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM.|
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.
|In vitro||DMSO||76 mg/mL (199.74 mM)|
|Ethanol||76 mg/mL (199.74 mM)|
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