标签归档：trxr

Ethaselen(Synonyms: BBSKE)

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。

Ethaselen (Synonyms: BBSKE) 纯度: ≥98.0%

Ethaselen (BBSKE) 是具有口服活性的，选择性的硫氧还蛋白还原酶 (TrxR) 抑制剂，对野生型人 TrxR1 和大鼠 TrxR1 的 IC50 分别为 0.5 和 0.35 μM。Ethaselen 特异性结合哺乳动物 TrxR1 C 端活性位点中独特的硒代半胱氨酸-半胱氨酸氧化还原对。Ethaselen 是一种有机硒化合物，一种有效的抗肿瘤候选药物，可通过靶向 TrxR 对非小细胞肺癌 (NSCLC) 发挥有效抑制作用。

Ethaselen(Synonyms: BBSKE)

Ethaselen Chemical Structure

CAS No. : 217798-39-5

规格 价格 是否有货 数量
5 mg ￥3000 In-stock
10 mg ￥4900 In-stock
25 mg ￥9800 In-stock
50 mg ￥15000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Ethaselen 相关产品

•相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Orally Active Compound Library
  • Anti-Lung Cancer Compound Library

生物活性

Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC50s of 0.5 and 0.35 μM for the wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair in the C-terminal active site of mammalian TrxR1. Ethaselen, an organoselenium compound, is a potent antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxR[1][2].

IC50 & Target

TrxR[1]
体外研究
(In Vitro)

Ethaselen (2.5-10 μM; 12, 24 hours) suppresses A549 cell viability in a both concentration- and time-dependent manner. H1666, which has considerably lower TrxR1 expression level, is less susceptible to 24 h treatment with Ethaselen[1].
Ethaselen inhibits the intracellular TrxR1 activity in a concentration- and time-dependent manner, with IC50 values of 4.2 and 2 μM for 12- and 24-h treatments, respectively[1].
Ethaselen (2.5-10 μM; 12, 24 hours) has no effect on the protein amounts of TrxR1 and Trx. The mRNA level of TrxR1 does not show significant alteration in Ethaselen-treated A549 cells[1].
Ethaselen (2.5-50 μM; 1-24 hours) causes intracellular Trx oxidation in A549 cells[1].
Ethaselen (5-10 μM; 12, 24 hours) causes a clear concentration-dependent increase in ROS levels in A549 cells[1].
The inhibition constants for Ethaselen binding to free enzyme (Ki) and the enzyme-substrate complex (Kis) were determined to be 0.022 and 0.087 μM, respectively. Ethaselen also inhibits mammalian TrxR1 in a time-dependent manner possibly by forming a covalent Se-S bond with Cys497 of Trx[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: A549 cell
Concentration: 2.5, 5, 7.5, 10 μM
Incubation Time: 12, 24 hours
Result: Suppressed A549 cell viability in a both concentration- and time-dependent manner.

体内研究
(In Vivo)

Ethaselen (BBSKE; 36-108 mg/kg/day; PO; for 10 days) shows increased inhibition of tumor growth in a dose-independent manner[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.

Animal Model: Five-week-old female BALB/c nude mice with A549 cell[2]
Dosage: 36, 72, 108 mg/kg
Administration: PO; daily; for 10 days
Result: Showed increased inhibition of tumor growth, and the inhibition levels increased with the dose.
The TrxR activity levels of the high dose group (108 mg/kg) decreased more than the middle dose group (72 mg/kg) and low dose group (36 mg/kg).

Clinical Trial

分子量

422.20

Formula

C16H12N2O2Se2
CAS 号

217798-39-5
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 : 12.5 mg/mL (29.61 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3685 mL 11.8427 mL 23.6855 mL
5 mM 0.4737 mL 2.3685 mL 4.7371 mL
10 mM 0.2369 mL 1.1843 mL 2.3685 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    90% corn oil

    Solubility: ≥ 1.25 mg/mL (2.96 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (2.96 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 12.5 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]. Lihui Wang, et al. Ethaselen: a potent mammalian thioredoxin reductase 1 inhibitor and novel organoselenium anticancer agent. Free Radic Biol Med. 2012 Mar 1;52(5):898-908.

    [2]. Suo-Fu Ye, et al. Dose-biomarker-response modeling of the anticancer effect of ethaselen in a human non-small cell lung cancer xenograft mouse model. Acta Pharmacol Sin. 2017 Feb;38(2):223-232.

