GSK-591

GSK-591

【产品别名】GSK591, GSK-591, GSK 591, EPZ 015866, EPZ-015866, GSK 3203591, GSK-3203591, GSK3203591

【CAS号】 1616391-87-7

【目录编号】

【纯度】 98%

【分子式】 C22H28N4O2

【分子量】 380.22

【简介】 EPZ015866 (GSK591) is a potent selective inhibitor of the arginine methyltransferase PRMT5.

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GSK-591 详细介绍

EPZ015866 (GSK591) is a potent selective inhibitor of the arginine methyltransferase PRMT5. It maintained excellent selectivity against other PMT enzymes observed with EPZ015666 [1].
IC50:61 nM-904 nM in Maver-1 cells [2]
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. [2]
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). [2]
 


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