Nrf2

抑制剂选择性比较

Nrf2产品

所有产品 Nrf2抑制剂(2) Nrf2激活剂(11)

目录号	产品描述	文献引用	实验数据
S7956^New	Brustaol Brustaol，可分离自B. javanica果实，是一种NRF2抑制剂。
S8790	ML385 ML385是一种新型的、特异的NRF2抑制剂，IC50为1.9 μM。它能抑制NRF2的下游靶基因的表达。NRF2 可调节多种铁死亡和脂质过氧化相关蛋白的活性。	Front Immunol, 2020, 10:2969 Oxid Med Cell Longev, 2020, 12;2020:1898213 Med Sci Monit, 2020, 26;26:e923251
S1848	Curcumin Curcumin 是流行的印度香料姜黄的主要姜黄色素，属于姜科（Zingiberaceae）。它是p300 histone acetylatransferase（IC50~25 μM）和Histone deacetylase的抑制剂，能够激活Nrf2 pathway并抑制NF-κB的激活。	Front Microbiol, 2020, 15;10:3016 Protein Sci, 2020, 29(6):1366-1372 Pharm Biol, 2020, 58(1):25-34
S2586	Dimethyl Fumarate Dimethyl Fumarate 是一种很有前途的新型口服治疗选择，治疗复发-缓解型多发性硬化症患者，降低疾病恶化。	PLoS Pathog, 2020, 16;16(3):e1008341 Am J Cancer Res, 2020, 1;10(5):1442-1454 Cancer Biol Ther, 2014, 15(12):1646-57	DMF enhances proteasome inhibitor toxicity in tumor cells. (A) GBM5/6/12/14 cells were treated with DMF (5 μM), velcade (10 nM) or the drug combination. Cells were isolated 24 h after treatment and viability determined by trypan blue exclusion assay (n = 3, +/− SEM) *P < 0.05 greater than DMF alone.
S7864	Oltipraz Oltipraz 是一种有效的 Nrf2 激活剂，也是一种有效的II期解毒酶诱导剂，显著作用于谷胱甘肽-S-转移酶(GST)。Phase 3。	Biomaterials, 2019, 219:119368 Free Radic Biol Med, 2019, 137:1-12 Inflammation, 2018, 41(3):948-958	Effects of p21 depletion and Nrf2 activation on dexamethasone-induced apoptosis in MC3T3-E1 cells. Cells were transfected with control siRNA or p21 siRNA. Subsequently, transfected cells were pre incubated with oltipraz (20 μM) for 1 h, and then co-incubated with 1 μM dexamethasone for 24 h. Apoptosis was measured by flow cytometry, followed by Annexin V-FITC/PI double staining. Effects of p21 depletion and Nrf2 activation on dexamethasone-induced apoptosis in MC3T3-E1 cells. Cells were transfected with control siRNA or p21 siRNA. Subsequently, transfected cells were pre-incubated with oltipraz (20 μM) for 1 h, and then co-incubated with 1 μM dexamethasone for 24 h. Apoptosis was measured by flow cytometry, followed by Annexin V-FITC/PI double staining.
S4863	4-Hydroxyphenylacetic acid 4-Hydroxyphenylacetic acid是一种存在于橄榄油和啤酒中的化合物，作为一种化学中间体用于合成阿替洛尔（atenolol）和3,4-dihydroxyphenylacetic acid。
S6647^New	Bardoxolone Bardoxolone通过从KEAP1释放Nrf2起作用，是Nrf2的激活剂，可以诱导癌细胞凋亡。
S5771	sulforaphane Sulforaphane是一种天然存在的异硫氰酸盐，存在于十字花科蔬菜如西兰花、卷心菜、羽衣甘蓝。它是Nrf2的诱导物。	Int Immunopharmacol, 2019, 74:105646
S3784	Obacunone Obacunone, a natural compound present in citrus fruits, has been demonstrated for various biological activities including anti-cancer and anti-inflammatory properties. It significantly inhibits aromatase activity in an in vitro enzyme assay with an IC50 value of 28.04 μM; also a novel activator of Nrf2.
S3808	Mangiferin Mangiferin is a bioactive compound that demonstrates many health perspectives and has been used to prepare medicinal and food supplements.
S4990	TBHQ Tert-butylhydroquinone (TBHQ)是一种抗氧化剂，用于阻止脂质过氧化，具有多种细胞保护作用。同时，它也是Nrf2的激活剂。	Oxid Med Cell Longev, 2020, 12;2020:1898213 Biochim Biophys Acta Mol Basis Dis, 2019, 10.1016/j.bbadis.2018.12.007 J Appl Toxicol, 2019, 39(10):1394-1404
S5929	4-Octyl Itaconate 4-Octyl Itaconate激活Nrf2信号，在人类巨噬细胞和分离自全身性红斑狼疮患者的PBMC中抑制促炎性因子的产生。
S4712	Diethylmaleate Diethylmaleate是Nrf2的激活剂，是马来酸的二乙酯形式，能消耗谷胱甘肽并抑制NFkB。

