标签归档：nrf

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

Nrf2 activator-2

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。

Nrf2 activator-2 

Nrf2 activator-2 (compound O15) 是一种蛇床子素衍生物，一种有效的 Nrf2 激动剂，在 293 T 细胞中的 EC50 为 2.9 μM。Nrf2 activator-2有效抑制 Keap1 和 Nrf2 的相互作用，从而显示出对 Nrf2 的激活作用。Nrf2 activator-2 显示细胞中泛素化 Nrf2 水平显着降低。

Nrf2 activator-2

Nrf2 activator-2 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

Nrf2 activator-2 (compound O15), a Osthole derivative, is a potent Nrf2 agonist with an EC50 of 2.9 μM in 293 T cells. Nrf2 activator-2 effectively inhibits the interaction between Keap1 and Nrf2, thus showing the activation effect on Nrf2. Nrf2 activator-2 shows a marked decrease in the level of ubiquitinated Nrf2 in cells[1].

分子量

385.25

Formula

C20H17BrO3
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]. Weiwei Huang, et al. Design and synthesis of Osthole-based compounds as potential Nrf2 agonists. Bioorg Med Chem Lett. 2022 Apr 1;61:128547.

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

Nrf2 activator-2

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。

Nrf2 activator-2 

Nrf2 activator-2 (compound O15) 是一种蛇床子素衍生物，一种有效的 Nrf2 激动剂，在 293 T 细胞中的 EC50 为 2.9 μM。Nrf2 activator-2有效抑制 Keap1 和 Nrf2 的相互作用，从而显示出对 Nrf2 的激活作用。Nrf2 activator-2 显示细胞中泛素化 Nrf2 水平显着降低。

Nrf2 activator-2

Nrf2 activator-2 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

Nrf2 activator-2 (compound O15), a Osthole derivative, is a potent Nrf2 agonist with an EC50 of 2.9 μM in 293 T cells. Nrf2 activator-2 effectively inhibits the interaction between Keap1 and Nrf2, thus showing the activation effect on Nrf2. Nrf2 activator-2 shows a marked decrease in the level of ubiquitinated Nrf2 in cells[1].

分子量

385.25

Formula

C20H17BrO3
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]. Weiwei Huang, et al. Design and synthesis of Osthole-based compounds as potential Nrf2 agonists. Bioorg Med Chem Lett. 2022 Apr 1;61:128547.

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

Nrf2 activator-2

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。

Nrf2 activator-2 

Nrf2 activator-2 (compound O15) 是一种蛇床子素衍生物，一种有效的 Nrf2 激动剂，在 293 T 细胞中的 EC50 为 2.9 μM。Nrf2 activator-2有效抑制 Keap1 和 Nrf2 的相互作用，从而显示出对 Nrf2 的激活作用。Nrf2 activator-2 显示细胞中泛素化 Nrf2 水平显着降低。

Nrf2 activator-2

Nrf2 activator-2 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

Nrf2 activator-2 (compound O15), a Osthole derivative, is a potent Nrf2 agonist with an EC50 of 2.9 μM in 293 T cells. Nrf2 activator-2 effectively inhibits the interaction between Keap1 and Nrf2, thus showing the activation effect on Nrf2. Nrf2 activator-2 shows a marked decrease in the level of ubiquitinated Nrf2 in cells[1].

分子量

385.25

Formula

C20H17BrO3
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]. Weiwei Huang, et al. Design and synthesis of Osthole-based compounds as potential Nrf2 agonists. Bioorg Med Chem Lett. 2022 Apr 1;61:128547.

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

Nrf2-IN-1

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。

Nrf2-IN-1  纯度: 99.89%

Nrf2-IN-1 是 Nrf2 的抑制剂，被用于急性髓性白血病 (AML) 药物研究。

Nrf2-IN-1

Nrf2-IN-1 Chemical Structure

CAS No. : 1610022-76-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3850 In-stock
5 mg ￥3500 In-stock
10 mg ￥5500 In-stock
50 mg ￥16500 In-stock
100 mg ￥26500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Nrf2-IN-1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • NF-κB Signaling Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Oxygen Sensing Compound Library
  • Ferroptosis Compound Library
  • Anti-Blood Cancer Compound Library
  • Transcription Factor Targeted Library
  • Targeted Diversity Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Nrf2-IN-1 is an inhibitor of nuclear factor-erythroid 2-related factor 2 (Nrf2). Nrf2-IN-1 is developed for the research of acute myeloid leukemia (AML)[1].

