WS-383

An inhibitor of the protein-protein interaction between DCNL1-UBC12 (IC50 = 11 nM in a cell-free assay), selectively inhibits neddylation of cullin-3 and -1 over other cullin proteins and increases levels of p21, p27, and Nrf2 in MGC803 cells at 10 µM, inhibits LSD1 activity in a cell-free assay (IC50 = 288 nM), inhibits growth and migration and induces G2M phase cell cycle arrest and apoptosis in MGC803 cells, decreases tumor size in an MGC803 mouse xenograft model at 25 or 50 mg/kg. SMILES: ClC1=CC=C(CSC2=NN3C(SC4=NN=NN4CCN(C)C)=CC(C)=NC3=N2)C=C1.Cl. InChi Code: InChI=1S/C18H20ClN9S2.ClH/c1-12-10-15(30-18-22-24-25-27(18)9-8-26(2)3)28-16(20-12)21-17(23-28)29-11-13-4-6-14(19)7-5-13,/h4-7,10H,8-9,11H2,1-3H3,1H. InChi Key: LJZUAAKUJAXXHQ-UHFFFAOYSA-N