nrf2

Nrf2 activator-3 is a potent Nrf2 activator with potential anti-inflammatory, antioxidant, and anti-tumor activities, suitable for studying neurological and immune-related diseases.

Nrf2-IN-3 is a mKEAP1-selective NRF2 inhibitor that selectively binds KEAP1 mutants and restores their NRF2 inhibitory function by repairing the disrupted KEAP1 NRF2 interaction, and selectively sensitizes cisplatin in xenografts of mouse mKEAP1 cancer cells.

Nrf2 activator-4 is an Nrf2 activator that inhibits the production of reactive oxygen species in microglia for the treatment of fatty liver disease associated with metabolic dysfunction in humans.

Omaveloxolone (RTA-408) (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.

2-tert-Butyl-1,4-benzoquinone (TBQ), an electrophilic metabolite of butylated hydroxyanisole (BHA), activates Nrf2 and S-arylates its negative regulator Keap1 in RAW264.7 cells.

Bardoxolone (CDDO) is a synthetic oleanane triterpenoid that blocks the cellular synthesis of inducible nitric oxide synthase and inducible COX-2 in INF-γ-activated mouse macrophages with an IC50 value of 0.4 nM. By suppressing reactive oxygen and nitrogen species (ROS RNS) formation, it promotes the cellular control of ROS RNS levels that would lead to DNA damage associated with tumorigenesis. In various Y cell lines, Bardoxolone has been shown to specifically inhibit proliferation and induce apoptosis. Mechanism studies revealed that Bardoxolone is a ligand for peroxisome proliferator-activated receptor γ, and also that it induces genes regulated by Nrf2, including heme oxygenase-1 and eotaxin-1, which play a role in antioxidant response element signaling activity.

Nrf2-ARE hMAO-B QR2 modulator 1, a resveratrol derivative and multi-target-directed ligand (mtdl), activated the NRF2-ARE pathway (CD = 9.83 μM), selectively inhibited hMAO-B and QR2（quinone reductase-2，NQO2) (IC 50 = 8.05 and 0.57 μM), and was able to promote hippocampal neurogenesis and exert neuroprotective and antioxidant effects in an Alzheimer's disease model.

Gingerenone A is an effective Nrf2-Gpx4 activator. It is a small molecule compound isolated from ginger. It has anti-cancer activity, can prolong the cell cycle of cancer cells, and can inhibit dextran sodium sulfate (DSS)-induced colitis. Ferroptosis in secondary liver injury (SLI) in mice.

AEM1 is an inhibitor of deregulated NRF2 transcriptional activity in cancer. AEM1 acts by broadly decreasing the expression of NRF2 controlled genes, sensitizing A549 cells to various chemotherapeutic agents, and inhibiting the growth of A549 cells in vitro and in vivo.

Ginsenoside Rh3 is a natural product extracted from Ginseng C. A. Mey.Ginsenoside Rh3 has antifungal and antioxidant activities and induces Nrf2 activation in human retinal cells.

Eupatolide is isolated from the flowers of Inula japonica with anti-inflammatory activity. Eupatolide can be used in studies about TRAIL resistance in breast cancer cells.

Nrf2-IN-1 is an nuclear factor-erythroid 2-related factor 2 (Nrf2) inhibitor. Nrf2-IN-1 is developed for the research of acute myeloid leukemia (AML).

Nrf2 degrader 30 is a small molecule PROTAC that inhibits the degradation of Nrf2, thereby enhancing its activity. Nrf2 is a key transcription factor that regulates cellular antioxidant responses and various protective mechanisms. The activity of Nrf2 is primarily regulated by its interaction with Keap1, which serves as an E3 ubiquitin ligase complex adapter to promote Nrf2 ubiquitination and proteasomal degradation。

DDO-7263 is a 1,2,4-Oxadiazole derivative that upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 is a potent Nrf2 activator that activates the Nrf2-ARE signaling pathway and exerts anti-inflammatory activity [1].

Nrf2 activator-1 is a potent activator of NF-E2-related factor 2 (Nrf2) and can be used to study COPD and other respiratory diseases, including asthma, acute lung injury (ALI), acute respiratory distress syndrome (ARDS), and pulmonary fibrosis.

Hesperin (6-MSITC), a flavonoid isolated from orange peel, is a circadian decapping enzyme in plants, inhibiting lipid accumulation and production of reactive oxygen and nitrogen species in 3T3-L1 and RAW264.7 cells.

Zederone is a natural sesquiterpene that modulates inflammatory response, smooth muscle relaxation and endocrinology to treat dysmenorrhea; down-regulates mRNA levels of mTOR and p70s6K to inhibit the proliferation of ovarian cancer cells, and interacts with hypoglycemic proteins 3L4Y and 5UBA to be anti-diabetic and anti-oxidant.

Nrf2-Activator-12G is a potent Nrf-2 activator.

Nrf2 degrader 1 (compound 1), a PROTAC Nrf2 degrader, exhibits anticancer properties by inhibiting the growth of cancer cells. It demonstrates IC 50 values of 100 nM for A549 cells and 40 nM for LK-2 cells, indicating potent efficacy [1].

Nrf2 activator-9 (compound D-36) is an agent that mitigates oxidative stress by inhibiting the apoptosis of HUVEC cells induced by oxidized low-density lipoprotein (oxLDL) and high glucose (HG), also protecting vascular endothelial cells (VEC) from oxLDL and HG-induced injury, offering potential therapeutic benefits for atherosclerosis prevention and treatment [1].

Keap1-Nrf2-IN-23 (compound 56) acts as an inhibitor of the Keap1–Nrf2 PPI (IC50=16.0 nM). It exhibits a Kd value of 3.07 nM when binding to Keap1 and demonstrates oral activity.

Nrf2 activator 18 (Compound 11a) is an orally active activator of the Keap1 Nrf2 HO-1 signaling pathway, promoting Nrf2 nuclear translocation and enhancing antioxidant effects. It inhibits IL-6 release with an IC50 of 4.816 μM. In a mouse model of PM2.5-induced lung injury, Nrf2 activator 18 demonstrates anti-inflammatory activity.

Keap1-Nrf2-IN-25 (Compound 19) is a potent Keap1-Nrf2 inhibitor with an IC50 of 0.55 μM and exhibits a Keap1 binding affinity (Kd of 0.50 μM). This compound activates Nrf2, reducing reactive oxygen species (ROS) and pro-inflammatory cytokines (IL-1β, IL-6). Additionally, Keap1-Nrf2-IN-25 provides protective effects against DSS-induced colitis.

Nrf2 activator-5 is a potent activator of Nrf2 that attenuates H2O2-induced oxidative stress and LPS-stimulated inflammation in BV-2 microglia, exhibiting antioxidant and anti-inflammatory activity.