目录号

产品描述

文献引用

实验数据

S7956^New

Brustaol

Brustaol，可分离自B. javanica果实，是一种NRF2抑制剂。

S8790

ML385

ML385是一种新型的、特异的NRF2抑制剂，IC50为1.9 μM。它能抑制NRF2的下游靶基因的表达。NRF2 可调节多种铁死亡和脂质过氧化相关蛋白的活性。

Front Immunol,2020, 10:2969

Oxid Med Cell Longev,2020, 12;2020:1898213

Med Sci Monit,2020, 26;26:e923251

目录号	产品描述	文献引用	实验数据
S1848	Curcumin Curcumin 是流行的印度香料姜黄的主要姜黄色素，属于姜科（Zingiberaceae）。它是p300 histone acetylatransferase（IC50~25 μM）和Histone deacetylase的抑制剂，能够激活Nrf2 pathway并抑制NF-κB的激活。	Front Microbiol, 2020, 15;10:3016 Protein Sci, 2020, 29(6):1366-1372 Pharm Biol, 2020, 58(1):25-34
S2586	Dimethyl Fumarate Dimethyl Fumarate 是一种很有前途的新型口服治疗选择，治疗复发-缓解型多发性硬化症患者，降低疾病恶化。	PLoS Pathog, 2020, 16;16(3):e1008341 Am J Cancer Res, 2020, 1;10(5):1442-1454 Cancer Biol Ther, 2014, 15(12):1646-57	DMF enhances proteasome inhibitor toxicity in tumor cells. (A) GBM5/6/12/14 cells were treated with DMF (5 μM), velcade (10 nM) or the drug combination. Cells were isolated 24 h after treatment and viability determined by trypan blue exclusion assay (n = 3, +/− SEM) *P < 0.05 greater than DMF alone.
S7864	Oltipraz Oltipraz 是一种有效的 Nrf2 激活剂，也是一种有效的II期解毒酶诱导剂，显著作用于谷胱甘肽-S-转移酶(GST)。Phase 3。	Biomaterials, 2019, 219:119368 Free Radic Biol Med, 2019, 137:1-12 Inflammation, 2018, 41(3):948-958	Effects of p21 depletion and Nrf2 activation on dexamethasone-induced apoptosis in MC3T3-E1 cells. Cells were transfected with control siRNA or p21 siRNA. Subsequently, transfected cells were pre incubated with oltipraz (20 μM) for 1 h, and then co-incubated with 1 μM dexamethasone for 24 h. Apoptosis was measured by flow cytometry, followed by Annexin V-FITC/PI double staining. Effects of p21 depletion and Nrf2 activation on dexamethasone-induced apoptosis in MC3T3-E1 cells. Cells were transfected with control siRNA or p21 siRNA. Subsequently, transfected cells were pre-incubated with oltipraz (20 μM) for 1 h, and then co-incubated with 1 μM dexamethasone for 24 h. Apoptosis was measured by flow cytometry, followed by Annexin V-FITC/PI double staining.
S4863	4-Hydroxyphenylacetic acid 4-Hydroxyphenylacetic acid是一种存在于橄榄油和啤酒中的化合物，作为一种化学中间体用于合成阿替洛尔（atenolol）和3,4-dihydroxyphenylacetic acid。
S6647^New	Bardoxolone Bardoxolone通过从KEAP1释放Nrf2起作用，是Nrf2的激活剂，可以诱导癌细胞凋亡。
S5771	sulforaphane Sulforaphane是一种天然存在的异硫氰酸盐，存在于十字花科蔬菜如西兰花、卷心菜、羽衣甘蓝。它是Nrf2的诱导物。	Int Immunopharmacol, 2019, 74:105646
S3784	Obacunone Obacunone, a natural compound present in citrus fruits, has been demonstrated for various biological activities including anti-cancer and anti-inflammatory properties. It significantly inhibits aromatase activity in an in vitro enzyme assay with an IC50 value of 28.04 μM; also a novel activator of Nrf2.
S3808	Mangiferin Mangiferin is a bioactive compound that demonstrates many health perspectives and has been used to prepare medicinal and food supplements.
S4990	TBHQ Tert-butylhydroquinone (TBHQ)是一种抗氧化剂，用于阻止脂质过氧化，具有多种细胞保护作用。同时，它也是Nrf2的激活剂。	Oxid Med Cell Longev, 2020, 12;2020:1898213 Biochim Biophys Acta Mol Basis Dis, 2019, 10.1016/j.bbadis.2018.12.007 J Appl Toxicol, 2019, 39(10):1394-1404
S5929	4-Octyl Itaconate 4-Octyl Itaconate激活Nrf2信号，在人类巨噬细胞和分离自全身性红斑狼疮患者的PBMC中抑制促炎性因子的产生。
S4712	Diethylmaleate Diethylmaleate是Nrf2的激活剂，是马来酸的二乙酯形式，能消耗谷胱甘肽并抑制NFkB。