VII-31 是 NEDDylation 通路激活剂，可在体内外抑制肿瘤 。VII-31 还诱导凋亡 (apoptosis)。

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.

Solid

NEDDylation

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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.

VII-31 inhibits the tumor progression in vivo, while showing no obvious toxicity to mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mice bearing MGC803 xenograft tumors

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[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.

In Vitro: DMSO : 250 mg/mL (584.78 mM; Need ultrasonic)配制储备液