LLY-283 (C09-0935-944)

InformationLLY-283 LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) . LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. LLY-283 shows antitumor activity.TargetsPRMT5 (Cell-free assay); PRMT5 (Cell-based assay) 22 nM; 25 nMIn vitroLLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 ± 3 and 25 ± 1 nM, respectively. LLY-283 directly binds to and occupies the SAM pocket. LLY-283 is a low nanomolar enzymatic inhibitor of the PRMT5:MEP50 complex in biochemical assays and is selective for PRMT5 over other methyltransferases including related family members.In vivoLLY-283 shows antitumor activity in mouse xenografts when dosed orally and can serves as an excellent probe molecule for understanding the biological function of PRMT5 in normal and cancer cells. LLY-283 can be used as an in vivo tool compound to evaluate the pharmacology of PRMT5 inhibition.Cell Research(from reference)Cell lines：Sf9 cells, A375 tumor cells, MCF7 cells Concentrations：1 µM, 10 µM Incubation Time：48 h. Specification: 0.98 Molecular Formula: C17H18N4O4 Molecular Weight: 342.35 PubChem CID: 122669401 Isomeric SMILES: C1=CC=C(C=C1)[C@H]([C@@H]2[C@H]([C@H]([C@@H](O2)N3C=CC4=C(N=CN=C43)N)O)O)O