nrf2 in 1

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/HO-1 Activator 3 (Compound C3a) is an activator of the Nrf2 signaling pathway that facilitates the translocation of Nrf2 into the nucleus and enhances the expression of heme oxygenase-1 (HO-1). In H9c2 cardiomyocytes subjected to H2O2 or high glucose stimulation, Nrf2/HO-1 Activator 3 inhibits the excessive expression of ROS and MDA, suppressing cell viability and colony formation, thereby exhibiting antioxidant activity.

Nrf2/HO-1 activator 1 (Compound 24) is a potent neuroprotective and antioxidant agent targeting Nrf2/HO-1, with significant potential for therapeutic applications in Parkinson's disease (PD) research [1].

Nrf2/HO-1 activator 2 (compound 13m), a difluoro-substituted derivative, is a highly potent activator of Nrf2/HO-1 with substantial neuroprotective and antioxidant properties. It functions by activating the Nrf2/HO-1 pathway through the phosphorylation of ERK1/2, JNK, or Akt in PC12 cells and is useful in investigating Parkinson's disease (PD) [1].

AChE/Nrf2 modulator 1, an orally active compound, serves as a modulator of acetylcholinesterase (AChE) and nuclear factor erythroid 2-related factor 2 (Nrf2). It exhibits Nrf2 inductive activity alongside inhibitory effects on eeAChE and hAChE, demonstrating IC 50 values of 0.07 μM and 0.38 μM, respectively. This compound is applicable in Alzheimer's disease research.

Nrf2/HO-1-IN-1 is a potent Nrf2/HO-1 pathway inhibitor, with an IC 50 value of 0.38 μM for NO . Nrf2/HO-1-IN-1 can significantly reduce the level of ROS in cells. Nrf2/HO-1-IN-1 can be used for researching anti-inflammatory .

Keap1/Nrf2/ARE activator 1 (compound HT-3) functions as an activator of the Keap1/Nrf2/ARE pathway. This compound has antioxidant properties and offers neuroprotective effects.

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.

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].

Keap1-Nrf2-IN-1 TFA (compound35) is a Keap1-Nrf2 protein-protein interaction inhibitor (IC50: 43 nM) that activates Nrf2-regulated cytoprotective responses and antagonizes acetaminophen-induced liver injury in both cellular and in vivo models.

Keap1-Nrf2-IN-11 (Compound 6k), a potent Keap1-Nrf2 inhibitor, exhibits a dissociation constant (KD) of 0.21 nM. It hampers the production of reactive oxygen species (ROS) and nitric oxide (NO), as well as the expression of tumor necrosis factor-alpha (TNF-α). By promoting Nrf2 nuclear translocation, it mitigates inflammation and is utilized in anti-inflammatory studies [1].

Keap1-Nrf2-IN-15 (Compound 24a) is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction, with IC50 values of 77 nM in a fluorescence polarization (FP) assay and 2.5 nM in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay [1].

Keap1-Nrf2-IN-10 (compound 15) is a potent inducer of NQO1 that effectively mitigates oxidative stress in gamma-irradiated mice by reducing MDA and ROS levels, and NQO1 in the liver, thereby enhancing survival rates [1].

Keap1-Nrf2-IN-17 (compound 18) is a potent inhibitor of the protein-protein interaction between Keap1 and Nrf2.

Keap1-Nrf2-IN-18 (Compound 22) is an orally active inhibitor of the Keap1-Nrf2 protein-protein interaction (PPI), demonstrating favorable pharmacokinetic (PK) properties and enhanced in vivo efficacy in rats. In structure-activity relationship (SAR) studies, Keap1-Nrf2-IN-18 exhibits the strongest inhibitory activity (KD = 0.0029 μM).

Keap1-Nrf2-IN-19 (compound 33) is an orally active inhibitor of the Keap1-Nrf2 protein-protein interaction (PPI), with a Kd value of 0.0014 μM. Keap1-Nrf2-IN-19 exhibits less than 50% inhibition of hERG at 30 μM and CYPs at 10 μM.

Keap1-Nrf2-IN-14 is a KEAP1-NRF2 inhibitor that effectively disrupts the KEAP1-NRF2 interaction (IC50: 75 nM) with a Kd=24 nM for KEAP1. Keap1-Nrf2-IN-14 induces the expression of NRF2 target genes and is able to enhance downstream antioxidant and anti-inflammatory effects. -Nrf2-IN-14 can be used to study oxidative stress-related inflammation.

eap1-Nrf2-IN-12 is a potent inhibitor of Keap1-Nrf2 (IC50: 2.30 μM). eap1-Nrf2-IN-12 is metabolically stable in human liver microsomes.

Keap1-Nrf2-IN-13 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction (PPI) with an IC50 value of 0.15 μM, indicating high efficacy. It binds strongly to Keap1 by forming hydrogen bonds with critical polar residues (Asn414, Arg415, Arg483, Gln530), showcasing specificity. This compound has implications for research into diseases associated with oxidative stress and inflammation, such as pulmonary fibrosis, chronic obstructive pulmonary disease (COPD), and cancers, due to its mechanism of action.

Keap1-Nrf2-IN-16 is a biologically active peptide with KEAP1 binding activity.

VVD-130037 is a small molecule activator specifically targeting Kelch-like ECH-associated protein 1 (KEAP1) with potential antitumor activity.VVD-130037 inhibits tumor growth in advanced solid tumors by degrading NRF2.

DCG066 is an inhibitor of lysine methyltransferase G9a with anticancer activity.DCG066 inhibits the proliferation of MM cells and induces iron death through the Nrf2/HO-1 pathway and can be used in the study of leukemias.

Oltipraz (RP 35972) is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties. Oltipraz induces phase II detoxification enzymes, such as glutathione S transferase (GST) and NAD(P)H: quinone oxidoreductase 1 (NQO1). The induction of detoxification enzymes enhances the detoxification of certain cancer-causing agents, thereby enhancing their elimination and preventing carcinogen-induced DNA damages. Although the exact mechanism through which the anti-angiogenesis effect remains to be fully elucidated, oltipraz maybe able to modulate the expression of a number of angiogenic factors, thereby blocking the sustained and focal neovascularization in multiple tumor cell types.

1. Linalool (Linalol), a natural compound of the essential oils, has been shown to have antinociceptive, antimicrobial, and anti-inflammatory properties. 2. Linalool was protected against LPS/GalN-induced liver injury through induction of antioxidant defense via Nrf2 activating and reduction inflammatory response via NF-κB inhibition. 3. Linalool biosynthesis and accumulation might be involved in plant defense against bacterial and fungal pathogens and be associated with field resistance to citrus canker. 4. Linalool significantly increased the expression of antioxidant enzymes regulated by Nrf-2 and diminished lung tissue levels of several pro-inflammatory cytokines, including tumor necrosis factor α (TNF-α) and interleukin (IL)-6.