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Keap1-IN-2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Aminotransferases (Transaminases) (1) AMPK (2) Apoptosis (11) Autophagy (2) Bcl-2 Family (3) Caspase (3) Cholinesterase (ChE) (2) COX (3) Cytochrome P450 (1) Deubiquitinase (1) Drug Derivative (1) Drug Isomer (1) E1/E2/E3 Enzyme (2) Environmental Pollutants (1) Ferroptosis (2) Fungal (1) Glutathione S-transferase (1) HDAC (2) Heme Oxygenase (HO) (4) HSP (1) HyT (1) Interleukin Related (5) Keap1-Nrf2 (68) Lactate Dehydrogenase (1) NF-κB (6) NO Synthase (2) NOD-like Receptor (NLR) (4) p38 MAPK (1) p62 (1) PARP (2) Pyroptosis (2) Quinone Reductase (5) Reactive Oxygen Species (ROS) (14) Reference Standards (5) ROS Kinase (1) Sirtuin (2) SOD (2) TNF Receptor (5) Transferrin Receptor (1)
By Research Areas:	Cancer (26) Cardiovascular Disease (4) Infection (1) Inflammation/Immunology (43) Metabolic Disease (13) Neurological Disease (13)
Click Chemistry:	Azide (1)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13755

Sulforaphane Maximum Cited Publications 69 Publications Verification	HDAC Keap1-Nrf2 Apoptosis Bcl-2 Family Caspase Reactive Oxygen Species (ROS)	Inflammation/Immunology Cancer
Sulforaphane is an orally active inducer of the *Keap1/Nrf2/ARE* pathway. Sulforaphane promotes the transcription of tumor-suppressing proteins and effectively inhibits the activity of HDACs. Through the activation of the Keap1/Nrf2/ARE pathway and further induction of HO-1 expression, Sulforaphane protects the heart. Sulforaphane suppresses high glucose-induced pancreatic cancer through AMPK-dependent signal transmission. Sulforaphane exhibits both anticancer and anti-inflammatory properties .

HY-101140

KI696 15+ Cited Publications	Keap1-Nrf2	Metabolic Disease Inflammation/Immunology
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-N0147

Rutaecarpine 5+ Cited Publications RutecarpINe	COX Keap1-Nrf2	Neurological Disease Inflammation/Immunology Cancer
Rutaecarpine, an alkaloid of Evodia rutaecarpa, is an inhibitor of COX-2 with an IC₅₀ value of 0.28 μM. Rutaecarpine can target and activate the NRF2/HO-1 pathway to reduce craniofacial injury. Rutaecarpine sttenuates oxidative stress-induced traumatic brain injury (TBI) and reduces secondary injury via the PGK1/KEAP1/NRF2 signaling pathway. Rutaecarpine can cross the blood-brain barrier (BBB).

HY-113298

Citraconic acid 4 Publications Verification Methylmaleic acid	NOD-like Receptor (NLR) Keap1-Nrf2 Reactive Oxygen Species (ROS)	Cardiovascular Disease Inflammation/Immunology
Citraconic acid (Methylmaleic acid) is an orally active inhibitor targeting the NLRP3 inflammasome and *Keap1-Nrf2* pathway. Citraconic acid reduces reactive oxygen species (ROS) generation by inhibiting succinate dehydrogenase (SDH) activity. Citraconic acid also modifies the conformation of Keap1 protein, relieves its inhibition of Nrf2, promotes antioxidant gene expression, and inhibits NLRP3 activation and the release of pro-inflammatory factors such as IL-1β and IL-18. Citraconic acid has anti-inflammatory and antioxidant activities, can reduce oxidative stress and cell pyroptosis, improve tissue damage, and can be used for the research of inflammation-related diseases such as acute renal ischemia-reperfusion injury. Citraconic acid is an isomer of Itaconic acid (HY-Y052) .

HY-110258

ML334 10+ Cited Publications LH601A	Quinone Reductase Keap1-Nrf2	Cancer
ML334 is a potent, cell permeable activator of NRF2 by inhibition of *Keap1-NRF2* protein-protein interaction. ML334 binds to Keap1 Kelch domain with a K_d of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity .

