S8790 |
ML385
|
ML385 is a novel and specific NRF2 inhibitor with an IC50 of 1.9 μM. It inhibits the downstream target gene expression of NRF2. NRF2 regulates the activity of several ferroptosis and lipid peroxidation-related proteins. |
-
J Adv Res, 2024, S2090-1232(24)00422-3
-
Int J Biol Sci, 2024, 20(6):2323-2338
-
Cell Death Dis, 2024, 15(2):175
|
|
S1848 |
Curcumin
|
Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on. |
-
Cancer Cell Int, 2024, 24(1):303
-
Front Pharmacol, 2024, 15:1418902
-
PLoS Negl Trop Dis, 2024, 18(8):e0012428
|
|
S8078 |
Bardoxolone Methyl
|
Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor. Bardoxolone Methyl abrogates ferroptosis. Bardoxolone methyl induces apoptosis and autophagy in cancer cells. |
-
Nat Commun, 2024, 15(1):7249
-
Sci Rep, 2024, 14(1):22572
-
Nat Commun, 2023, 14(1):3648
|
|
S4990 |
TBHQ
|
Tert-butylhydroquinone (TBHQ) is an antioxidant compound which is used to prevent lipid peroxidation and shows multiple cytoprotective actions. It is an activator of Nrf2. |
-
Mol Med, 2024, 30(1):111
-
Adv Sci (Weinh), 2023, 10(14):e2204438
-
Adv Sci (Weinh), 2023, 10(3):e2203718
|
|
S2586 |
DMF (Dimethyl Fumarate)
|
DMF (Dimethyl Fumarate) is the methyl ester of fumaric acid, used to treat people with relapsing forms of multiple sclerosis. |
-
Mil Med Res, 2024, 11(1):22
-
J Neuroinflammation, 2024, 21(1):112
-
Cell Death Dis, 2024, 15(3):224
|
|
S7956 |
Brusatol
|
Brusatol (NSC 172924), isolated from the fruit of B. javanica, is a NRF2 inhibitor. |
-
Redox Biol, 2024, 72:103137
-
Iran J Immunol, 2024, 21(1)
-
bioRxiv, 2024, 2024.07.09.602769
|
|
S7864 |
Oltipraz
|
Oltipraz is a potent Nrf2 activator and a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST). Phase 3.
|
-
J Neuroinflammation, 2023, 20(1):212
-
PLoS Genet, 2022, 18(3):e1010128
-
Int Immunopharmacol, 2021, 96:107738
|
|
S7672 |
Omaveloxolone (RTA-408)
|
Omaveloxolone (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.
|
-
Front Oncol, 2023, 13:1126354
-
Cell Discov, 2022, 8(1):106
-
Brain Behav, 2021, 11(1):e01918
|
|
S5144 |
Neferine
|
Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. Neferine induces apoptosis in renal cancer cells. Neferine prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. Neferine strongly inhibits NF-κB activation. Neferine possesses a number of therapeutic effects such as anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV. |
-
Bone Res, 2022, 10(1):27
-
Cell Death Dis, 2022, 13(11):1000
-
iScience, 2022, 25(11):105394
|
|
S6647 |
Bardoxolone (CDDO)
|
Bardoxolone (CDDO), acts by releasing Nrf2 from KEAP1,is a highly potent activator of Nrf2 that induce programmed cell death (apoptosis) in cancer cells. |
-
Cell Rep, 2023, 42(4):112399
-
Mol Cancer Ther, 2021, molcanther.0973.2020
-
Arch Biochem Biophys, 2021, 708:108964
|
|
S5929 |
4-Octyl Itaconate
|
4-Octyl Itaconate activates Nrf2 signaling to inhibit the production of pro-inflammatory cytokines in human macrophages and systemic lupus erythematosus (SLE) patient-derived PBMCs. |
-
Cell Death Dis, 2022, 13(6):521
-
Eur Rev Med Pharmacol Sci, 2021, 25(16):5189-5198
|
|
S3275 |
Senkyunolide I
|
Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9. |
-
World J Emerg Med, 2024, 15(3):206-213
-
SSRN , 2024, 10.2139/ssrn.4696834
-
Cancer Biol Med, 2022, 19(11)j.issn.2095-3941.2022.0451
|
|
S9723 |
CDDO-Im (RTA-403)
|
