Keap1-Nrf2 Inducer

Co(III) protoporphyrin IX chloride (Protoporphyrin IX cobaltic chloride) is an inducer of HO-1. Co(III) protoporphyrin IX chloride has activities such as anti-inflammation and antibacterial properties. Co(III) protoporphyrin IX chloride can also be used in the research of ischemia-reperfusion injury models.

Diethyl fumarate is a Nrf2 inducer. Diethyl fumarate induces non-immunological contact urticaria, causing erythema, edema, and dose-dependent skin responses characterized by rapid onset, peak response, and subsequent resolution. The hybrid of Diethyl fumarate and Curcumin (HY-N0005) exerts neuroprotective effects. Diethyl fumarate can be used in the research of Parkinson's disease and non-immunological contact urticaria.

Moringa Extract is the extract of Moringa with antioxidative and antibacterial activity. Moringa Extract increases Nrf2 and NQO1 expression, scavenges radicals, reduces oxidative stress, inhibits growth of Staphylococcus aureus and Escherichia coli. Moringa Extract can be used for the research of dietary supplements, cosmetics, and natural water purification.

Tigloylgomisin H is a lignan isolated from the fruits of S. chinensis, can induce quinone reductase (QR) activity in Hepa1c1c7 mouse hepatocarcinoma cells. Tigloylgomisin H functions as a monofunctional inducer that specifically upregulates phase II detoxification enzyme NQO1 through the NF-E2-related factor 2 (Nrf2)-ARE pathway, thus represents a potential liver cancer prevention agent.

MAO-B-IN-39 (compound11) is a selective monoamine oxidase B (MAO-B) inhibitor. MAO-B-IN-39 inhibits MAO-Bwith an IC₅₀ of 3.61 μM. MAO-B-IN-39 demonstrates a potent NRF2 induction capacity. MAO-B-IN-39 exhibits potent anti-inflammatory and neuroprotective activity in OS (oxidative stress)-related in vitro models. MAO-B-IN-39 demonstrates high liver microsomal stability and favorable pharmacokinetics in mice. MAO-B-IN-39 is potential for Parkinson’s disease (PD) research.

Aβ-IN-6 reduces pro-inflammatory cytokine release from microglia cells. Aβ-IN-6 significantly induces Nrf2 nuclear translocation and hamperes Aβ oligomers formation. Aβ-IN-6 exerts a consistent neuroprotective effect by modulating the redox-sensitive signalling pathways in vivo oxidative stress model. Aβ-IN-6 is an orally active and has antiinflammatory, Antioxidant and Anti-oligomeric activity. Aβ-IN-6 has the potential for Alzheimer's disease (AD) research.

Bakkenolide B is isolated from petasites japonicas leaves and has anti-allergic and anti-inflammatory effects. Bakkenolide B can be used for the study of asthma.

D-Leucine amide-CDDO-Me-HMP is a prodrug composed of CDDO-Me (HY-13324) and ligustrazine (HY-N0264). D-Leucine amide-CDDO-Me-HMP can protect against CCl₄-induced liver injury. D-Leucine amide-CDDO-Me-HMP can inhibit ROS production, alleviates mitochondrial damage and inhibits cell apoptosis. D-Leucine amide-CDDO-Me-HMP can be used for the research of liver injury.

DI-1548 is a potent, selective, and irreversible covalent inhibitor of DCN1 (IC₅₀ = 4.6 nM). DI-1548 potently and selectively inhibits cullin 3 neddylation at nanomolar concentrations, and exhibits no obvious effect on the neddylation of other cullin members (including cullin 1, 2, 4A, 4B, and 5). DI-1548 exhibits no cytotoxicity. DI-1548 covalently binds to DCN1, disrupting the DCN1-UBC12 interaction, causing the collapse of the neddylation complex, inactivating CRL3, leading to NRF2 accumulation and upregulation of its target genes, and ultimately protecting mice from liver damage. DI-1548 can be used in liver injury research.

ALR2-IN-9 is a potent ALR2 inhibitor (IC₅₀ = 21.8 nM) with excellent antioxidant activity (EC₅₀ for DPPH radical scavenging = 2.8 μM). ALR2-IN-9 interacts directly with Reactive Oxygen Species (ROS)/Reactive Nitrogen Species (RNS) and interrupts the free radical chain reactions, and as an endogenous enzymatic antioxidant regulator, which regulates enzyme functions of CAT and SOD. ALR2-IN-9 regulates PI3K/Akt/Nrf2 pathway to attenuate hyperglycemia-mediated mitochondrial superoxide overproduction in vitro, and ameliorates CuSO₄- and H₂O₂-induced oxidative stress in vivo. ALR2-IN-9 prolongs lifespan of C. elegans via the regulation of stress response genes such as PMK-1. ALR2-IN-9 is a promising anti-aging drug candidate. ALR2-IN-9 can be used for diabetic complication research.