Nrf2
抑制剂选择性比较
Nrf2产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S8790 |
ML385ML385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。 |
||
S7956 |
BrusatolBrusatol (NSC 172924),可分离自B. javanica果实,是一种NRF2抑制剂。 |
||
S8078 |
Bardoxolone MethylBardoxolone 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。 |
![]() ![]() 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 |
CurcuminCurcumin (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。 |
![]() ![]() |
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S2586 |
Dimethyl FumarateDimethyl 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。 |
![]() ![]() 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。 |
||
S7864 |
OltiprazOltipraz 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。 |
![]() ![]() 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. |
|
S3168New |
cis-Resveratrolcis-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。 |
||
S9723New |
CDDO-ImCDDO-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。 |
||
S3275New |
Senkyunolide ISenkyunolide 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。 |
||
S3301New |
CynarinCynarin (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。 |
||
S3205New |
PerillaldehydePerillaldehyde (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 |
NeferineNeferine ((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。 |
||
S4863 |
4-Hydroxyphenylacetic acid4-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 |
BardoxoloneBardoxolone (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。 |
||
S5771 |
SulforaphaneSulforaphane 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。 |
||
S3784 |
ObacunoneObacunone, 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 |
MangiferinMangiferin (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 |
TBHQTert-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。 |
||
S5929 |
4-Octyl Itaconate4-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 |
DiethylmaleateDiethylmaleate (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 |
ML385ML385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。 |
||
S7956 |
BrusatolBrusatol (NSC 172924),可分离自B. javanica果实,是一种NRF2抑制剂。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S8078 |
Bardoxolone MethylBardoxolone 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。 |
![]() ![]() 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 |
CurcuminCurcumin (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。 |
![]() ![]() |
|
S2586 |
Dimethyl FumarateDimethyl 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。 |
![]() ![]() 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。 |
||
S7864 |
OltiprazOltipraz 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。 |
![]() ![]() 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. |
|
S3168New |
cis-Resveratrolcis-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。 |
||
S9723New |
CDDO-ImCDDO-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。 |
||
S3275New |
Senkyunolide ISenkyunolide 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。 |
||
S3301New |
CynarinCynarin (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。 |
||
S3205New |
PerillaldehydePerillaldehyde (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 |
NeferineNeferine ((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。 |
||
S4863 |
4-Hydroxyphenylacetic acid4-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 |
BardoxoloneBardoxolone (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。 |
||
S5771 |
SulforaphaneSulforaphane 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。 |
||
S3784 |
ObacunoneObacunone, 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 |
MangiferinMangiferin (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 |
TBHQTert-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。 |
||
S5929 |
4-Octyl Itaconate4-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 |
DiethylmaleateDiethylmaleate (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。 |