CDDO-Im (RTA-403) is an activator of nuclear factor erythroid 2–related factor 2 (Nrf2) and peroxisome proliferator-activated receptor (PPAR). CDDO-Im binds to PPARα and PPARγ with Ki of 232 nM and 344 nM, respectively. CDDO-Im inhibits inflammatory response and tumor growth in vivo. |
-
Ecotoxicol Environ Saf, 2022, 241:113754
-
Int J Mol Sci, 2022, 23(19)11715
|
|
S3784 |
Obacunone (AI3-37934)
|
Obacunone (AI3-37934, CCRIS 8657), 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. |
-
Int J Mol Sci, 2023, 24(14)11484
-
Cell Mol Biol Lett, 2022, 27(1):29
|
|
S3168 |
cis-Resveratrol
|
cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively. |
-
J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
|
|
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. |
-
Front Pharmacol, 2022, 13:1028932
|
|
E1141 |
KI696
|
KI696 is a potent and selective inhibitor of KEAP1/NRF2 interaction. KI696 induces the expression of each of the Nqo1, Ho-1, Txnrd1, Srxn1, Gsta3, Gclc genes in a dose-dependent manner. |
-
Redox Biol, 2024, 72:103137
|
|
S3301 |
Cynarin
|
Cynarin (Cynarine) is an artichoke phytochemical that possesses a variety of pharmacological features including free-radical scavenging, antioxidant, antihistamic and antiviral activities. Cynarin blocks the interaction between the CD28 of T-cell receptor and CD80 of antigen presenting cells. Cynarin triggers Nrf2 nuclear translocation, restores the balance of glutathione (GSH) and reactive oxygen species (ROS), and inhibits mitochondrial depolarization. |
|
|
S5771 |
Sulforaphane
|
Sulforaphane is a naturally occurring isothiocyanate derived from the consumption of cruciferous vegetables, such as broccoli, cabbage, and kale. It is an inducer of Nrf2. Sulforaphane is also an inhibitor of histone deacetylase (HDAC) and NF-κB. Sulforaphane increases heme oxygenase-1 (HO-1) and reduces the levels of reactive oxygen species (ROS). Sulforaphane induces cell cycle arrest and apoptosis. |
-
Nucleic Acids Res, 2024, gkae761
-
Redox Biol, 2024, 72:103137
-
J Adv Res, 2024, S2090-1232(24)00422-3
|
|
E0441 |
NK-252
|
NK-252 is an activator of Nrf2 and interacts with the Nrf2-binding site of Keap1. |
|
|
E1339 |
HPPE
|
HPPE is a specific nonelectrophilic and physiological Bach1 inhibitor via heme-binding sites of Bach1 protein, derepresses Bach1-mediated repression. |
|
|
E1220 |
CBR-470-1
|
CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nrf2 activator. CBR-470-1 protects SH-SY5Y neuronal cells against MPP+-induced cytotoxicity through activation of the Keap1-Nrf2 cascade. |
|
|
E1281 |
Dimethyl itaconate
|
Dimethyl itaconate can reprogram neurotoxic to neuroprotective primary astrocytes through the regulation of LPS-induced Nod-like receptor protein 3 (NLRP3) inflammasome and nuclear factor 2/heme oxygenase-1 (NRF2/HO-1) pathways. |
|
|
E0526 |
sappanone A
|
Sappanone A, a homoisoflavanone isolated from the heartwood of Caesalpinia sappan (Leguminosae), induces HO-1 expression by activating Nrf2 through the p38 MAPK pathway, suppresses LPS-induced NF-κB activation by suppressing the phosphorylation of RelA/p65 at Ser536, exerting its anti-inflammatory effect. |
|
|
E0023 |
5,7-Dihydroxychromone
|
5,7-Dihydroxychromone (DHC), a natural antioxidant extracted from plants, is a potent activator of Nrf2/ARE signal. 5,7-dihydroxychromone also is a potent activator of PPARγ and LXRα. 5,7-Dihydroxychromone may contributes to regulate blood glucose levels and shows anti-diabetic property. |
