标签归档：keap

Keap1-Nrf2-IN-4

发表于由

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

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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].

Shanghai Jinpan Biotech Co Ltd 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].

Shanghai Jinpan Biotech Co Ltd 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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Keap1-Nrf2-IN-4

发表于由

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

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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].

Shanghai Jinpan Biotech Co Ltd 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].

Shanghai Jinpan Biotech Co Ltd 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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Keap1-Nrf2-IN-4

发表于由

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

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

K67

发表于由

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。

K67 

K67 特异性抑制 Keap1 和 S349磷酸化 p62 之间的相互作用。K67 抑制 p-p62 与 Keap1 的竞争性结合，通过恢复 Keap1 驱动的 Nrf2 泛素化降解，有效抑制高表达S351磷酸化 p62 的 HCC 细胞的增殖。

K67

K67 Chemical Structure

CAS No. : 2046250-48-8

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

K67 specifically inhibits the interaction between Keap1 and S349-phosphorylated p62. K67 prevents p-p62 from blocking the binding of Keap1 and Nrf2. K67 effectively inhibits the proliferation of HCC cultures with high cellular S351-phosphorylated p62 by restoring the ubiquitination and degradation of Nrf2 driven by Keap1[1].

分子量

582.69

Formula

C29H30N2O7S2
CAS 号

2046250-48-8
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]. Saito T, et al. p62/Sqstm1 promotes malignancy of HCV-positive hepatocellular carcinoma through Nrf2-dependent metabolic reprogramming. Nat Commun. 2016 Jun 27;7:12030.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务