LLY-283

LLY-283 is an inhibitor of protein arginine methyltransferase 5 (PRMT5, IC50 = 22 nM). It is selective for PRMT5 over a panel of methyltransferases, including PRMT4, -6, and -7 at 1 µM. It reduces symmetric demethylation of SmBB' in MCF-7 cells (IC50 = 25 nM) and inhibits proliferation of various breast, gastric, hematological, lung, skin, and ovarian cancer cell lines (IC50s = 3-30 nM). LLY-283 (20 mg/kg) inhibits tumor growth in an A375 mouse xenograft model. It also disrupts alternative splicing events in, and inhibits proliferation and self-renewal of, patient-derived glioblastoma stem cells and increases survival in an orthotopic patient-derived xenograft (PDX) mouse model. See the Structural Genomics Consortium (SGC) website for more information.Formal Name: 7-[(5R)-5-C-phenyl-beta-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine. CAS Number: 2040291-27-6. Molecular Formula: C17H18N4O4. Formula Weight: 342.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 60 mg/ml, Ethanol: 60 mg/ml. lambdamax: 230, 274 nm. SMILES: O[C@H](C1=CC=CC=C1)[C@@]2([H])O[C@@H](N3C=CC4=C3N=CN=C4N)[C@H](O)[C@@H]2O. InChi Code: InChI=1S/C17H18N4O4/c18-15-10-6-7-21(16(10)20-8-19-15)17-13(24)12(23)14(25-17)11(22)9-4-2-1-3-5-9/h1-8,11-14,17,22-24H,(H2,18,19,20)/t11-,12+,13-,14-,17-/m1/s1. InChi Key: WWOOWAHTEXIWBO-QFRSUPTLSA-N.