2. Signaling Pathways
  3. NF-κB
  4. Keap1-Nrf2
  5. Keap1-Nrf2 Inhibitor

Keap1-Nrf2 Inhibitor

Keap1-Nrf2 Inhibitors (45):

Cat. No. Product Name Effect Purity
  • HY-100523
    ML385
    		Inhibitor 99.96%
    ML385 is a specific nuclear factor erythroid 2-related factor 2 (NRF2) inhibitor with an IC50 of 1.9 μM.
  • HY-169201
    Nrf2 activator-12
    		Inhibitor 98.57%
    Nrf2 activator-12 (compund 10v) potently activates Nrf2 (EC50=83.5 nM) and exhibits promising pharmacological properties, reversing disease progression and alleviating demyelination in an experimental autoimmune encephalomyelitis mouse model.
  • HY-N0162
    Luteolin
    		Inhibitor 99.51%
    Luteolin (Luteoline), a flavanoid compound, is a potent Nrf2 inhibitor. Luteolin has anti-inflammatory, anti-cancer properties, including the induction of apoptosis and cell cycle arrest, and the inhibition of metastasis and angiogenesis, in several cancer cell lines, including human non-small lung cancer cells.
  • HY-19543
    Brusatol
    		Inhibitor 99.89%
    Brusatol (NSC?172924) is a unique inhibitor of the Nrf2 pathway that sensitizes a broad spectrum of cancer cells to Cisplatin and other chemotherapeutic agents. Brusatol enhances the efficacy of chemotherapy by inhibiting the Nrf2-mediated defense mechanism. Brusatol can be developed into an adjuvant chemotherapeutic agent. Brusatol increases cellular apoptosis.
  • HY-N1914
    Ergothioneine
    		Inhibitor 99.99%
    Ergothioneine is an imidazole-2-thione derivative with orally active histidine betaine. Ergothioneine is a specific inhibitor of p38-MAPK and Akt, which plays a protective role in cell apoptosis induced by stress. Ergothioneine has antioxidant activity.
  • HY-101140
    KI696
    		Inhibitor 99.26%
    KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction. KI696 is a potent and selective inhibitor of the KEAP1/NRF2 interaction.
  • HY-B2230
    Hinokitiol
    		Inhibitor 99.83%
    Hinokitiol is a component of essential oils isolated from Chymacyparis obtusa, reduces Nrf2 expression, and decreases DNMT1 and UHRF1 mRNA and protein expression, with anti-infective, anti-oxidative, and anti-tumor activities.
  • HY-101025
    Nrf2-IN-1
    		Inhibitor 99.78%
    Nrf2-IN-1 is an inhibitor of nuclear factor-erythroid 2-related factor 2 (Nrf2). Nrf2-IN-1 is developed for the research of acute myeloid leukemia (AML).
  • HY-N0162R
    Luteolin (Standard)
    		Inhibitor 98.71%
    Luteolin (Standard) is the analytical standard of Luteolin. This product is intended for research and analytical applications. Luteolin (Luteoline), a flavanoid compound, is a potent Nrf2 inhibitor. Luteolin has anti-inflammatory, anti-cancer properties, including the induction of apoptosis and cell cycle arrest, and the inhibition of metastasis and angiogenesis, in several cancer cell lines, including human non-small lung cancer cells.
  • HY-N4118
    Cephaeline
    		Inhibitor 98.94%
    Cephaeline ((-)-Cephaeline), a desmethyl analog of Emetine, is a phenolic alkaloid in Indian Ipecac roots isolated from the Cephaelis ipecacuanha. Cephaeline exhibits potent inhibition of both Zika virus (ZIKV) and Ebola virus (EBOV) infections. Cephaeline is an inductor of histone H3 acetylation and an inhibitor of mucoepidermoid carcinoma cancer stem cells (MEC), which promotes ferroptosis by inhibiting NRF2 to exert anti-lung cancer efficacy.
  • HY-113848
    AEM1
    		Inhibitor 98.99%
    AEM1 is an Nrf2 inhibitor with anti-tumor and oral activity. AEM1 promotes the differentiation of HepaRG cells towards mature liver cells, aiding in the recovery of damaged liver.
  • HY-N3075
    Phytol
    		Inhibitor 98.93%
    Phytol ((E)-Phytol) is an orally active diterpenoid alcohol that can be extracted from chlorophyll. Phytol has antioxidant, anti-inflammatory, anti-schistosomiasis and antibacterial activities.
  • HY-131592
    Tricetin
    		Inhibitor 99.19%
    Tricetin is a potent competitive inhibitor of the Keap1-Nrf2 Protein Protein Interaction (PPI). Tricetin protects against 6-OHDA-induced neurotoxicity in Parkinson's disease model by activating Nrf2/HO-1 signaling pathway and preventing mitochondria-dependent apoptosis pathway.
  • HY-149508
    Nrf2-IN-3
    		Inhibitor 99.19%
    Nrf2-IN-3 (Compound R16) is a small-molecule NRF2 inhibitor and increases reactive oxygen species (ROS) production. Nrf2-IN-3 selectively binds KEAP1 mutants and restores their NRF2-inhibitory function by repairing the disrupted KEAP1/NRF2 interactions, leading to proteasome-dependent NRF2 degradation in cells. Nrf2-IN-3 sensitizes KEAP1-mutated tumor cells to Cisplatin (HY-17394),Gefitinib (HY-50895), and KEAP1 G333C-mutated xenograft to Cisplatin .
  • HY-N0818
    Chikusetsusaponin Iva
    		Inhibitor 98.95%
    Chikusetsusaponin Iva is the main active component of triterpenoid saponins, acts as an activator of protein kinases, and has a resistance effect against thrombosis and some metabolic diseases.
  • HY-101140A
    KI696 isomer
    		Inhibitor 99.32%
    KI696 isomer is the less active isomer of KI696 (HY-101140). KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction.
  • HY-N7617
    Toralactone
    		Inhibitor 98.75%
    Toralactone, isolated from Cassia obtusifolia, mediates hepatoprotection via an Nrf2-dependent anti-oxidative mechanism.
  • HY-149010
    NXPZ-2
    		Inhibitor
    NXPZ-2 is an orally active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with a Ki value of 95 nM, EC50 value of 120 and 170 nM. NXPZ-2 can dose-dependently ameliorate Aβ[1-42]-Induced cognitive dysfunction, improve brain tissue pathological changes in Alzheimer’s disease (AD) mouse by increasing neuron quantity and function. NXPZ-2 can inhibit oxidative stress by increasing Nrf2 expression levels and promoting its cytoplasm to nuclear translocation, which is helpful for Keap1-Nrf2 PPI inhibitors and AD associated disease research.
  • HY-N4028
    Hydrangenol
    		Inhibitor 99.62%
    Hydrangenol is an orally active antiphotoaging compound. It can be isolated from Hydrangea serrata leaves. Hydrangenol prevents wrinkle formation by reducing MMP and inflammatory cytokine expression and increasing moisturizing factors and antioxidant genes level.
  • HY-150579
    Keap1-Nrf2-IN-13
    		Inhibitor
    Keap1-Nrf2-IN-13 is a Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with an IC50 value of 0.15 μM. Keap1-Nrf2-IN-13 has strong binding affinities to the Keap1 protein by forming hydrogen bond with the key polar residues (Asn414, Arg415, Arg483, Gln530). Keap1-Nrf2-IN-13 can be used in the research of oxidative stress-related and inflammatory diseases, including pulmonary fibrosis, chronic obstructive pulmonary disorder (COPD) and cancers.