|
|
E1973New |
R16
|
R16(NSC29869, Nrf2-IN-3) is an inhibitor of NRF2 (nuclear factor erythroid 2-related factor 2) that selectively binds KEAP1 mutants and restores their NRF2-inhibitory function by repairing the disrupted KEAP1/NRF2 interactions. It significantly enhances the sensitivity of KEAP1-mutated tumor cells to cisplatin and gefitinib. |
|
|
E0129 |
Oxysophocarpine
|
Oxysophocarpine (OSC) is an alkaloid extracted from Sophora alopecuroides. Oxysophocarpine inhibits the growth and metastasis of oral squamous cell carcinoma (OSCC) by targeting the Nrf2/HO-1 axis. OSC protects cells against apoptosis and inflammatory responses and compromised miR-155 activity by attenuating MAPK and NF-κB pathways. |
|
|
E4007 |
L-Sulforaphane
|
L-Sulforaphane ((R)-Sulforaphane) is a highly potent inducer of the Keap1/Nrf2/ARE pathway. It is a more potent inducer of the carcinogen-detoxifying enzyme systems in rat liver and lung than the S-isomer. |
|
|
S4712 |
Diethylmaleate
|
Diethylmaleate (Diethyl ester, Maleic acid diethyl ester) is the diethyl ester of maleic acid and a glutathione-depleting compound that inhibits NF-κB. |
|
|
S3205 |
Perillaldehyde
|
Perillaldehyde (Perilladehyde, Perillal, PAE, PA), the main component of Perilla frutescens (a traditional medicinal antioxidant herb), inhibits BaP-induced AHR activation and ROS production, inhibits BaP/AHR-mediated release of the CCL2 chemokine, and activats the NRF2/HO1 antioxidant pathway. |
|
|
E1339 |
HPPE
|
HPPE is a specific nonelectrophilic and physiological Bach1 inhibitor via heme-binding sites of Bach1 protein, derepresses Bach1-mediated repression. |
|
|
E0526 |
sappanone A
|
Sappanone A, a homoisoflavanone isolated from the heartwood of Caesalpinia sappan (Leguminosae), induces HO-1 expression by activating Nrf2 through the p38 MAPK pathway, suppresses LPS-induced NF-κB activation by suppressing the phosphorylation of RelA/p65 at Ser536, exerting its anti-inflammatory effect. |
|
|
S1848 |
Curcumin
|
Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on. |
- Cancer Cell Int, 2024, 24(1):303
- Front Pharmacol, 2024, 15:1418902
- PLoS Negl Trop Dis, 2024, 18(8):e0012428
|
|
S8078 |
Bardoxolone Methyl
|
Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor. Bardoxolone Methyl abrogates ferroptosis. Bardoxolone methyl induces apoptosis and autophagy in cancer cells. |
- Nat Commun, 2024, 15(1):7249
- Sci Rep, 2024, 14(1):22572
- Nat Commun, 2023, 14(1):3648
|
|
S4990 |
TBHQ
|
Tert-butylhydroquinone (TBHQ) is an antioxidant compound which is used to prevent lipid peroxidation and shows multiple cytoprotective actions. It is an activator of Nrf2. |
- Mol Med, 2024, 30(1):111
- Adv Sci (Weinh), 2023, 10(14):e2204438
- Adv Sci (Weinh), 2023, 10(3):e2203718
|
|
S2586 |
DMF (Dimethyl Fumarate)
|
DMF (Dimethyl Fumarate) is the methyl ester of fumaric acid, used to treat people with relapsing forms of multiple sclerosis. |
- Mil Med Res, 2024, 11(1):22
- J Neuroinflammation, 2024, 21(1):112
- Cell Death Dis, 2024, 15(3):224
|
|
S7864 |
Oltipraz
|
Oltipraz is a potent Nrf2 activator and a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST). Phase 3.
|
- J Neuroinflammation, 2023, 20(1):212
- PLoS Genet, 2022, 18(3):e1010128
- Int Immunopharmacol, 2021, 96:107738
|
|
S7672 |
Omaveloxolone (RTA-408)
|
Omaveloxolone (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.
