VII-31

Modify Date: 2024-09-25 07:20:53

VII-31 Structure
VII-31 structure
Common Name VII-31
CAS Number 2305757-96-2 Molecular Weight 427.51
Density N/A Boiling Point N/A
Molecular Formula C23H25NO5S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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[1].

 Names

Name VII-31

 VII-31 Biological Activity

Description 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].
Related Catalog
Target

NEDDylation[1]

In Vitro 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 Concentration: 100, 200 nM Incubation Time: 48 hours Result: Inhibited the cell viability in dose-depend manner. Cell Cycle Analysis[1] Cell 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 Analysis[1] Cell 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 Analysis[1] Cell 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[1]. Animal Model: Mice bearing MGC803 xenograft tumors[1] 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.
References

[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.

 Chemical & Physical Properties

Molecular Formula C23H25NO5S
Molecular Weight 427.51