HY-13755A

(R)-Sulforaphane 2 Publications Verification L-Sulforaphane	Keap1-Nrf2 Bcl-2 Family Caspase Reactive Oxygen Species (ROS) NF-κB	Inflammation/Immunology Cancer
(R)-Sulforaphane (L-Sulforaphane) is a orally active, potent inducer of the Keap1/Nrf2/ARE pathway, exhibiting antioxidant and anticancer activities. (R)-Sulforaphane primarily functions by upregulating phase II detoxifying enzymes in cells, aiding in the removal of carcinogens and combating oxidative stress. (R)-Sulforaphane is capable of modulating gene expression, influencing various signaling pathways, including Nrf2, NF-κB, and AP-1. (R)-Sulforaphane can be used in studies of tumor biology, antioxidant defense mechanisms, as well as inflammation and immune responses .

HY-N0806

Sweroside 3 Publications Verification	Keap1-Nrf2 AMPK Sirtuin NF-κB NOD-like Receptor (NLR) Pyroptosis Apoptosis Autophagy PARP	Cardiovascular Disease Metabolic Disease Inflammation/Immunology Cancer
Sweroside is an iridoid glycoside that targets multiple targets, including the Keap1/Nrf2 axis, NLRP3 inflammasome, SIRT1, NF-κB, AMPK/mTOR pathway, and caspase family. Sweroside promotes Nrf2 nuclear translocation by competitively binding to Keap1. Sweroside also inhibits oxidative stress and NLRP3-mediated pyroptosis by activating Nrf2, inhibits NF-κB inflammatory pathway by activating SIRT1, and promotes autophagy and induces caspase-dependent apoptosis via the AMPK/mTOR pathway. Sweroside has antioxidant, anti-inflammatory, anti-apoptotic, and lipid metabolism regulating activities, and can be used in the research of myocardial ischemia-reperfusion injury, leukemia, acute lung injury, non-alcoholic fatty liver disease, and other fields .

HY-113162

Bovinic acid 1 Publications Verification	Keap1-Nrf2 Ferroptosis Reactive Oxygen Species (ROS) SOD	Metabolic Disease Cancer
Bovinic acid is an orally active anti-inflammatory agent. Bovinic acid inhibits oxidative stress and ferroptosis by regulating the *Keap1-Nrf2* signaling pathway. Bovinic acid exerts hepatoprotective effects against alcohol-associated liver disease. Bovinic acid can be used for the research of alcohol-associated liver disease .

HY-131592

Tricetin 1 Publications Verification	Apoptosis Keap1-Nrf2	Neurological Disease Inflammation/Immunology Cancer
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-147517

Keap1-Nrf2-IN-9	Keap1-Nrf2	Neurological Disease Inflammation/Immunology
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 no cytotoxic activity in ARPE19 cells .

HY-101140A

KI696 isomer	Keap1-Nrf2	Metabolic Disease Inflammation/Immunology
KI696 isomer is the less active isomer of KI696 (HY-101140). KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction .

HY-120371

CPUY192018 1 Publications Verification	Keap1-Nrf2 Apoptosis Reactive Oxygen Species (ROS) NF-κB	Inflammation/Immunology
CPUY192018 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction, with an IC₅₀ of 0.63 µM. CPUY192018 exhibits anti-inflammatory and antioxidant activities. CPUY192018 can activate the Nrf2-dependent antioxidant pathway and inhibit the NF-κB-related inflammatory response. CPUY192018 can be used in the research of inflammation-related diseases .

HY-B0854

Mancozeb	Environmental Pollutants Lactate Dehydrogenase Apoptosis Fungal Cytochrome P450 Keap1-Nrf2	Infection Metabolic Disease Cancer
Mancozeb is a widely used fungicide that is effective against fungal diseases in most cereals, vegetables, fruits and ornamental plants. In addition, Mancozeb can cause liver damage in mice by activating the *Keap1/Nrf2* signaling pathway. Mancozeb upregulates lactate dehydrogenase and cytochrome c to alter cell metabolism and induce cell death. Mancozeb has reproductive toxicity and can induce apoptosis in ovarian cells .