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TrxR inhibitor D9

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。

TrxR inhibitor D9 

TrxR inhibitor D9 是一种有效和选择性的硫氧还蛋白还原酶 (TrxR) 的抑制剂，EC50 值为 2.8 nM。TrxR inhibitor D9 具有在体外和体内抑制肿瘤增殖的能力。

TrxR inhibitor D9

TrxR inhibitor D9 Chemical Structure

CAS No. : 1527513-89-8

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

TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo[1][2].

IC50 & Target

EC50: 2.8 nM (TrxR)[1]
体外研究
(In Vitro)

TrxR inhibitor D9 (0.1-1 μM; 72 h) inhibits the cell proliferation with IC50s of 0.03 and 0.1 μM for MCF-7 and HT-29 cells, respectively[1].
TrxR inhibitor D9 (72 h) completely inhibits all cancer cells (A549, KB, MDA MB-231, HeLa, MCF-7 and HT-29) viability at the concentration of 0.60 μM, and the IC50s of all cancer cells could be as low as 0.55 μM, and dose not significantly affects normal cells viability[1].
TrxR inhibitor D9 (0.8 μM; 4 and 8 h) induces HT-29 cells necrosis/apoptosis[1].
TrxR inhibitor D9 (2-20 nM; 1-60 s) inhibits TrxR activity in a concentration-dependent manner[1].
TrxR inhibitor D9 (1-1000 nM) does not significantly inhibits the catalytic activity of glutathione reductase (GR) even when the concentration increases to more than 1000 nM[1].
TrxR inhibitor D9 (0.4 μM) could effectively avoid the ligand exchange with albumin[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: MCF-7 and HT-29 cells
Concentration: 0.1, 0.5, 1 μM
Incubation Time: 72 hours
Result: Killed 70% MCF-7 cells and 50% HT-29 cells with the concentration as low as 0.1 μM.

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.8 μM
Incubation Time: 4 and 8 hours
Result: Led to more than 50% necrosis/apoptosis of cells compared to control after 4 h of treatment.
Induced all cells necrosis/apoptosis after 8 h of incubation.

体内研究
(In Vivo)

TrxR inhibitor D9 (5 mg/kg; i.v. once every 2 d for 15 d) effectively inhibits the growth of tumors in mice[1].

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

Animal Model: BALB/c nude mice (17-18 g) bearing a MCF-7 tumor[1]
Dosage: 5 mg/kg
Administration: I.v. once every 2 days for 15 days
Result: Inhibited tumor growth with IR (inhibition ratio) of 91.5% and was well tolerated.

分子量

596.43

Formula

C25H20AuOPS
CAS 号

1527513-89-8
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]. Zhang D, et, al. Synthesis and molecular recognition studies on small-molecule inhibitors for thioredoxin reductase. J Med Chem. 2014 Oct 9;57(19):8132-9.

    [2]. Lin YX, et, al. pH-Sensitive Polymeric Nanoparticles with Gold(I) Compound Payloads Synergistically Induce Cancer Cell Death through Modulation of Autophagy. Mol Pharm. 2015 Aug 3;12(8):2869-78.

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

TrxR inhibitor D9

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。

TrxR inhibitor D9 

TrxR inhibitor D9 是一种有效和选择性的硫氧还蛋白还原酶 (TrxR) 的抑制剂，EC50 值为 2.8 nM。TrxR inhibitor D9 具有在体外和体内抑制肿瘤增殖的能力。

TrxR inhibitor D9

TrxR inhibitor D9 Chemical Structure

CAS No. : 1527513-89-8

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

TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo[1][2].

IC50 & Target

EC50: 2.8 nM (TrxR)[1]
体外研究
(In Vitro)

TrxR inhibitor D9 (0.1-1 μM; 72 h) inhibits the cell proliferation with IC50s of 0.03 and 0.1 μM for MCF-7 and HT-29 cells, respectively[1].
TrxR inhibitor D9 (72 h) completely inhibits all cancer cells (A549, KB, MDA MB-231, HeLa, MCF-7 and HT-29) viability at the concentration of 0.60 μM, and the IC50s of all cancer cells could be as low as 0.55 μM, and dose not significantly affects normal cells viability[1].
TrxR inhibitor D9 (0.8 μM; 4 and 8 h) induces HT-29 cells necrosis/apoptosis[1].
TrxR inhibitor D9 (2-20 nM; 1-60 s) inhibits TrxR activity in a concentration-dependent manner[1].
TrxR inhibitor D9 (1-1000 nM) does not significantly inhibits the catalytic activity of glutathione reductase (GR) even when the concentration increases to more than 1000 nM[1].
TrxR inhibitor D9 (0.4 μM) could effectively avoid the ligand exchange with albumin[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: MCF-7 and HT-29 cells
Concentration: 0.1, 0.5, 1 μM
Incubation Time: 72 hours
Result: Killed 70% MCF-7 cells and 50% HT-29 cells with the concentration as low as 0.1 μM.

