Nrf2

抑制剂选择性比较

Nrf2产品

所有产品(21) Nrf2抑制剂(2) Nrf2激活剂(19)

目录号	产品描述	文献引用	实验数据
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。	Free Radic Biol Med, 2021, 164:249-257 Biochem Biophys Res Commun, 2021, 536:100-106 Cell Biochem Biophys, 2021, 10.1007/s12013-020-00959-6
S7956	Brusatol Brusatol (NSC 172924)，可分离自B. javanica果实，是一种NRF2抑制剂。	J Mol Histol, 2020, 10.1007/s10735-020-09904-6
S8078	Bardoxolone Methyl Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) 是一种IKK抑制剂，具有强的促凋亡和抗炎活性。同时还是有效的Nrf2激活剂和NF-κB抑制剂。Bardoxolone Methyl 可抑制铁死亡。Bardoxolone Methyl 在癌细胞中可诱导凋亡和自噬。	Drug Des Devel Ther, 2021, 15:21-35 Cancers (Basel), 2020, 12(6):E1645 Antioxidants (Basel), 2020, 9(1)	Renal Nrf2 activity was shown in RTA402-treated acFSGS (RTA402 + acFSGS) mice as early as day 7 (RTA402 + acFSGS) and persisted to day 28, compared to vehicle + acFSGS mice. Kidney in situ ROS production demonstrated by DHE detection.
S1848	Curcumin Curcumin (Diferuloylmethane) 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 (HDAC)的抑制剂，能够激活Nrf2 pathway并抑制NF-κB的激活。Curcumin 可诱导线粒体自噬、细胞自噬、凋亡和细胞周期阻滞，并具有抗肿瘤的活性。Curcumin 可通过减少铁死亡介导的细胞死亡来减少横纹肌溶解相关的肾衰竭。Curcumin 对各种人类病原体（如流感病毒，丙型肝炎病毒，HIV等）具有抗感染特性。	Adv Biol Regul, 2021, S2212-4926(20)30091-9 Mol Cell, 2020, 80(3):525-540.e9 Front Microbiol, 2020, 15;10:3016
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.
S7672	Omaveloxolone (RTA-408) Omaveloxolone (RTA-408)是一种合成的三萜类化合物，其激活细胞保护转录因子 Nrf2 并抑制 NF-κB 信号。Phase 2。	Brain Behav, 2021, 11(1):e01918 Cancers (Basel), 2020, 12(9)E2668 Int J Neurosci, 2020, 7:1-16
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.
S3168^New	cis-Resveratrol cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) 是Resveratrol的顺式异构体。Resveratrol 是一种天然的酚类化合物，具有抗氧化、抗炎、保护心脏和抗癌的特性。Resveratrol 是 pregnane X receptor (PXR) 的抑制剂，也是 Nrf2 和 SIRT1 的激活剂，并可能诱导凋亡。Resveratrol 还可抑制多种靶标，包括 5-lipoxygenase (LOX)、cyclooxygenase (COX)、IKKβ、DNA polymerases α和δ，IC50分别为2.7 μM、<1 μM、1 μM、3.3 μM和5 μM。
S9723^New	CDDO-Im CDDO-Im (CDDO-Imidazolide, RTA-403, TP-235) 是一种 nuclear factor erythroid 2–related factor 2 (Nrf2) 和 peroxisome proliferator-activated receptor (PPAR) 的激活剂。CDDO-Im 可与PPARα和PPARγ结合，对应的Ki值分别以232 nM和344 nM。CDDO-Im 在体内抑制炎症反应和肿瘤生长。
S3275^New	Senkyunolide I Senkyunolide I (SEI, SENI) 是一种从 Ligusticum chuanxiong 中提取的口服活性化合物，具有止痛、抗偏头痛、神经保护、抗氧化和抗凋亡的活性。Senkyunolide I (SEI, SENI) 可上调 Erk1/2 的磷酸化，并诱导 Nrf2 的核易位，伴随着HO-1和NQO1的表达增强。Senkyunolide I (SEI, SENI) 可提高 Bcl-2/Bax 的比例，并抑制裂化的 caspase 3 和 caspase 9 的表达。
