Keap1-Nrf2-IN-4

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Keap1-Nrf2-IN-4 

Keap1-Nrf2-IN-4 是一种有效的 neddylation 抑制剂。Keap1-Nrf2-IN-4 对 MGC-803 细胞表现出较强的抗增殖活性 (IC50=2.55 µM)。Keap1-Nrf2-IN-4 阻断胃癌细胞的迁移能力并诱导细胞凋亡 apoptosis。Keap1-Nrf2-IN-4 抑制肿瘤生长且无明显毒性。

Keap1-Nrf2-IN-4

Keap1-Nrf2-IN-4 Chemical Structure

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生物活性

Keap1-Nrf2-IN-4 is a potent neddylation inhibitor. Keap1-Nrf2-IN-4 exhibits potent anti-proliferation activity against MGC-803 cells (IC50=2.55 µM). Keap1-Nrf2-IN-4 blocks the migration ability and induces apoptosis of gastric cancer cells. Keap1-Nrf2-IN-4 inhibits tumor growth without obvious toxicity[1].

体外研究
(In Vitro)

Keap1-Nrf2-IN-4 (compound 4g) (72 h) shows anti-proliferation activity (IC50 s of 2.55, 3.88, 3.74, 2.89 µM in MGC-803, MCF-7, A549, HepG-2 cells, respectively)[1].
Keap1-Nrf2-IN-4 inhibits neddylation of cullin1, cullin3, cullin5[1].
Keap1-Nrf2-IN-4 blocks the migration ability of MGC-803 without cell cycle arrest[1].
Keap1-Nrf2-IN-4 (24, 48 h) induces apoptosis of MGC-803 and HGC-27 cells in concentration- and time-dependent manners[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: MGC-803, MCF-7, A549, HepG-2 cells
Concentration:
Incubation Time: 72 h
Result: Showed anti-proliferation activity (IC50 of 2.55, 3.88, 3.74, 2.89 µM in MGC-803, MCF-7, A549, HepG-2 cells, respectively).

Apoptosis Analysis[1]

Cell Line: MGC-803, HGC-27 cells
Concentration: 2.5, 5, 7.5 µM for MGC-803 cells; 3, 6, 9 µM for HGC-27 cells
Incubation Time: 24 h, 48 h
Result: Induced apoptosis of MGC-803 and HGC-27 cells in concentration- and time-dependent manners.

体内研究
(In Vivo)

Keap1-Nrf2-IN-4 (50, 100 mg/kg; i.g.; per day for 21 days) exhibits antitumor activity on xenograft model without obvious side effect[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 5-6 weeks, 18-20 g, NOD SCID mice (xenograft tumor model)[1]
Dosage: 50, 100 mg/kg
Administration: i.g.; per day, 21 days
Result: Exihibited good antitumor activity on xenograft model without obvious side effect.

分子量

390.56

Formula

C26H34N2O
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Wang B, et al. Discovery of a cinnamyl piperidine derivative as new neddylation inhibitor for gastric cancer treatment. Eur J Med Chem. 2021; 226:113896.

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