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

Keap1-Nrf2 Inhibitor

Keap1-Nrf2 Inhibitors (34):

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-157929
    Keap1-Nrf2-IN-19
    		Inhibitor
    Keap1-Nrf2-IN-19 (compound 33) is an oral active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with the Kd value of 0.0014 μM. Keap1-Nrf2-IN-19 exhibits less than 50% inhibition at 30 μM against hERG and 10 μM against CYPs.
  • HY-N0162
    Luteolin
    		Inhibitor 99.01%
    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-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 98.97%
    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-N3075
    Phytol
    		Inhibitor ≥98.0%
    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-113848
    AEM1
    		Inhibitor 98.99%
    AEM1 is a Nrf2 inhibitor. AEM1 reduces the expressions of Nrf2-dependent genes in A549 cells and inhibits the growth of A549 cells in vitro and in vivo.
  • 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-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-N7617
    Toralactone
    		Inhibitor 98.75%
    Toralactone, isolated from Cassia obtusifolia, mediates hepatoprotection via an Nrf2-dependent anti-oxidative mechanism.
  • HY-N0162R
    Luteolin (Standard)
    		Inhibitor 98.72%
    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-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-144635
    Nrf2-ARE/hMAO-B/QR2 modulator 1
    		Inhibitor 98.44%
    Nrf2-ARE/hMAO-B/QR2 modulator 1 is a Resveratrol-based multitarget-directed ligands with IC50s of 8.05, 9.83 and 0.57 μM for hMAO-B, NRF2 and QR2. Nrf2-ARE/hMAO-B/QR2 modulator 1 has neuroprotection, decreasing ROS production in okadaic acid-treated mice hippocampal slices.
  • HY-N4028
    Hydrangenol
    		Inhibitor
    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-147517
    Keap1-Nrf2-IN-9
    		Inhibitor
    Keap1-Nrf2-IN-9 (compound 11) is a potent Keap1-Nrf2 PPI (Keap1-Nrf2 protein−protein interaction) inhibitor with an IC50 of 0.575 µM. Keap1-Nrf2-IN-9 increases the expression of Nrf2 target genes including heme oxygenase 1 (Hmox1), glutathione S-transferase P (GstP), and glutamate-cysteine ligase catalytic (Gclc) and modulatory (Gclm) subunits. Keap1-Nrf2-IN-9 shows not cytotoxic activity in ARPE19 cells.
  • HY-146577
    Keap1-Nrf2-IN-7
    		Inhibitor
    Keap1-Nrf2-IN-7 (compound 7v) is a potent Keap1-Nrf2 PPI (Keap1-Nrf2 protein−protein interaction) inhibitor with an IC50 of 0.45 µM.
  • HY-139862
    Keap1-Nrf2-IN-3
    		Inhibitor
    Keap1-Nrf2-IN-3 is a KEAP1:NRF2 protein−protein interaction inhibitor, and with a Kd value of 2.5 nM for KEAP1 protein.
  • HY-143892
    Keap1-Nrf2-IN-5
    		Inhibitor
    Keap1-Nrf2-IN-5 (compound 1) is a potent Keap1-Nrf2 PPI (Keap1-Nrf2 protein−protein interaction) inhibitor with an IC50 of 4.1 µM, Kd of 3.7 µM.
  • HY-157928
    Keap1-Nrf2-IN-18
    		Inhibitor
    Keap1-Nrf2-IN-18 (Compound 22) is an orally active Keap1-Nrf2 protein-protein interaction (PPI) inhibitor with good pharmacokinetics (PK) profiles and more potent in vivo activities in rats. Keap1-Nrf2-IN-18 has the strongest inhibitory activity in structure−activity relationship (SAR) study (KD = 0.0029 μM).
  • HY-149508
    Nrf2-IN-3
    		Inhibitor
    Nrf2-IN-3 (Compound R16) is a Nrf2 inhibitor. Nrf2-IN-3 binds KEAP1 mutants (G333C mKEAP1) and repairs the disrupted KEAP1/NRF2 interactions. Nrf2-IN-3 sensitizes KEAP1-mutated cancer cells to Cisplatin (HY-17394) and Gefitinib (HY-50895) by repairing the mKEAP1/NRF2 complex.