HY-149508

Nrf2-IN-3	Keap1-Nrf2 Reactive Oxygen Species (ROS)	Cancer
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-151362

Keap1-Nrf2-IN-14 1 Publications Verification	Keap1-Nrf2 Reactive Oxygen Species (ROS)	Inflammation/Immunology
Keap1-Nrf2-IN-14 (compound 20c) is a *KEAP1-NRF2* inhibitor that effectively disrupts the *KEAP1-NRF2* interaction (IC₅₀=75 nM) with a K_d value of 24 nM for *KEAP1. Keap1-Nrf2-IN-14* induces the expression of NRF2 target genes and enhances the downstream antioxidant and anti-inflammatory activities. Keap1-Nrf2-IN-14 can be used in the study of oxidative stress-related inflammation .

HY-149010

NXPZ-2	Keap1-Nrf2	Neurological Disease
NXPZ-2 is an orally active *Keap1-Nrf2* protein–protein interaction (PPI) inhibitor with a K_i 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-134205A

CBR-470-1 3 Publications Verification	Keap1-Nrf2	Neurological Disease Metabolic Disease
CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nrf2 activator. CBR-470-1 protects SH-SY5Y neuronal cells against MPP ⁺-induced cytotoxicity through activation of the Keap1-Nrf2 cascade .

HY-103435

Vialinin A 2 Publications Verification TerrestrIN A	Deubiquitinase TNF Receptor E1/E2/E3 Enzyme Keap1-Nrf2	Inflammation/Immunology Cancer
Vialinin A (Terrestrin A) is a p-terphenyl compound that can be derived from a Chinese edible mushroom. Vialinin A is an inhibitor of ubiquitin-specific peptidase 4 (USP4) and has anti-inflammatory and antioxidant properties. Vialinin A can alleviate cerebral ischaemia-reperfusion injury-induced neurological deficits and neuronal apoptosis. Vialinin A promotes activation of *Keap1-Nrf2-ARE* signaling pathway and increases the protein degradation of *Keap1. Vialinin A possesses various pharmacological activities in cancer, Kawasaki disease, asthma, and pathological scarring. Vialinin A is a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1*). Vialinin A can be studied in reseach for autoimmune diseases, cancer and ischaemic stroke .

HY-121523

MIND4-17	Keap1-Nrf2	Metabolic Disease
MIND4-17 is a potent NRF2 activator that covalently modifies a C151 residue of Keap1. MIND4-17 disrupts Keap1-Nrf2 association, leading to Nrf2 protein stabilization and nuclear translocation. MIND4‐17 exerts potent antioxidant activity .

HY-173444

HDAC11-IN-3	HDAC Transferrin Receptor Apoptosis Ferroptosis	Cancer
HDAC11-IN-3 (Compound A9) is a selective HDAC11 inhibitor (IC₅₀: 4.1 nM). HDAC11-IN-3 has inhibitory effects on U937 and OCI-AML2 acute myeloid leukemia (AML) cell lines (IC₅₀: 10 μM). HDAC11-IN-3 has significant anti-AML activity, inducing apoptosis, cell cycle arrest, and differentiation. HDAC11-IN-3 upregulates the iron transporters transferrin (TF) and transferrin receptor (TFRC), and activates the p62-Keap1-Nrf2-HMOX1 pathway, which together lead to increased intracellular iron levels and induce ferroptosis in AML cells. HDAC11-IN-3 can be used alone or in combination with Cytarabine (HY-13605) for AML research .

HY-174287

*Keap1-IN-2*	Keap1-Nrf2	Inflammation/Immunology
Keap1-IN-2 (Compound 164) is a *KEAP1* inhibitor (IC₅₀: 2 nM). Keap1-IN-2 indirectly activates Nrf2 by inhibiting KEAP1, thereby enhancing the antioxidant capacity of cells. Keap1-IN-2 promotes the accumulation and nuclear translocation of Nrf2 by blocking KEAP1-mediated Nrf2 degradation. Keap1-IN-2 can be used to study diseases associated with oxidative stress, such as inflammatory bowel disease, Crohn's disease, and immune diseases such as ulcerative colitis .