IC50 & Target

Nrf2[1]
体外研究
(In Vitro)

Nrf2-IN-1 (Compound 4f) (10 μM) inhibits Nrf2 activation[1].
Nrf2-IN-1(1-20 μM; 48 hours) inhibits growth of the three AML cell[1].
Nrf2-IN-1 (5-10 μM; 48 hours) induces apoptosis of three AML cells in vitro[1].
Nrf2-IN-1 induces apoptotic signaling involving Bcl-2 and Bax[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 Viability Assay[1]

Cell Line: THP-1 cells, HL-60 cells, U937 cells
Concentration: 1 μM, 5 μM, 10 μM, 20 μM
Incubation Time: 48 hours
Result: Inhibited growth of the three AML cell types at 5 μM, 10 μM or 20 μM for 48 hours.

Apoptosis Analysis[1]

Cell Line: THP-1 cells, HL-60 cells, U937 cells
Concentration: 5 μM, 10 μM
Incubation Time: 48 hours
Result: Induced apoptosis in AML cells in vitro.

Western Blot Analysis[1]

Cell Line: THP-1 cells, HL-60 cells, U937 cells
Concentration: 5 μM, 10 μM
Incubation Time: 48 hours
Result: Triggered caspase-dependent apoptotic signaling in AML cells.

体内研究
(In Vivo)

Nrf2-IN-1 inhibits tumor growth via apoptosis in chicken eggs[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.
分子量

383.87

Formula

C21H22ClN3O2
CAS 号

1610022-76-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 260 mg/mL (677.31 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6050 mL 13.0252 mL 26.0505 mL
5 mM 0.5210 mL 2.6050 mL 5.2101 mL
10 mM 0.2605 mL 1.3025 mL 2.6050 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (5.65 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (5.65 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.17 mg/mL (5.65 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (5.65 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (5.65 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (5.65 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Zhang J, et al. Discovery of a novel Nrf2 inhibitor that induces apoptosis of human acute myeloid leukemia cells. Oncotarget. 2017 Jan 31;8(5):7625-7636.

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

NK-252

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。

NK-252  纯度: 99.93%

NK-252 是一种潜在的 Nrf2 激活剂，具有很好的 Nrf2 活化能力。

NK-252

NK-252 Chemical Structure

CAS No. : 1414963-82-8

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥726 In-stock
5 mg ￥660 In-stock
10 mg ￥1100 In-stock
25 mg ￥2300 In-stock
50 mg ￥4000 In-stock
100 mg ￥6900 In-stock
200 mg   询价  
500 mg   询价  

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NK-252 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • NF-κB Signaling Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Oxygen Sensing Compound Library
  • Ferroptosis Compound Library
  • Transcription Factor Targeted Library

生物活性

NK-252 is a potential Nrf2 activator, which exhibits a great Nrf2-activating potential.

IC50 & Target

Nrf2[1]
体外研究
(In Vitro)

The luciferase activity in Huh-7.5 cells treated with Oltipraz (OPZ) or NK-252 shows activation of the NAD(P)H quinone oxidoreductase 1 (NQO1)-ARE in a dose-dependent manner. NK-252 displays this effect with higher potency than OPZ based on the fact that the EC2 value (concentration for a 2-fold induction above background), calculated with linear extrapolation from the values above and below the induction threshold, is 20.8 μM for OPZ and 1.36 μM for NK-252. NK-252 has potential as an Nrf2 activator in hepatic cells. Prototypical Nrf2 activators that include OPZ have been reported to protect microglial cells from H2O2-induced cytotoxicity. The protective effects of OPZ and NK-252 are examined against H2O2-induced cytotoxicity using Huh-7 cells to evaluate their antioxidant properties. The cells treated with OPZ or NK-252 show increased resistance to H2O2-induced cytotoxicity compared with control cells[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.
体内研究
(In Vivo)

Rats on a choline-deficient L-amino acid–defined (CDAA) diet given OPZ or NK-252 display decreased fibrosis scores compared with CDAA control rats, with median scores of 3, corresponding to bridging fibrosis. CDAA control rats display approximately 20-fold augmentation of the liver fibrosis area compared with rats fed a normal control diet (naive) (14.7 and 0.72%, respectively).This augmentation is also drastically reduced by administration of OPZ or NK-252 (5.80% for OPZ, 6.20% for NK-252_low, and 4.97% for NK-252_high). The effects of NK-252 on both fibrosis score and fibrosis area are dose-dependent[1]. NK-252 alone has no antitumour effect in P388/S- and P388/VCR-mice. The combination therapy of Etoposide with NK-252 administered p.o. significantly increases the life-span of mice inoculated i.p. with P388/S compared with the corresponding therapeutic effects with Etoposide alone. The combination therapy with Etoposide and NK-252 significantly increases the life-span of mice inoculated i.p. with P388/VCR compared with the corresponding survival time with Etoposide alone[2].