S3301^New	Cynarin Cynarin (Cynarine) 是一种来自artichoke洋蓟的植物化学成分，具有多种药理特性，包括自由基清除、抗氧化剂、抗组氨酸和抗病毒活性。Cynarin 可阻断T细胞受体的 CD28 和抗原呈递细胞的 CD80 之间的相互作用。Cynarin 可触发 Nrf2 的核易位，恢复 glutathione (GSH) 和 reactive oxygen species (ROS) 的平衡，并抑制线粒体去极化。
S3205^New	Perillaldehyde Perillaldehyde (Perilladehyde, Perillal, PAE, PA) 是紫苏 Perilla frutescens（一种传统的抗氧化剂）的主要成分，可抑制BaP诱导的 AHR 的活化和 ROS 的产生，抑制 BaP/AHR 介导的 CCL2 chemokine 的释放，并激活 NRF2/HO1 抗氧化剂途径。
S5144	Neferine Neferine ((R)-1,2-Dimethoxyaporphine) 是 Nelumbo nucifera 的天然成分，具有抗肿瘤功效。Neferine 可诱导肾癌细胞凋亡。Neferine 通过激活肌肉细胞中的 Akt/mTOR 通路和 Nrf2 来防止自噬。Neferine 可抑制 NF-κB 的激活。Neferine具有多种治疗作用，例如抗糖尿病，抗衰老，抗微生物，抗血栓形成，抗心律不齐，抗炎甚至抗HIV。	Oncol Rep, 2020, 44(3):1116-1126
S4863	4-Hydroxyphenylacetic acid 4-Hydroxyphenylacetic acid (p-Hydroxyphenylacetic acid, parahydroxy phenylacetate) 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	Bardoxolone Bardoxolone (CDDO, RTA 401)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。	Cell, 2020, S0092-8674(20)31626-3
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。Sulforaphane 也是 histone deacetylase (HDAC) 和 NF-κB 的抑制剂。Sulforaphane 可增加 heme oxygenase-1 (HO-1)，并降低 reactive oxygen species (ROS) 的水平。Sulforaphane 诱导细胞周期停滞和凋亡。	Int Immunopharmacol, 2019, 74:105646 Chem Res Toxicol, 2018, 31(2):127-136
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 (Alpizarin, Chinomin, Hedysarid) is a bioactive compound that demonstrates many health perspectives and has been used to prepare medicinal and food supplements. Mangiferin is a Nrf2 activator. Mangiferin suppresses nuclear translocation of the NF-κB subunits p65 and p50.
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 Oxid Med Cell Longev, 2020, 2020:6123459 Biochim Biophys Acta Mol Basis Dis, 2019, 10.1016/j.bbadis.2018.12.007
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 (Diethyl ester, Maleic acid diethyl ester) 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
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。	Free Radic Biol Med,2021, 164:249-257 Biochem Biophys Res Commun,2021, 536:100-106 Cell Biochem Biophys,2021, 10.1007/s12013-020-00959-6
S7956	Brusatol Brusatol (NSC 172924)，可分离自B. javanica果实，是一种NRF2抑制剂。	J Mol Histol,2020, 10.1007/s10735-020-09904-6

