Keap1-Nrf2

Loganic acid is an iridoid isolated from cornelian cherry fruits. Loganic acid inhibits NF-κB signaling pathway, activates Nrf2 signaling pathway, exhibits anti-inflammatory activity. Loganic acid can modulate diet-induced atherosclerosis and redox status. Loganic acid has strong free radical scavenging activity and remarkable cyto-protective effect against heavy metal mediated toxicity. Loganic acid is orally active.

Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway. Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM_2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes.

3',4'-Dihydroxyacetophenone (3,4-DHAP) is a phenolic compound with oral bioavailability, possessing potent antioxidant, anti-inflammatory, anticancer and cardiovascular protective activities. 3',4'-Dihydroxyacetophenone inhibits mushroom Tyrosinase activity with an IC₅₀ of 10 μM, thereby suppressing melanogenesis. 3',4'-Dihydroxyacetophenone inhibits platelet aggregation in platelet-rich plasma. 3',4'-Dihydroxyacetophenone reduces ROS levels in human umbilical vein endothelial cells treated with high glucose, upregulates the expression of Nrf2, HO-1 and PARP-1 in cells, and promotes the nuclear translocation of Nrf2. 3',4'-Dihydroxyacetophenone induces autophagy and apoptosis. 3',4'-Dihydroxyacetophenone inhibits seed germination/growth in most plants. 3',4'-Dihydroxyacetophenone can be used in the research of cancer, neurodegenerative diseases, non-alcoholic steatohepatitis, diabetes, obesity, skin pigmentation disorders, and cardiovascular and cerebrovascular diseases.

Gypenoside XLIX is a multifunctional bioactive compound that can be isolated from Gynostemma pentaphyllum, with a K_a value of 1.58 μM for its binding to SIRT1. Gypenoside XLIX acts as a PPAR-α agonist. It inhibits the activation of TLR4-mediated NF-κB signaling pathway by activating the Sirt1/Nrf2 signaling pathway, reduces ROS accumulation, and alleviates hepatic inflammatory injury in mice with sepsis-induced liver disease. Gypenoside XLIX targets SIRT1 to block YAP-NLRP3 activation and improve sepsis-induced cardiomyopathy. Gypenoside XLIX inhibits apoptosis (Apoptosis), pyroptosis (Pyroptosis), autophagy (Autophagy), lipid peroxidation, pro-inflammatory cytokines and anti-inflammatory cytokines. Gypenoside XLIX alleviates sepsis-induced splenic injury by inhibiting inflammation and oxidative stress, and mitigates sepsis-associated encephalopathy by targeting PPAR-α. Gypenoside XLIX prevents acute kidney injury by inhibiting IGFBP7/IGF1R-mediated programmed cell death and inflammation. Gypenoside XLIX inhibits the expression and activity of vascular cell adhesion molecule-1 in cytokine-induced human endothelial cells. Gypenoside XLIX is applicable to research related to acute liver injury, lung injury, cardiomyopathy, acute splenic injury, sepsis-associated encephalopathy, acute kidney injury, atherosclerosis and chronic inflammation.

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.

Epmedin C (Epimedin-C; Baohuoside-VI) is an orally active anti-inflammatory agent and immunomodulator that binds to multiple key proteins including UCP1, Caspase-1, CDK2 and Keap1. Epmedin C inhibits epithelial cell proliferation by disrupting the complex function of CDK2/Cyclin E. Epmedin C also upregulates Nrf2 expression, reduces ROS levels and inhibits pro-inflammatory cytokine secretion, thereby effectively restoring antibody production and alleviating tissue damage. Epmedin C has good safety with no hepatotoxicity or skin sensitization, and it has been used in studies on diseases such as obesity, Deoxynivalenol (HY-N6684)-induced immunotoxicity and mammary hyperplasia.

Moracin N is a benzofuran compound. At low concentrations, Moracin N activates the Keap1/Nrf2 pathway, downregulates the expression of FTH1 and ACSL4, enhances glutathione synthesis, and inhibits neuronal ferroptosis. At high concentrations, Moracin N induces ROS accumulation, activates mitochondrial apoptosis, and triggers autophagy-mediated cell death by inhibiting the AKT/mTOR pathway. Moracin N can be used in research related to non-small cell lung cancer, hepatocellular carcinoma and ischemic brain injury.

Gomisin N is an orally active lignan compound. Gomisin N can be isolated from Schisandra chinensis. Gomisin N induces Apoptosis in a variety of cells. Gomisin N activates AMPK, Akt, MAPK/ERK, Nrf2, caspase-3 and PARP-1. Gomisin N inhibits GSK3β, nitric oxide (NO), and proinflammatory cytokines (IL-1β, IL-6, TNF-α). Gomisin N has anti-inflammatory, antioxidant, anti-obesity, anti-diabetic, and anti-melanogenesis activities. Gomisin N has anti-tumor activity against cervical cancer and liver cancer. Gomisin N improves Alzheimer's disease.

Ezetimibe ketone is an orall active Nrf2 activator and ROS inhibitor. Ezetimibe ketone attenuates H₂O₂-induced reactive oxygen species production and reduces H₂O₂-induced apoptosis in renal tubular epithelial cells. Ezetimibe ketone suppresses renal tubular injury and inflammation.