|
- Front Oncol, 2023, 13:1126354
- Cell Discov, 2022, 8(1):106
- Brain Behav, 2021, 11(1):e01918
|
|
S5144 |
Neferine
|
Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. Neferine induces apoptosis in renal cancer cells. Neferine prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. Neferine strongly inhibits NF-κB activation. Neferine possesses a number of therapeutic effects such as anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV. |
- Bone Res, 2022, 10(1):27
- Cell Death Dis, 2022, 13(11):1000
- iScience, 2022, 25(11):105394
|
|
S6647 |
Bardoxolone (CDDO)
|
Bardoxolone (CDDO), acts by releasing Nrf2 from KEAP1,is a highly potent activator of Nrf2 that induce programmed cell death (apoptosis) in cancer cells. |
- Cell Rep, 2023, 42(4):112399
- Mol Cancer Ther, 2021, molcanther.0973.2020
- Arch Biochem Biophys, 2021, 708:108964
|
|
S5929 |
4-Octyl Itaconate
|
4-Octyl Itaconate activates Nrf2 signaling to inhibit the production of pro-inflammatory cytokines in human macrophages and systemic lupus erythematosus (SLE) patient-derived PBMCs. |
- Cell Death Dis, 2022, 13(6):521
- Eur Rev Med Pharmacol Sci, 2021, 25(16):5189-5198
|
|
S3275 |
Senkyunolide I
|
Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9. |
- World J Emerg Med, 2024, 15(3):206-213
- SSRN , 2024, 10.2139/ssrn.4696834
- Cancer Biol Med, 2022, 19(11)j.issn.2095-3941.2022.0451
|
|
S9723 |
CDDO-Im (RTA-403)
|
CDDO-Im (RTA-403) is an activator of nuclear factor erythroid 2–related factor 2 (Nrf2) and peroxisome proliferator-activated receptor (PPAR). CDDO-Im binds to PPARα and PPARγ with Ki of 232 nM and 344 nM, respectively. CDDO-Im inhibits inflammatory response and tumor growth in vivo. |
- Ecotoxicol Environ Saf, 2022, 241:113754
- Int J Mol Sci, 2022, 23(19)11715
|
|
S3784 |
Obacunone (AI3-37934)
|
Obacunone (AI3-37934, CCRIS 8657), 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. |
- Int J Mol Sci, 2023, 24(14)11484
- Cell Mol Biol Lett, 2022, 27(1):29
|
|
S3168 |
cis-Resveratrol
|
cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively. |
- J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
|
|
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. |
- Front Pharmacol, 2022, 13:1028932
|
|
S3301 |
Cynarin
|
Cynarin (Cynarine) is an artichoke phytochemical that possesses a variety of pharmacological features including free-radical scavenging, antioxidant, antihistamic and antiviral activities. Cynarin blocks the interaction between the CD28 of T-cell receptor and CD80 of antigen presenting cells. Cynarin triggers Nrf2 nuclear translocation, restores the balance of glutathione (GSH) and reactive oxygen species (ROS), and inhibits mitochondrial depolarization. |
|
|
S5771 |
Sulforaphane
|
Sulforaphane is a naturally occurring isothiocyanate derived from the consumption of cruciferous vegetables, such as broccoli, cabbage, and kale. It is an inducer of Nrf2. Sulforaphane is also an inhibitor of histone deacetylase (HDAC) and NF-κB. Sulforaphane increases heme oxygenase-1 (HO-1) and reduces the levels of reactive oxygen species (ROS). Sulforaphane induces cell cycle arrest and apoptosis. |
- Nucleic Acids Res, 2024, gkae761
- Redox Biol, 2024, 72:103137
- J Adv Res, 2024, S2090-1232(24)00422-3
|
|
E0441 |
NK-252
|
NK-252 is an activator of Nrf2 and interacts with the Nrf2-binding site of Keap1. |
|
|
E1220 |
CBR-470-1
|
CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nrf2 activator. CBR-470-1 protects SH-SY5Y neuronal cells against MPP+-induced cytotoxicity through activation of the Keap1-Nrf2 cascade. |
|
|
E0023 |
5,7-Dihydroxychromone
|
5,7-Dihydroxychromone (DHC), a natural antioxidant extracted from plants, is a potent activator of Nrf2/ARE signal. 5,7-dihydroxychromone also is a potent activator of PPARγ and LXRα. 5,7-Dihydroxychromone may contributes to regulate blood glucose levels and shows anti-diabetic property. |
|
|
E4007 |
L-Sulforaphane
|
L-Sulforaphane ((R)-Sulforaphane) is a highly potent inducer of the Keap1/Nrf2/ARE pathway. It is a more potent inducer of the carcinogen-detoxifying enzyme systems in rat liver and lung than the S-isomer. |
|
|
S4712 |
Diethylmaleate
|
Diethylmaleate (Diethyl ester, Maleic acid diethyl ester) is the diethyl ester of maleic acid and a glutathione-depleting compound that inhibits NF-κB. |
|
|
S3205 |
Perillaldehyde
|
Perillaldehyde (Perilladehyde, Perillal, PAE, PA), the main component of Perilla frutescens (a traditional medicinal antioxidant herb), inhibits BaP-induced AHR activation and ROS production, inhibits BaP/AHR-mediated release of the CCL2 chemokine, and activats the NRF2/HO1 antioxidant pathway. |
|
|