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.8 μM
Incubation Time: 4 and 8 hours
Result: Led to more than 50% necrosis/apoptosis of cells compared to control after 4 h of treatment.
Induced all cells necrosis/apoptosis after 8 h of incubation.

体内研究
(In Vivo)

TrxR inhibitor D9 (5 mg/kg; i.v. once every 2 d for 15 d) effectively inhibits the growth of tumors in mice[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: BALB/c nude mice (17-18 g) bearing a MCF-7 tumor[1]
Dosage: 5 mg/kg
Administration: I.v. once every 2 days for 15 days
Result: Inhibited tumor growth with IR (inhibition ratio) of 91.5% and was well tolerated.

分子量

596.43

Formula

C25H20AuOPS
CAS 号

1527513-89-8
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]. Zhang D, et, al. Synthesis and molecular recognition studies on small-molecule inhibitors for thioredoxin reductase. J Med Chem. 2014 Oct 9;57(19):8132-9.

    [2]. Lin YX, et, al. pH-Sensitive Polymeric Nanoparticles with Gold(I) Compound Payloads Synergistically Induce Cancer Cell Death through Modulation of Autophagy. Mol Pharm. 2015 Aug 3;12(8):2869-78.

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

TrxR inhibitor D9

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。

TrxR inhibitor D9 

TrxR inhibitor D9 是一种有效和选择性的硫氧还蛋白还原酶 (TrxR) 的抑制剂，EC50 值为 2.8 nM。TrxR inhibitor D9 具有在体外和体内抑制肿瘤增殖的能力。

TrxR inhibitor D9

TrxR inhibitor D9 Chemical Structure

CAS No. : 1527513-89-8

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

TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo[1][2].

IC50 & Target

EC50: 2.8 nM (TrxR)[1]
体外研究
(In Vitro)

TrxR inhibitor D9 (0.1-1 μM; 72 h) inhibits the cell proliferation with IC50s of 0.03 and 0.1 μM for MCF-7 and HT-29 cells, respectively[1].
TrxR inhibitor D9 (72 h) completely inhibits all cancer cells (A549, KB, MDA MB-231, HeLa, MCF-7 and HT-29) viability at the concentration of 0.60 μM, and the IC50s of all cancer cells could be as low as 0.55 μM, and dose not significantly affects normal cells viability[1].
TrxR inhibitor D9 (0.8 μM; 4 and 8 h) induces HT-29 cells necrosis/apoptosis[1].
TrxR inhibitor D9 (2-20 nM; 1-60 s) inhibits TrxR activity in a concentration-dependent manner[1].
TrxR inhibitor D9 (1-1000 nM) does not significantly inhibits the catalytic activity of glutathione reductase (GR) even when the concentration increases to more than 1000 nM[1].
TrxR inhibitor D9 (0.4 μM) could effectively avoid the ligand exchange with albumin[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: MCF-7 and HT-29 cells
Concentration: 0.1, 0.5, 1 μM
Incubation Time: 72 hours
Result: Killed 70% MCF-7 cells and 50% HT-29 cells with the concentration as low as 0.1 μM.

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.8 μM
Incubation Time: 4 and 8 hours
Result: Led to more than 50% necrosis/apoptosis of cells compared to control after 4 h of treatment.
Induced all cells necrosis/apoptosis after 8 h of incubation.

体内研究
(In Vivo)

TrxR inhibitor D9 (5 mg/kg; i.v. once every 2 d for 15 d) effectively inhibits the growth of tumors in mice[1].

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

Animal Model: BALB/c nude mice (17-18 g) bearing a MCF-7 tumor[1]
Dosage: 5 mg/kg
Administration: I.v. once every 2 days for 15 days
Result: Inhibited tumor growth with IR (inhibition ratio) of 91.5% and was well tolerated.

分子量

596.43

Formula

C25H20AuOPS
CAS 号

1527513-89-8
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]. Zhang D, et, al. Synthesis and molecular recognition studies on small-molecule inhibitors for thioredoxin reductase. J Med Chem. 2014 Oct 9;57(19):8132-9.

    [2]. Lin YX, et, al. pH-Sensitive Polymeric Nanoparticles with Gold(I) Compound Payloads Synergistically Induce Cancer Cell Death through Modulation of Autophagy. Mol Pharm. 2015 Aug 3;12(8):2869-78.