Rosolutamide (ASC-JM17) is an orally active Nrf1/Nrf2 activator. Rosolutamide activates Hsf1 pathways, upregulates proteasome subunits and antioxidant enzymes, induces proteasome complex structural rearrangement, and enhances ubiquitin-proteasome system-mediated degradation. Rosolutamide reduces mutant androgen receptor and ataxin-3 aggregates, restores mitochondrial function, attenuates reactive oxygen species (ROS) levels, induces apoptosis and ferroptosis, and inhibits cancer cell growth. Rosolutamide can be used for the research of spinal and bulbar muscular atrophy, Huntington’s disease, and temozolomide-resistant glioblastoma.

Clemastine (HS-592; Meclastine) is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation.

Carveol is an orally active monoterpenoid alcohol with neuroprotective, antioxidant, anti-inflammatory, anticonvulsant, antidiabetic, hypolipidemic and hepatoprotective activities. Carveol upregulates the expression of Bcl2, downregulates the expression of caspase-3, TNF-α, IL1β and IL6, activates the Nrf2/HO-1 antioxidant signaling pathway, inhibits the RAGE/NF-κB signaling pathway, and suppresses neuroinflammation and neuronal apoptosis. Carveol inhibits α-synuclein aggregation, improves cognitive ability, and inhibits α-amylase activity. Carveol exerts neuroprotective effects in a rat model of Parkinson's disease. Carveol exhibits antidiabetic effects in alloxan-induced diabetic rats. Carveol alleviates PTZ-induced seizures in rats. Carveol can be used in research related to Parkinson's disease, epilepsy, diabetes and ischemic stroke.

L-Cystine hydrochloride is an orally active extracellular form of L-Cysteine (HY-Y0337), occurring in proteins of plants and animals. L-Cystine hydrochloride elevates Nrf2 protein expression and activates Nrf2 transcription factor. L-Cystine hydrochloride reduces ROS generation and protects against oxidant- or Doxorubicin (HY-15142A)-induced apoptosis. L-Cystine hydrochloride 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 hydrochloride is promising for research of cystinuria and kidney stones

CDDO-EA is an NF-E2 related factor 2/antioxidant response element (Nrf2/ARE) activator.

Garcinone D is an activator of the STAT3/Cyclin D1 and Nrf2/HO-1 pathways, and an inhibitor of CDK2/CyclinE1 (IC₅₀ for CDK2/CyclinE1 is 28.23 μM). Garcinone D promotes neural stem cell proliferation by activating STAT3 phosphorylation and Cyclin D1 expression and enhancing the Nrf2/HO-1 signaling pathway. In addition, Garcinone D blocks the tumor cell cycle by inhibiting CDK2/CyclinE1. Garcinone D can promote the proliferation of C17.2 neural stem cells and inhibit prostate and breast cancer.

Vialinin A (Terrestrin A) is a p-terphenyl compound that can be derived from a Chinese edible mushroom. Vialinin A is an inhibitor of ubiquitin-specific peptidase 4 (USP4) and has anti-inflammatory and antioxidant properties. Vialinin A can alleviate cerebral ischaemia-reperfusion injury-induced neurological deficits and neuronal apoptosis. Vialinin A promotes activation of Keap1-Nrf2-ARE signaling pathway and increases the protein degradation of Keap1. Vialinin A possesses various pharmacological activities in cancer, Kawasaki disease, asthma, and pathological scarring. Vialinin A is a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Vialinin A can be studied in reseach for autoimmune diseases, cancer and ischaemic stroke.

Maackiain (DL-Maackiain) is an orally active multi-target inhibitor with anti-tumor activity and neuroprotective effects. Maackiain activates the AMPK, NLRP3 and Nrf2/HO-1 pathways, and inhibits key targets such as NF-κB, mTOR, MAO-B, NFATc1 and PKCδ, thereby precisely regulating processes including apoptosis, autophagy and pyroptosis. Maackiain also effectively inhibits microglial activation, osteoclast formation, and proliferation and invasion of tumor cells, and protects dopaminergic neurons from damage. Maackiain is applicable to the research of various diseases such as Alzheimer's disease, osteoporosis, sepsis and dengue fever。

Diroximel fumarate (ALKS 8700) is an orally-active and well-tolerated monomethyl fumarate (MMF) proagent in a controlled-release formulation. Diroximel fumarate is considered as active equivalent to its active metabolite dimethyl fumarate (DMF). Diroximel fumarate has a favorable safety and efficacy profile, has the potential for the study of multiple sclerosis (MS). Diroximel fumarate is a Nrf2 activator that alleviate MGO-induced pain hypersensitivity.

L-Methionine (Standard) is the analytical standard of L-Methionine. This product is intended for research and analytical applications. L-Methionine is an L-isomer of orally active Methionine, an essential amino acid. Methionine is a strong liver antidote that acts as a liver protector. L-Methionine can inhibit cell proliferation and induce cell apoptosis. L-Methionine has antitumor and antioxidant activity.

Nrf2 activator-4 (Compound 20a) is a highly potent, orally active Nrf2 activator with an EC₅₀ of 0.63 µM. Nrf2 activator-4 suppresses reactive oxygen species against oxidative stress in microglia. Nrf2 activator-4 effectively recovers the learning and memory impairment in a scopolamine-induced mouse model.