VII-31

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 In Vitro VII-31 (100 nM, 200 nM; 48 hours) inhibits the cell viability of gastric cell line MGC803 with an IC 50 of 0.09±0.01 μM. VII-31 also inhibits the cell viability of MCF-7 and PC-3 with IC 50 s of 0.10±0.006 and 1.15±0.28μM , respectively. VII-31 (50-150 nM; 24 hours) arrests MGC803 cells cycle in G2/M phase. VII-31 (50-150 nM; 48 hours) induces apoptosis via intrinsic and extrinsic pathways. VII-31 (50-150 nM; 24 hours) activates NEDDylation in MGC803 cells. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Gastric cancer MGC803 cells Concentration: 100, 200 nM Incubation Time: 48 hours Result: Inhibited the cell viability in dose-depend manner. Cell Cycle AnalysisCell Line: MGC803 cells Concentration: 50, 100, 150 nM Incubation Time: 24 hours Result: Arrested cells in G2/M phase, and a clear sub-G1 peak was observed in the high dose group. Apoptosis AnalysisCell Line: MGC803 cells Concentration: 50, 75, 100, and 150 nM Incubation Time: 48 hours Result: High dose (150 nM) treatment significantly elevated the early and late apoptosis rate to 92.8% from 4.8%. Western Blot AnalysisCell Line: MGC803 cells Concentration: 50, 100, 150 nM Incubation Time: 24 hours Result: Resulted in NEDDylation activation of MGC803 cells, the NEDDylation of 3 important proteins NAE1, Ubc12 and CUL1 has been activated. In Vivo VII-31 inhibits the tumor progression in vivo, while showing no obvious toxicity to mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mice bearing MGC803 xenograft tumors Dosage: 50, 100, 150 mg/kg Administration: Subcutaneous injection; daily for 28 days Result: The mice had a much smaller tumor compared with vehicle control. The tumor volumes of middle/high dose treated mice at certain time points were evidently decreased comparing with untreated group. Form:Solid IC50& Target:NEDDylation

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