VII-31 is a potent NEDDylation pathway activator to inhibit the tumor progression in vitro and in vivo. VII-31 induces apoptosis via intrinsic and extrinsic pathways[1].
VII-31 (100 nM, 200 nM; 48 hours) inhibits the cell viability of gastric cell line MGC803 with an IC50 of 0.09±0.01 μM. VII-31 also inhibits the cell viability of MCF-7 and PC-3 with IC50s of 0.10±0.006 and 1.15±0.28μM , respectively[1].VII-31 (50-150 nM; 24 hours) arrests MGC803 cells cycle in G2/M phase[1].VII-31 (50-150 nM; 48 hours) induces apoptosis via intrinsic and extrinsic pathways[1].VII-31 (50-150 nM; 24 hours) activates NEDDylation in MGC803 cells[1].VII-31 (50-150 nM; 48 hours) up-regulates pro-apoptotic proteins FADD, Fasl, PIDD, Bax, Bad; while down-regulates anti-apoptotic proteins Bcl-xL, Bcl-2, XIAP, c-IAP1[1]. Cell Viability Assay[1] Cell Line: Gastric cancer MGC803 cells
VII-31 inhibits the tumor progression in vivo, while showing no obvious toxicity to mice[1]. Animal Model: Mice bearing MGC803 xenograft tumors[1]
[1]. Dong-Jun Fu, et al. Discovery of Novel Tertiary Amide Derivatives as NEDDylation Pathway Activators to Inhibit the Tumor Progression in Vitro and in Vivo. Eur J Med Chem. 2020 Apr 15;192:112153.