2016年5月23日星期一

EPZ015866,EPZ-015866(GSK591)|PRMT5 inhibitor

EPZ015866,EPZ-015866(GSK591)|PRMT5 inhibitor

EPZ015866(GSK591) is a potent, selective PRMT5 inhibitor.

Product Name: EPZ015866(GSK591)|Cat No. DC9267|cas: 1616391-87-7|Other names: EPZ-015866,EPZ 015866,GSK-591,GSK 591,GSK3203591,GSK-3203591,GSK 3203591| Molecule formular: C22H28N4O2Molecule Weight: 380.22

In an in vitro biochemical assay, EPZ015866(GSK591) potently inhibits the PRMT5/MEP50 complex from methylating (histone) H4 with IC50 = 11 nM. In Z-138 cells, EPZ015866(GSK591) inhibits the symmetric arginine methylation of SmD3 with EC50 = 56 nM. Further, EPZ015866(GSK591) is selective for PRMT5 (up to 50 micromolar) relative to a panel of methyltransferases.


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