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.
分子量

285.26

Formula

C13H11N5O3
CAS 号

1414963-82-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 29 mg/mL (101.66 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5056 mL 17.5279 mL 35.0557 mL
5 mM 0.7011 mL 3.5056 mL 7.0111 mL
10 mM 0.3506 mL 1.7528 mL 3.5056 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.29 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.29 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.29 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Shimozono R et al. Nrf2 activators attenuate the progression of nonalcoholic steatohepatitis-related fibrosis in a dietary rat model. Mol Pharmacol. 2013 Jul, 84(1):62-70.

    [2]. Kiue A, et al. Enhancement of antitumour activity of etoposide by dihydropyridines on drug-sensitive and drug-resistant leukaemia in mice. Br J Cancer. 1991 Aug;64(2):221-6.
Cell Assay
[1]

The Huh-7.5 cells, a subline derived from Huh-7 cells, are transfected with ARE/pGL4.32 by lipofectamine LTX. The stable clonal transfectant is isolated by selection in hygromycin B (0.1 mg/mL). Cells derived from stable clones are transfected with control or Nrf2 small interfering RNA by lipofectamine RNAiMAX (30 hours), then treated with OPZ, NK-252 (0.1-30 μM, 16 hours) , or DMSO alone (control). The luciferase activity values are measured using the Steady-Glo Luciferase Assay System[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 Administration
[1][2]

Rats[1]
Six-week-old male Fischer 344 rats are randomly divided into four compound administration groups and four control groups. Compound administration groups of rats fed a CDAA diet receive oral administration as follows: 1) OPZ from 1 week after feeding at a dose of 60 mg/kg once daily for 9 weeks (CDAA+OPZ group; N=8), 2) NK-252 from 1 week after feeding at a dose of 20 mg/kg once daily for 9 weeks (CDAA+NK-252_low group; N=8), 3) NK-252 from 1 week after feeding at a dose of 60 mg/kg once daily for 9 weeks (CDAA+NK-252_high group; N=8), or 4) NK-252 from 6 weeks after feeding at a dose of 60 mg/kg once daily for 4 weeks (CDAA+NK-252_delayed administration: DA group; N=7). Two control groups of rats are fed a CDAA diet for 6 or 10 weeks (pre-CDAA control or CDAA control group; N=9 each), and the other two control groups of rats are fed standard rodent chow (CRF-1) for 6 or 10 weeks (prenaive or naive; N=3 each). Laparotomy and blood sampling are performed under isoflurane anesthesia. After blood sampling, rats are euthanized by exsanguination under isoflurane anesthesia, and the livers are immediately extirpated. [2]Mice[2]
Six- to 8-week-old male BALB/c x DBA/2 F1 (hereafter called CD2F1) mice weighing 22 to 26 g are used. Male CD2F1 mice are inoculated i.p. with 106 cells of P388/S and P388/VCR cell line on day 0. Each group consist of six mice. NK-250 and NK-252 (100, 300, and 1000 mg/kg) are given p.o. daily from day 1 to 5. Mean survival days and the range of survival days are analysed.

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.
参考文献

  • [1]. Shimozono R et al. Nrf2 activators attenuate the progression of nonalcoholic steatohepatitis-related fibrosis in a dietary rat model. Mol Pharmacol. 2013 Jul, 84(1):62-70.

    [2]. Kiue A, et al. Enhancement of antitumour activity of etoposide by dihydropyridines on drug-sensitive and drug-resistant leukaemia in mice. Br J Cancer. 1991 Aug;64(2):221-6.

