Keap1-Nrf2 Activator

Isoeucommin A is a lignan compound. Isoeucommin A activates the Nrf2/HO-1 pathway and induces phosphorylation of GSK-3β. Isoeucommin A reduces the levels of pro-inflammatory cytokines TNF-α, IL-1β and IL-6, decreases the oxidative stress marker MDA, increases the antioxidants SOD and GSH, and alleviates oxidative stress in mesangial cells. Isoeucommin A alleviates renal tissue injury, improves impaired renal function and enhances the viability of renal tubular epithelial cells in diabetic nephropathy models. Isoeucommin A can be used in the research of diabetic nephropathy.

Propoxue (Standard) is the analytical standard of Propoxue (HY-B0916). This product is intended for research and analytical applications. Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests.

Nrf2 activator 18 (Compound 11a) is an orally active activator for Keap1/Nrf2/HO-1 signaling pathway, that promotes the Nrf2 nuclear translocation, and enhances the antioxidant efficacy. Nrf2 activator 18 inhibits the release of IL-6 with an IC₅₀ of 4.816 μM. Nrf2 activator 18 exhibits anti-inflammatory efficacy in mouse PM2.5-induced lung injury model.

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.

Propoxur-d₇ is the deuterium labeled Propoxur. Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests.

Pulegone-d₈ is deuterated labeled Pulegone (HY-N1500). Pulegone is a monoterpene ketone compound widely present in the essential oils of many plants. Pulegone can also be used as a bird repellent. Pulegone has multiple activities such as anti-inflammatory, antibacterial, antifungal, and anti-hyperalgesic effects. Pulegone is particularly effective against bacteria of the Salmonella species.

Corynoline (Standard) is the analytical standard of Corynoline. This product is intended for research and analytical applications. Corynoline is a reversible and noncompetitive acetylcholinesterase (AChE) inhibitor with an IC₅₀ of 30.6 μM. Corynoline exhibits anti-inflammatory activity by activating Nrf2.

Anti-inflammatory agent 72 (compound 5) is a novel resveratrol derivative hybrid with benzoylhydrazine. Anti-inflammatory agent 72 shows anti-inflammatory and antioxidant activities by activating Nrf2 and inhibiting NF-κB p65/iNOS and MAPKs signaling pathways.

Sesaminol is an orally active activator for Nrf2-ARE pathway, that promotes the the nuclear translocation of Nrf2 and enhances the NQO1 expression, thereby enhances the cell's defense against oxidative stress. Sesaminol inhibits 6-OHDA (HY-B1081)-induced ROS production and apoptosis in cell SH-SY5Y. Sesaminol exhibits neuroprotective efficacy against Rotenone (HY-B1756)-induced Parkinson's disease.

Dibenzoylmethane (Standard) is the analytical standard of Dibenzoylmethane. This product is intended for research and analytical applications. Dibenzoylmethane, a minor ingredient in licorice, activates Nrf2 and prevents various cancers and oxidative damage. Dibenzoylmethane, an analog of curcumin, results in dissociation from Keap1 and nuclear translocation of Nrf2.

Nrf2 activator-21 is a Nrf2 activator with dual antioxidant and neuroprotective properties. Nrf2 activator-21 binds to Keap1 Kelch domain and disrupts Keap1-Nrf2 interactions and activate antioxidant defense mechanisms. Nrf2 activator-21 reduces apoptosis and decreases caspase-3 activity in the hippocampal neurons. Nrf2 activator-21 targets cerebral ischemia/reperfusion injury (CIRI) via Nrf2 pathway activation. Nrf2 activator-21 improves neurological function, alleviates anxiety-like behavior, enhances memory in rats with 2-vessel occlusion (2VO)-induced CIRI. Nrf2 activator-21 can be used for the study of cerebral ischemia/reperfusion injury.

