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Business Type:Lab/Research institutions
EPZ015866 (GSK591) is a potent selective inhibitor of the arginine methyltransferase PRMT5. It maintained excellent selectivity against other PMT enzymes observed with EPZ015666. IC50:61 nM-904 nM in Maver-1 cells. target: PRMT5 in vitro: A375 cells treated for 18 h with 1 μM EPZ015666 showed stabilization of PRMT5 in cellular thermal shift analysis in whole-cell lysates. In vivo: EPZ015666 or vehicle (0.5% methylcellulose in water) was administered orally BID at a dose volume of 10 mL/kg for 21 d (Granta-519 was dosed for 18 d).