目录号

产品描述

文献引用

实验数据

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。

Free Radic Biol Med,2021, 164:249-257

Biochem Biophys Res Commun,2021, 536:100-106

Cell Biochem Biophys,2021, 10.1007/s12013-020-00959-6

S7956

Brusatol

Brusatol (NSC 172924)，可分离自B. javanica果实，是一种NRF2抑制剂。

J Mol Histol,2020, 10.1007/s10735-020-09904-6

目录号	产品描述	文献引用	实验数据
S8078	Bardoxolone Methyl Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) 是一种IKK抑制剂，具有强的促凋亡和抗炎活性。同时还是有效的Nrf2激活剂和NF-κB抑制剂。Bardoxolone Methyl 可抑制铁死亡。Bardoxolone Methyl 在癌细胞中可诱导凋亡和自噬。	Drug Des Devel Ther, 2021, 15:21-35 Cancers (Basel), 2020, 12(6):E1645 Antioxidants (Basel), 2020, 9(1)	Renal Nrf2 activity was shown in RTA402-treated acFSGS (RTA402 + acFSGS) mice as early as day 7 (RTA402 + acFSGS) and persisted to day 28, compared to vehicle + acFSGS mice. Kidney in situ ROS production demonstrated by DHE detection.
S1848	Curcumin Curcumin (Diferuloylmethane) 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 (HDAC)的抑制剂，能够激活Nrf2 pathway并抑制NF-κB的激活。Curcumin 可诱导线粒体自噬、细胞自噬、凋亡和细胞周期阻滞，并具有抗肿瘤的活性。Curcumin 可通过减少铁死亡介导的细胞死亡来减少横纹肌溶解相关的肾衰竭。Curcumin 对各种人类病原体（如流感病毒，丙型肝炎病毒，HIV等）具有抗感染特性。	Adv Biol Regul, 2021, S2212-4926(20)30091-9 Mol Cell, 2020, 80(3):525-540.e9 Front Microbiol, 2020, 15;10:3016
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.
S7672	Omaveloxolone (RTA-408) Omaveloxolone (RTA-408)是一种合成的三萜类化合物，其激活细胞保护转录因子 Nrf2 并抑制 NF-κB 信号。Phase 2。	Brain Behav, 2021, 11(1):e01918 Cancers (Basel), 2020, 12(9)E2668 Int J Neurosci, 2020, 7:1-16
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.
S3168^New	cis-Resveratrol cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) 是Resveratrol的顺式异构体。Resveratrol 是一种天然的酚类化合物，具有抗氧化、抗炎、保护心脏和抗癌的特性。Resveratrol 是 pregnane X receptor (PXR) 的抑制剂，也是 Nrf2 和 SIRT1 的激活剂，并可能诱导凋亡。Resveratrol 还可抑制多种靶标，包括 5-lipoxygenase (LOX)、cyclooxygenase (COX)、IKKβ、DNA polymerases α和δ，IC50分别为2.7 μM、<1 μM、1 μM、3.3 μM和5 μM。
S9723^New	CDDO-Im CDDO-Im (CDDO-Imidazolide, RTA-403, TP-235) 是一种 nuclear factor erythroid 2–related factor 2 (Nrf2) 和 peroxisome proliferator-activated receptor (PPAR) 的激活剂。CDDO-Im 可与PPARα和PPARγ结合，对应的Ki值分别以232 nM和344 nM。CDDO-Im 在体内抑制炎症反应和肿瘤生长。
S3275^New	Senkyunolide I Senkyunolide I (SEI, SENI) 是一种从 Ligusticum chuanxiong 中提取的口服活性化合物，具有止痛、抗偏头痛、神经保护、抗氧化和抗凋亡的活性。Senkyunolide I (SEI, SENI) 可上调 Erk1/2 的磷酸化，并诱导 Nrf2 的核易位，伴随着HO-1和NQO1的表达增强。Senkyunolide I (SEI, SENI) 可提高 Bcl-2/Bax 的比例，并抑制裂化的 caspase 3 和 caspase 9 的表达。
S3301^New	Cynarin Cynarin (Cynarine) 是一种来自artichoke洋蓟的植物化学成分，具有多种药理特性，包括自由基清除、抗氧化剂、抗组氨酸和抗病毒活性。Cynarin 可阻断T细胞受体的 CD28 和抗原呈递细胞的 CD80 之间的相互作用。Cynarin 可触发 Nrf2 的核易位，恢复 glutathione (GSH) 和 reactive oxygen species (ROS) 的平衡，并抑制线粒体去极化。
S3205^New	Perillaldehyde Perillaldehyde (Perilladehyde, Perillal, PAE, PA) 是紫苏 Perilla frutescens（一种传统的抗氧化剂）的主要成分，可抑制BaP诱导的 AHR 的活化和 ROS 的产生，抑制 BaP/AHR 介导的 CCL2 chemokine 的释放，并激活 NRF2/HO1 抗氧化剂途径。
S5144	Neferine Neferine ((R)-1,2-Dimethoxyaporphine) 是 Nelumbo nucifera 的天然成分，具有抗肿瘤功效。Neferine 可诱导肾癌细胞凋亡。Neferine 通过激活肌肉细胞中的 Akt/mTOR 通路和 Nrf2 来防止自噬。Neferine 可抑制 NF-κB 的激活。Neferine具有多种治疗作用，例如抗糖尿病，抗衰老，抗微生物，抗血栓形成，抗心律不齐，抗炎甚至抗HIV。	Oncol Rep, 2020, 44(3):1116-1126
S4863	4-Hydroxyphenylacetic acid 4-Hydroxyphenylacetic acid (p-Hydroxyphenylacetic acid, parahydroxy phenylacetate) 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	Bardoxolone Bardoxolone (CDDO, RTA 401)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。	Cell, 2020, S0092-8674(20)31626-3
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。Sulforaphane 也是 histone deacetylase (HDAC) 和 NF-κB 的抑制剂。Sulforaphane 可增加 heme oxygenase-1 (HO-1)，并降低 reactive oxygen species (ROS) 的水平。Sulforaphane 诱导细胞周期停滞和凋亡。	Int Immunopharmacol, 2019, 74:105646 Chem Res Toxicol, 2018, 31(2):127-136
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 (Alpizarin, Chinomin, Hedysarid) is a bioactive compound that demonstrates many health perspectives and has been used to prepare medicinal and food supplements. Mangiferin is a Nrf2 activator. Mangiferin suppresses nuclear translocation of the NF-κB subunits p65 and p50.
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 Oxid Med Cell Longev, 2020, 2020:6123459 Biochim Biophys Acta Mol Basis Dis, 2019, 10.1016/j.bbadis.2018.12.007
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 (Diethyl ester, Maleic acid diethyl ester) 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。

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