LLY-283 (LLY283) is a potent, selective inhibitor of arginine methyltransferase 5 (PRMT5) with IC50 of 22 nM.
LLY-283 displays excellent against other arginine methyltransferases including the closely related PRMT7 and the type II PRMTs such as PRMT4 and 6.
LLY-283 decreases SmBB’-Rme2s levels in MCF7 cells with IC50 of 25 nM, also inhibits the PRMT5 mediated regulation of the splicing of MDM4.
LLY-283 inhibits proliferation of A375 cells with IC50 of 45.6 nM.
LLY-283 inhibits Tumor growth in mouse xenograft (A375, 20 mg/kg; QD).
