Keap1–Nrf2 IN-1 (compound35) is a Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2 (Keap1-Nrf2) protein-protein interaction inhibitor, and with an IC50 of 43 nM for Keap1 protein. Keap1–Nrf2 IN-1 (compound35) activates Nrf2-regulated cytoprotective response and antagonizes acetaminophen-induced liver injury both in cellular and in vivo models[1].
Ginsenoside Rg3 is the main component of Red ginseng. Ginsenoside Rg3 inhibits Na+ and hKv1.4 channel with IC50s of 32.2±4.5 and 32.6±2.2 μM, respectively. Ginsenoside Rg3 also inhibits Aβ levels, NF-κB activity, and COX-2 expression.
DMX-129 is an ΙΚΚε and TBK-1 inhibitor with IC50 values of <30 nM for both TBK1 and IKKε[1].
Z-VRPR-FMK is an irreversible MALT1 protein inhibitor. Z-VRPR-FMK inhibits the growth and invasion of diffuse large B-cell lymphoma by inhibiting MALT1-induced NF-κB activation and MMP expression[1].
Astilbin, a flavonoid compound, is isolated from the rhizome of Smilax glabra. Astilbin enhances NRF2 activation. Astilbin also suppresses TNF-α expression and NF-κB activation.
Pyrrolidinedithiocarbamate ammonium is a selective NF-κB inhibitor.
Pyridoxine-d5 (hydrochloride) is the deuterium labeled Pyridoxine hydrochloride[1]. Pyridoxine hydrochloride (Pyridoxol;Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol;Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway[2].
Sulfasalazine is a drug for the treatment of rheumatoid arthritis and ulcerative colitis. Sulfasalazine is reported to suppress NF-κB activity.
NK-252 is a potential Nrf2 activator, which exhibits a great Nrf2-activating potential.
Antroquinonol ((+)-Antroquinonol), a ubiquinone derivative from the mushroom Antrodia camphorata, has hepatoprotective, anti-inflammatory, and anti-cancer effects[1]. Antroquinonol can be used for the research of colon cancer[2]. Antroquinonol reduces oxidative stress by enhancing the Nrf2 signaling pathway and inhibits inflammation and sclerosis in focal segmental glomerulosclerosis mice[3].
TBHQ is an antioxidant that activates Nrf2.
Baicalin is a flavonoid glycoside isolated from Scutellaria baicalensis. Baicalin reduces the expression of NF-κB.
BAY 11-7085 is an inhibitor of NF-κB activation and phosphorylation of IκBα; it stabilizes IκBα with an IC50 of 10 μM.
Eriodictyol is a flavonoid isolated from the Chinese herb, with antioxidant and anti-inflammatory activity. Eriodictyol induces Nrf2 signaling pathway.
Chaetominine is an alkaloidal metabolite. Chaetominine has cytotoxicity against human leukemia K562 and colon cancer SW1116 cell lines. Chaetominine reduces MRP1-mediated drug resistance via inhibiting PI3K/Akt/Nrf2 signaling pathway in K562/Adr human leukemia cells[1][2].
Garcinone D, a natural xanthone from mangosteen, promotes the proliferation of C17.2 neural stem cell. Garcinone D increases the protein levels of phosphorylated signal transducer and activator of transcription 3 (p-STAT3), Cyclin D1 and nuclear factor erythroid 2-related factor (Nrf2), heme oxygenase-1 (HO-1) in concentration- and time- dependent manners[1].
Microcystin-[D-Asp3]-LR/Microcystin A is a cyanotoxin. Microcystin-[D-Asp3]-LR/Microcystin A can activate Nrf2 and promote oxidative stress response. Microcystin-[D-Asp3]-LR/Microcystin A can also be used in toxicology research[1][2].
Dimethyl fumarate is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator and induces upregulation of antioxidant gene expression.
Keap1-Nrf2-IN-13 is a Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with an IC50 value of 0.15 μM. Keap1-Nrf2-IN-13 has strong binding affinities to the Keap1 protein by forming hydrogen bond with the key polar residues (Asn414, Arg415, Arg483, Gln530). Keap1-Nrf2-IN-13 can be used in the research of oxidative stress-related and inflammatory diseases, including pulmonary fibrosis, chronic obstructive pulmonary disorder (COPD) and cancers[1].
A novel potent, selective TBK1 PROTAC with DC50 of 12 nM, selectively degrades TBK1 with excellent selectivity against a related kinase IKKε; a chemical tool to assess TBK1 as a target in mutant K-Ras cancer cells.
AZD3264 is a selective IkB-kinase IKK2 inhibitor.
KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction.
R079 (compound 17) is a selective, orally active Nrf2 activator. R079 increases Nrf2 translocation activity (EC50 = 32.41 μM). R079 can neutralize excess levels of reactive oxygen species through activating Nrf2. R079 has anti-inflammatory properties and can be used in multiple sclerosis research [1].
7-Deacetylgedunin is an activator of Keap1/Nrf2/HO-1. 7-Deacetylgedunin alleviates mice mortality induced by LPS. 7-Deacetylgedunin inhibits Keap1 expression and suppresses macrophage proliferation. 7-Deacetylgedunin suppresses inflammation in vivo and in vitro[1].
5,7-Dihydroxychromone, the extract of Cudrania tricuspidata, activates Nrf2/ARE signal and exerts neuroprotective effects against 6-hydroxydopamine (6-OHDA)-induced oxidative stress and apoptosis. 5,7-Dihydroxychromone inhibits the expression of activated caspase-3 and caspase-9 and cleaved PARP in 6-OHDA-induced SH-SY5Y cells[1].
Hydrangenol is an orally active antiphotoaging compound. It can be isolated from Hydrangea serrata leaves. Hydrangenol prevents wrinkle formation by reducing MMP and inflammatory cytokine expression and increasing moisturizing factors and antioxidant genes level[1].
TPNA10168 is an Nrf-2 activator that activates the Keap1-Nrf2-ARE pathway. TPNA10168 is neuroprotective against oxidative stress-induced damage. TPNA10168 significantly reduces the transcription of inflammatory genes, including TNF-α, IL-1β, IL-6, and iNOS. TPNA10168 can be used in research on anti-inflammatory and neurological diseases[1].
(R)-MALT1-IN-3 (compound 121) is a potent MALT1 protease inhibitor with an IC50 of 20 nM. (R)-MALT1-IN-3 has IC50 of 60 nM, 40 nM for human IL6/IL10 in OCI-LY3 cells, respectively[1].
2-Trifluoromethyl-2'-methoxychalcone is a chalcone derivative. 2-Trifluoromethyl-2'-methoxychalcone is a potent Nrf2 activator. 2-Trifluoromethyl-2'-methoxychalcone can be used for oxidative stress and inflammation related diseases research[1].
TAT-14 is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1[1].