nrf2in1

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).

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

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].