keap1-nrf2

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

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

Dimethyl fumarate (DMF) is an Nrf2 activator with oral activity and blood-brain barrier permeability. Dimethyl fumarate has antimicrobial, anti-inflammatory, and immunomodulatory activities and has been used in the study of multiple sclerosis.

Luteolin (Luteolol) belongs to the flavonoid group of natural products and is a Nrf2 inhibitor, PDE inhibitor. Luteolin has a wide range of biological activities including antitumor, antioxidant, anti-inflammatory, antimicrobial, antiviral, antiallergic, and procoagulant.

Methyl 3,4-dihydroxybenzoate (Protocatechuic acid methyl ester), a key metabolite of antioxidant polyphenols in green tea, exhibits significant antioxidant and anti-inflammatory properties.

Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300 CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.

Danshensu (Dan shen suan A) is an active ingredient of *Salvia miltiorrhiza* with extensive cardiovascular benefits.

4-hydroxyphenylacetic acid (parahydroxy phenylacetate) is a major microbiota-derived metabolite of polyphenols. 4-hydroxyphenylacetic acid(p-Hydroxyphenylacetic acid) is involved in the antioxidative action. 4-hydroxyphenylacetic acid(p-Hydroxyphenylacetic acid) induces expression of Nrf2.

4-Octyl Itaconate, a cell-permeable derivative of Itaconate, is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1 and inhibits phosphorylation of STING.

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.

1. Eriodictyol (Huazhongilexone) is a flavonoid with anti-inflammatory and antioxidant activities. 2. Eriodictyol may possess antidiabetic properties through increasing glucose uptake and improving insulin resistance. 3. Eriodictyol may be a potential therapeutic resource for Atopic dermatitis and an adjunctive agent to control itchiness inAtopic dermatitis.

ML334 (LH601A) is a transmembrane and potent NRF2 activator that inhibits Keap1-NRF2 protein interactions to ameliorate myocardial infarction-induced cardiac fibrosis by inhibiting cardiac fibroblast activation and proliferation.

K67 competitively inhibits the interaction between Nrf2-ETGE and Keap1, inhibits the proliferation of HCC cells with high expression of S351 phosphorylated p62, and can be used to study cancer.

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.

(R)-Sulforaphane (L-Sulforaphane) is a potent inducer of the Keap1 Nrf2 ARE pathway.

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.

Garcinone D shows significant cytotoxicity against the CEM-SS cell line, with IC(50) value of 3.2 microg ml; it exhibits dose-dependent enzyme-based microsomal aromatase inhibitory activity. Garcinone D inhibits p65 activation with IC50 values of 3.2 micr

Sulforaphane is a natural isothiocyanate that activates Nrf2 and inhibits AMPK-dependent signaling. Sulforaphane has antitumor and anti-inflammatory activities by increasing the transcription of tumor suppressor proteins and inhibiting histone deacetylase activity.

Keap1-Nrf2-IN-22 (compound 19) acts as a Keap1-Nrf2 inhibitor with a KD2 value of 42.2 nM. It is utilized in research focused on acute lung injury (ALI) and cerebral ischemia reperfusion (I R) injuries.

Keap1-Nrf2-IN-24 (compound 57) is an effective Keap1-Nrf2 inhibitor with a Ki value of 13 nM. This compound enhances the protein expression of TRXR1 and NQO1, as well as the mRNA expression of AKR1B10. Additionally, Keap1-Nrf2-IN-24 demonstrates good metabolic stability.

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.

KEAP1-NRF2PPI-IN-1 (compound 23) is an inhibitor targeting the KEAP1-NRF2 interaction. In DNA damage tests, its IC50 values are 136 nM in human TK6 cell lines and 62 nM in insect SF9 cell lines.

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.

Keap1-Nrf2-IN-3 is a KEAP1:NRF2 protein-protein interaction inhibitor with a Kd value of 2.5 nM for the KEAP1 protein.