5,7-Dihydroxychromone (Standard) is the analytical standard of 5,7-Dihydroxychromone (HY-N1970). This product is intended for research and analytical applications. 5,7-Dihydroxychromone is a flavonoid compound with antioxidant properties. 5,7-Dihydroxychromone induces Nrf2 nuclear translocation, increases Nrf2/ARE binding activity, and up-regulates Nrf2-dependent antioxidant genes HO-1, NQO1, GCLc. 5,7-Dihydroxychromone attenuates excessive ROS generation, inhibits activated caspase-3, caspase-9, cleaved PARP expression, and prevents neuronal apoptosis and cell death. 5,7-Dihydroxychromone increases LXRα and PPARγ mRNA expression, induces preadipocyte differentiation, and regulates blood glucose levels. 5,7-Dihydroxychromone inhibits radial growth of soil pathogenic fungi, radicle elongation of select seedlings, and transiently inhibits Bradyrhizobium sp. growth in high mannitol medium. 5,7-Dihydroxychromone can be used for the research of Parkinson’s disease, type 2 diabetes mellitus and pathogenic fungal infection.

L-Cystine (dihydrochloride) (Standard) is the analytical standard of L-Cystine (dihydrochloride) (HY-W009203). This product is intended for research and analytical applications. L-Cystine dihydrochloride is the dihydrochloride salt form of L-Cystine (HY-N0394). L-Cystine dihydrochloride elevates Nrf2 protein expression and activates Nrf2 transcription factor. L-cystine dihydrochloride reduces ROS generation and protects against oxidant- or Doxorubicin (HY-15142A)-induced apoptosis. L-Cystine dihydrochloride combined with L-theanine (HY-15121) enhances the production of antigen-specific IgG by increasing glutathione (GSH) levels and T helper 2 (Th2) mediated responses in mice. L-Cystine dihydrochloride is promising for research of cystinuria and kidney stones

Dyclonine hydrochloride (Standard) (Dyclocaine hydrochloride (Standard)) is the analytical standard of Dyclonine hydrochloride (HY-B0364A). This product is intended for research and analytical applications. Dyclonine hydrochloride (Dyclocaine hydrochloride) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine hydrochloride acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine hydrochloride activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine hydrochloride alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine hydrochloride can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis.

Methylnissolin-3-O-glucoside (Standard) is the analytical standard of Methylnissolin-3-O-glucoside (HY-N2473). This product is intended for research and analytical applications. Methylnissolin-3-O-glucoside is a flavonoid glycoside derivative of Methylnissolin (HY-N2484). Methylnissolin-3-O-glucoside is isolated from plants of the genus Astragalus (Leguminosae). Methylnissolin-3-O-glucoside effectively induces the expression of AKT/Nrf2 and its downstream target genes HO-1 and NQO1. Methylnissolin-3-O-glucoside inhibits TNF-α-induced phosphorylation of MEK and ERK. Methylnissolin-3-O-glucoside exhibits free radical scavenging activity. Methylnissolin-3-O-glucoside inhibits cell proliferation and cell migration. Methylnissolin-3-O-glucoside is used in research on esophageal squamous cell carcinoma.

NFE2L2 activator 3 (Compound 3) is a NFE2L2/NRF2 activator. NFE2L2 activator 3 specifically activates the NAD(P)H:quinone oxidoreductase (NQO1) enzyme, with its EC₅₀ < 1 nM. NFE2L2 activator 3 can be used for research on respiratory system diseases such as chronic obstructive pulmonary disease.

Monotropein (Standard) is the analytical standard of Monotropein. This product is intended for research and analytical applications. Monotropein is an iridoid glycoside that can be isolated from the roots of Morinda officinalis. Monotropein inhibits the expression of inflammatory mediators in dextran sulfate sodium (DSS)-induced colitis mouse model. Monotropein exerts protective effects against IL-1β-induced apoptosis and catabolic responses on osteoarthritis chondrocytes. Monotropein has cartilage protective activity. Monotropein can alleviate Cisplatin (HY-17394)-induced acute kidney injury by inhibiting oxidative damage, inflammation and apoptosis through activation of Nrf2/HO-1 pathway and inhibition of NF-κB signaling. Monotropein can be studied in research for osteoarthritis, acute kidney injury and acute lung injury.

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.

Lithospermic acid (Standard) is the analytical standard of Lithospermic acid. This product is intended for research and analytical applications. Lithospermic acid ((+)-Lithospermic acid) is a plant-derived polycyclic phenolic carboxylic acid isolated from Salvia miltiorrhiza, and has the anti-oxidative and hepatoprotective activity on carbon tetrachloride (CCl4)-induced acute liver damage in vitro and in vivo.

ML334 (Standard) is the analytical standard of ML334 (HY-110258). This product is intended for research and analytical applications. ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a K_d of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity.