nrf2-dependent

Fluvastatin sodium (Fluvastatin sodium salt), a competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase (HMGCR), is a commonly used cholesterol lowering agent.

Omaveloxolone (RTA-408) is an oral, potent, and selective activator of the nuclear factor erythropoietin-related factor 2 (Nrf2) pathway, as well as a low-potency PPARγ agonist. Omaveloxolone inhibits osteoclast formation by suppressing the STING-dependent NF-κB signaling pathway. Omaveloxolone is being investigated for use in ALS, multiple sclerosis, non-alcoholic steatohepatitis, neurodegenerative diseases, and oncology research.

(3S,5R)-Fluvastatin sodium is the enantiomerically pure form of Fluvastatin, a fully synthetic and competitive HMG-CoA reductase inhibitor with nanomolar potency, (3S,5R)-Fluvastatin sodium additionally protects vascular smooth muscle cells from oxidative stress through activation of the Nrf2-dependent antioxidant pathway, supporting cardiovascular and redox biology research.

(Z)-Ligustilide (Ligustilide A) , an active ingredient isolated from the medicinal plants Angelica acutiloba and Cnidium officinale, inhibits benzo(a)pyrene-induced CYP1A1 upregulation in cultured human keratinocytes via ROS-dependent Nrf2 activation.

Antioxidant agent-20 (Compound 3d) exhibits potent anti-inflammatory and antioxidant activities. It reduces reactive oxygen species (ROS) and apoptosis in a dose-dependent manner. Antioxidant agent-20 demonstrates photoprotective effects on UVB-exposed human skin keratinocytes (HaCaT) (IC50=5.13 µM) by activating Nrf2/HO-1 signaling and inhibiting the NF-κB pathway.

Nrf2 activator-10 (Compound AI-1) is a PI3K-dependent antioxidant response element (ARE) inducer, with an EC50 of 2.7 μM, and also acts as an Nrf2 activator. It modifies Keap1, preventing the formation of the Cul3-Keap1 ubiquitin ligase complex, thereby activating Nrf2 transcription. Nrf2 activator-10 provides cellular protection against H2O2-induced apoptosis.

Nrf2-IN-4 is an Nrf2 inhibitor that induces ferroptosis by disrupting cellular iron homeostasis, promoting ferritin degradation, and ultimately triggering ferroptosis. It activates lysosomes through iron-dependent reactive oxygen species (ROS) production and lysosomal acidification. Nrf2-IN-4 demonstrates significant antitumor effects and is applicable in breast cancer research.

Fluvastatin (XU-62320) is a potent and competitive HMG-CoA reductase inhibitor (IC50: 8 nM) that inhibits oxidative stress in vascular smooth muscle cells through an Nrf2-dependent pathway, and is used for the reduction of plasma cholesterol levels and the prevention of cardiovascular disease.

Nrf2-IN-4 (Compound PhcY) hydrobromide is an Nrf2 inhibitor that promotes ferroptosis by inhibiting NRF2. It disrupts cellular iron homeostasis, leading to ferritin degradation and ultimately triggering ferroptosis. Additionally, Nrf2-IN-4 hydrobromide induces lysosomal activation by enhancing iron-dependent reactive oxygen species (ROS) production and lysosomal acidification. This compound shows significant antitumor effects and is applicable in breast cancer research.

KARS-IN-1 (152) is an AKR1C3-dependent KARS inhibitor with an AC50 of 9.1 nM for human KARS. It exhibits antiproliferative activity in both H460 (NRF2 pathway-mutant cell line with high AKR1C3 expression) and Hara (NRF2 pathway wild-type cell line with low AKR1C3 expression), with AC50 values of 21 nM and 16 nM, respectively. KARS-IN-1 is applicable in non-small cell lung cancer (NSCLC) research.

Nrf2-Activator-12G (compd 12g) is a direct activator of Nrf2 that induces robust expression of Nrf2-dependent antioxidant enzymes at both mRNA and protein levels in dopaminergic neuronal cells, thereby enhancing cellular defense against oxidative stress and providing a mechanistic platform for investigating neuroprotection and disease-modifying strategies in Parkinson’s disease research.

Trilobatin (P-Phlorizin) has anti-oxidant effect, can increase superoxide dismutase (SOD) activity.Trilobatin has anti-inflammatory effect, it potentially inhibits the lipopolysaccharide (LPS)-induced inflammatory response by suppressing the NF-κB signaling pathway.Trilobatin shows a strong inhibitory activity against α-glucosidase and a moderate inhibitory activity against α-amylase for management of postprandial hyperglycemia with less side effect.

1. Negletein (7-O-Methylbaicalein) has anti-inflammatory and immunomodulatory activities via inhibition of TNF-α, iNOS and IL-1β. 2. Negletein as a neuroprotectant enhances the action of nerve growth factor and induces neurite outgrowth in PC12 cells. 3. Negletein shows a comparable redox-active potential, and it (50 μM, 4 h) can activate Nrf2. 4. Negletein shows significant antimicrobial activity. 5. Negletein has anti-hypoxia activity, it can significantly prolong the survival time of hypoxic mice.6. Negletein has anti- Alzheimer's disease activity, it inhibits the iron-dependent formation of ROS and also blocks the iron-induced oligomerization of amyloid beta 42 in vitro. 7. Negletein (IC50: 3.89 +/- 0.39 microM) exhibits potent inhibitory activity against nuclear factor of activated T cells (NFAT) transcription factor.

Gypenoside XVII (Gynosaponin S) confers protection against Aβ25-35-induced neurotoxicity through estrogen receptor-dependent activation of PI3K/Akt pathways, activation of Nrf2/ARE/HO-1 and inactivation of GSK-3β pathways.

17-oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-Docosahexaenoic acid is a metabolite of lipoxygenase-mediated oxidation of DHA that is produced endogenously by aspirin-enhanced COX-2 activity. It has been shown to activate Nrf2-dependent antioxidant gene expression, to act as a PPARγ agonist (EC50 = ~200 nM), and to inhibit pro-inflammatory cytokine and nitric oxide production at biological concentration ranges (5-25 μM).

Docosapentaenoic acid (DPA) is a ω-3 fatty acid found in fish oils. 17-oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid is a metabolite of lipoxygenase-mediated oxidation of DPA that is produced endogenously by aspirin-enhanced COX-2 activity. It has been shown to activate Nrf2-dependent antioxidant gene expression, to act as a PPARγ agonist (EC50 = ~200 nM), and to inhibit pro-inflammatory cytokine and nitric oxide production at biological concentration ranges (5-25 μM).

(3R,5S)-Fluvastatin, the 3R,5S-isomer of Fluvastatin (XU 62-320 free acid), stands as the inaugural fully synthetic, competitive inhibitor of HMG-CoA reductase, exhibiting an IC50 value of 8 nM. It safeguards vascular smooth muscle cells from oxidative stress by activating the Nrf2-dependent antioxidant pathway.

1. 5,7-Dihydroxychromone (5,7-Dihydroxy-4H-Chromen-4-One) isolated from DME is one of the active compounds that may contribute to regulate blood glucose levels. 2. 5,7-Dihydroxychromone exerts neuroprotective effect against 6-OHDA-induced oxidative stress and apoptosis by activating Nrf2/ARE signal . 3. 5,7-Dihydroxychromone induces the translocation of Nrf2 to the nucleus and increases Nrf2/ARE binding activity which results in the up-regulation of the expression of Nrf2-dependent antioxidant genes, including HO-1, NQO1, and GCLc.

α-Lipoic Acid sodium (Thioctic acid sodium) is an antioxidant and essential cofactor for mitochondrial enzyme complexes. It inhibits NF-κB-dependent HIV-1 replication, induces endoplasmic reticulum stress-mediated apoptosis in hepatocellular carcinoma cells, and modulates SREBP-1, FOXO1, and Nrf2 to improve high-fat diet-induced hepatic steatosis.

(3R,5S)-Fluvastatin ((3R,5S)-XU 62-320) sodium, a specific isomer of Fluvastatin, functions as a fully synthetic, competitive inhibitor of HMG-CoA reductase, exhibiting an IC50 of 8 nM. It is notable for its efficacy in shielding vascular smooth muscle cells from oxidative stress via the Nrf2-dependent antioxidant pathway [1] [2] [3].'

Fluvastatin (XU 62-320) sodium monohydrate, a fully synthetic competitive HMG-CoA reductase inhibitor, features an IC 50 of 8 nM. This compound also safeguards vascular smooth muscle cells from oxidative stress via the Nrf2-dependent antioxidant pathway [1] [2].

Propoxur-d7 is the deuterium-labeled version of Propoxur. Propoxur serves as a reversible, competitive acetylcholinesterase (AChE) inhibitor that can be administered orally and cross the blood-brain barrier. It inhibits AChE activity, causing neurotoxicity, and simultaneously induces intracellular ROS production, activates the ERK/Nrf2 signaling pathway, promotes MMP-2 expression, and enhances the migration and invasion capabilities of tumor cells. While Propoxur inhibits AChE, leading to acetylcholine accumulation and neural dysfunction, it also facilitates ROS-dependent ERK1/2 phosphorylation, promoting nuclear translocation of Nrf2 and upregulation of invasion-related proteins like MMP-2. Additionally, Propoxur is an insecticide in the carbamate class used for controlling turf, forestry, and household pests.

Trigonelline-d3-1 chloride (Trigonelline-d3-1 hydrochloride) is a deuterium-labeled version of Trigonelline chloride. Trigonelline chloride, an alkaloid with potential antidiabetic properties, can be isolated from fenugreek or motherwort. It serves as an effective Nrf2 inhibitor, capable of blocking Nrf2-dependent proteasome activity, thereby enhancing apoptosis in pancreatic cancer cells. Additionally, Trigonelline chloride exhibits anti-HSV-1, antibacterial, and antifungal activities and can induce ferroptosis.

11-Keto-beta-boswellic acid (Standard) is a reference standard for research and analysis in studies involving 11-Keto-beta-boswellic acid. 11-Keto-beta-boswellic acid, a novel Nrf2 activator, and a selective 5-lipoxygenase (5-LOX) inhibitor; it exerts dose dependent cardioprotective effect manifested by dose-dependent reduction in serum lactate dehydrogenase