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ML334(Synonyms: LH601A)

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。

ML334 (Synonyms: LH601A) 纯度: 99.82%

ML334 (LH601A) 是一种有效的，细胞可渗透的 NRF2 激活剂，通过抑制 Keap1-NRF2 蛋白质相互作用来发挥作用。ML334 以 Kd 值为 1μM 来结合 Keap1 Kelch 域。ML334 刺激 NRF2 表达和核易位并诱导抗氧化反应元件 (ARE) 活性。

ML334(Synonyms: LH601A)

ML334 Chemical Structure

CAS No. : 1432500-66-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5450 In-stock
1 mg ￥1850 In-stock
5 mg ￥5550 In-stock
10 mg ￥9500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

ML334 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • NF-κB Signaling Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Oxygen Sensing Compound Library
  • Ferroptosis Compound Library
  • Transcription Factor Targeted Library

生物活性

ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity[1][2].

IC50 & Target

Ki: 1 μM (Keap1)[2]
体外研究
(In Vitro)

ML334 (LH601A; 50-100 µM; 6-16 hours; HEK293 cells) treatment increases NQO1 and TRX1 mRNAs between 2- and 3-fold at both 6 and 16 h. And also enhances HO-1 mRNA expression between 4- and 7-fold at 6 h, with lesser fold-changes at 16 h[1].
ML334 (LH601A; 50-100 µM; 16 hours; HEK293 cells) treatment induces HO-1 and TRX1 proteins in HEK293 cells[1].
ML334 (LH601A) stimulates NRF2 expression and nuclear translocation in HEK293 cells[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.

RT-PCR[1]

Cell Line: HEK293 cells
Concentration: 50 μM or 100 µM
Incubation Time: 6 hours, 16 hours
Result: Increased NQO1 and TRX1 mRNAs between 2- and 3-fold at both 6 and 16 h. Enhanced HO-1 mRNA expression between 4- and 7-fold at 6 h.

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 50 μM or 100 µM
Incubation Time: 16 hours
Result: Enhanced HO-1 and TRX1 protein expression at 16 h.

分子量

446.50

Formula

C26H26N2O5
CAS 号

1432500-66-7
运输条件

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

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : 44.65 mg/mL (100.00 mM; Need ultrasonic)

Ethanol : 44.65 mg/mL (100.00 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2396 mL 11.1982 mL 22.3964 mL
5 mM 0.4479 mL 2.2396 mL 4.4793 mL
10 mM 0.2240 mL 1.1198 mL 2.2396 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Wen X, et al. Activation of NRF2 Signaling in HEK293 Cells by a First-in-Class Direct KEAP1-NRF2 Inhibitor. J Biochem Mol Toxicol. 2015 Jun;29(6):261-6.

    [2]. Hu L, et al. Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction. Bioorg Med Chem Lett. 2013 May 15;23(10):3039-43.

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Artemisitene(Synonyms: 青蒿烯)

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。

Artemisitene (Synonyms: 青蒿烯)

Artemisitene 是 Artemisinin 的天然衍生物，是一种 Nrf2 激活剂，具有抗氧化和抗癌活性。Artemisitene 通过降低 Nrf2 泛素化并增加其稳定性来激活 Nrf2。

Artemisitene(Synonyms: 青蒿烯) Artemisitene(Synonyms: 青蒿烯)

Artemisitene Chemical Structure

CAS No. : 101020-89-7

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

Artemisitene, a natural derivative of Artemisinin, is a Nrf2 activator with antioxidant and anticancer activities. Artemisitene activates Nrf2 by decreasing Nrf2 ubiquitination and increasing its stability[1][2].

体外研究
(In Vitro)

Artemisitene selectively induces DNA double-stranded breaks (DSBs) and apoptosis in various human cancer cells by suppressing the expression of topoisomerases in human cancer cells. Artemisitene selectively destabilizes c-Myc in human cancer cells by promoting the ubiquitination of c-Myc through the specific induction of the c-Myc E3 ligase NEDD4[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

In Nrf2 wild-type mice, systemic administration of Artemisitene (5-10 mg/kg; i.p.) strongly inhibits bleomycin-induced lung damage[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

280.32

Formula

C15H20O5
CAS 号

101020-89-7
中文名称

青蒿烯
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]. Weimin Chen, et al. Artemisitene activates the Nrf2-dependent antioxidant response and protects against bleomycin-induced lung injury. FASEB J. 2016 Jul;30(7):2500-10.

    [2]. Jian Chen, et al. Artemisitene suppresses tumorigenesis by inducing DNA damage through deregulating c-Myc-topoisomerase pathway. Oncogene. 2018 Sep;37(37):5079-5087.

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