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

TrxR-IN-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。

TrxR-IN-2 

TrxR-IN-2 是一种潜在的硫氧还蛋白还原酶（TrxR）抑制剂，是一种治疗耐药性肝细胞癌的有希望的候选药物。

TrxR-IN-2

TrxR-IN-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

TrxR-IN-2, a potential thioredoxin reductase (TrxR) inhibitor, represents a promising candidate drug for the chemotherapy of drug-resistant hepatocellular carcinoma.

分子量

406.43

Formula

C22H22N4O4
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]. Qian J, et al. A Derivative of Piperlongumine and Ligustrazine as a Potential Thioredoxin Reductase Inhibitor in Drug-Resistant Hepatocellular Carcinoma. J Nat Prod. 2021 Nov 21.

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

TrxR-IN-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。

TrxR-IN-2 

TrxR-IN-2 是一种潜在的硫氧还蛋白还原酶（TrxR）抑制剂，是一种治疗耐药性肝细胞癌的有希望的候选药物。

TrxR-IN-2

TrxR-IN-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

TrxR-IN-2, a potential thioredoxin reductase (TrxR) inhibitor, represents a promising candidate drug for the chemotherapy of drug-resistant hepatocellular carcinoma.

分子量

406.43

Formula

C22H22N4O4
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]. Qian J, et al. A Derivative of Piperlongumine and Ligustrazine as a Potential Thioredoxin Reductase Inhibitor in Drug-Resistant Hepatocellular Carcinoma. J Nat Prod. 2021 Nov 21.

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

TrxR-IN-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。

TrxR-IN-2 

TrxR-IN-2 是一种潜在的硫氧还蛋白还原酶（TrxR）抑制剂，是一种治疗耐药性肝细胞癌的有希望的候选药物。

TrxR-IN-2

TrxR-IN-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

TrxR-IN-2, a potential thioredoxin reductase (TrxR) inhibitor, represents a promising candidate drug for the chemotherapy of drug-resistant hepatocellular carcinoma.

分子量

406.43

Formula

C22H22N4O4
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]. Qian J, et al. A Derivative of Piperlongumine and Ligustrazine as a Potential Thioredoxin Reductase Inhibitor in Drug-Resistant Hepatocellular Carcinoma. J Nat Prod. 2021 Nov 21.

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

TrxR-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。

TrxR-IN-4 

TrxR-IN-4 (Compound 1b) 是一种有效的 TrxR 抑制剂。TrxR-IN-4 通过激活内质网应激 (ERS) 诱导 HepG2 细胞凋亡。TrxR-IN-4 通过下调 TrxR 表达和炎症水平改善体内 CCl4 诱导的肝损伤。

TrxR-IN-4

TrxR-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

TrxR-IN-4 (Compound 1b) is a potent inhibitor of TrxR. TrxR-IN-4 induces HepG2 cells apoptosis by activating the endoplasmic reticulum stress (ERS). TrxR-IN-4 improves the CCl4-induced liver damage in vivo by down-regulation of TrxR expression and inflammation level[1].

分子量

651.43

Formula

C28H20AuF2N2O2
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]. Bian M, et al. Synthesis and biological evaluation of gold(III) Schiff base complexes for the treatment of hepatocellular carcinoma through attenuating TrxR activity. Eur J Med Chem. 2020 May 1;193:112234.

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TrxR-IN-3

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。

TrxR-IN-3 

TrxR-IN-3 (Compound 2c) 是一种有效的 TrxR 抑制剂。TrxR-IN-3 对五种人类癌细胞系表现出有效的抗增殖活性，尤其是对乳腺肿瘤细胞。TrxR-IN-3 通过调节乳腺癌细胞中表达的凋亡相关蛋白增加 ROS 水平并导致显着的细胞凋亡。TrxR-IN-3 还通过促进 LC3-II 和 Beclin-1 的表达，降低 LC3-I 和 p62 蛋白的表达，触发自噬体和自溶酶体的形成。

TrxR-IN-3

TrxR-IN-3 Chemical Structure

CAS No. : 2445565-58-0

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生物活性

TrxR-IN-3 (Compound 2c) is a potent inhibitor of TrxR. TrxR-IN-3 exhibits potent antiproliferative activities against five human cancer cell lines, especially against breast tumor cells. TrxR-IN-3 increases ROS levels and resulted in marked apoptosis by regulating apoptosis-related proteins expressed in the breast cancer cells. TrxR-IN-3 also triggers the formation of autophagosomes and autolysosomes by promoting the expression of LC3-II and Beclin-1 and diminishing the expression of LC3-I and p62 proteins[1].

分子量

268.23

Formula

C14H11F3O2
CAS 号

2445565-58-0
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]. Qian J, et al. Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy. Eur J Med Chem. 2020 Oct 15;204:112610.

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