HY-141439

TBE 31	Keap1-Nrf2 Quinone Reductase Glutathione S-transferase Apoptosis TNF Receptor	Inflammation/Immunology Cancer
TBE 31 is an orally active *Keap1/Nrf2* pathway activator and NQO1 inducer with a D_m value of 1.1 nM for NQO1. TBE 31 binds to cysteine residues of Keap1, inhibits ubiquitination and degradation of Nrf2, thereby activating the expression of ARE-dependent genes. TBE 31 induces cytoprotective enzymes including NQO1 and GST isoforms, promotes Nrf2 accumulation, and upregulates Nrf2-regulated genes related to antioxidation and lipid metabolism. TBE 31 inhibits pro-inflammatory responses, formation of AFB1-DNA adducts, endoplasmic reticulum stress, cell apoptosis (apoptosis), hepatic fibrosis, oxidative stress, and the expression of ChREBP. TBE 31 reduces the number of tumors in a mouse model of ultraviolet-induced skin carcinogenesis. TBE 31 enhances nerve growth factor-induced neurite outgrowth. TBE 31 attenuates LPS-induced serum TNF-α levels and immobility time in mice. TBE 31 can be used in research related to liver cancer, skin cancer, inflammation-related depression, and non-alcoholic steatohepatitis .

HY-146577

Keap1-Nrf2-IN-7	Keap1-Nrf2	Inflammation/Immunology
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-P5909F

*FITC-labeled Keap1-Nrf2* probe**	Keap1-Nrf2	Others
FITC-labeled Keap1-Nrf2 probe is aFITC-labeled Keap1-Nrf2 probe (HY-P5909).

HY-139862

Keap1-Nrf2-IN-3	Keap1-Nrf2	Others
Keap1-Nrf2-IN-3 is a *KEAP1:NRF2* protein−protein interaction inhibitor, and with a K_d value of 2.5 nM for KEAP1 protein.

HY-178054

LMDP10	Keap1-Nrf2 Drug Derivative	Neurological Disease
LMDP10 is an orally active 3-amino quinazoline derivative with *Keap1-Nrf2* pathway activation activity. LMDP10 binds to Keap1 to inhibit *Keap1-Nrf2* interaction, thereby activating the Nrf2 pathway. LMDP10 elevates Nrf2, SOD, and GSH levels, reduces MDA and TNF-α levels, attenuates neurodegeneration, and improves memory function in Alzheimer’s disease (AD) rats. LMDP10 can be used for the study of AD .

HY-N10313

Dehydrobruceine B	Bcl-2 Family Keap1-Nrf2 Apoptosis	Cancer
Dehydrobruceine B, a quassinoid, can be isolated from Brucea javanica. Dehydrobruceine B shows a synergistic effect with Cisplatin (HY-17394) to induce apoptosis via mitochondrial method. Dehydrobruceine B increases apoptosis-inducing factor (AIF) and Bax expression and suppresses *Keap1-Nrf2* .

HY-110258B

(R,S,R)-ML334 (R,S,R)-LH601A	Drug Isomer	Cancer
(R,S,R)-ML334 is the isomer of ML334 (HY-110258), and can be used as an experimental control. ML334 is a potent, cell permeable activator of NRF2 by inhibition of *Keap1-NRF2* protein-protein interaction. ML334 binds to Keap1 Kelch domain with a K_d of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity .

HY-175548

Nrf2 activator-21	Keap1-Nrf2 Apoptosis Caspase	Neurological Disease
Nrf2 activator-21 is a Nrf2 activator with dual antioxidant and neuroprotective properties. Nrf2 activator-21 binds to *Keap1* Kelch domain and disrupts *Keap1-Nrf2* interactions and activate antioxidant defense mechanisms. Nrf2 activator-21 reduces apoptosis and decreases caspase-3 activity in the hippocampal neurons. Nrf2 activator-21 targets cerebral ischemia/reperfusion injury (CIRI) via Nrf2 pathway activation. Nrf2 activator-21 improves neurological function, alleviates anxiety-like behavior, enhances memory in rats with 2-vessel occlusion (2VO)-induced CIRI. Nrf2 activator-21 can be used for the study of cerebral ischemia/reperfusion injury .

HY-179398

Keap1-Nrf2-IN-29	Keap1-Nrf2	Cancer
Keap1-Nrf2-IN-29 (Compound 1a), a Curcumin (HY-N0005) analog, is a *Keap1* protein inhibitor. Keap1-Nrf2-IN-29 exhibits significant inhibitory activity against A549, PC-3 and MCF-7 cells. Keap1-Nrf2-IN-29 can be used for the study of prostate cancer .

HY-150579

Keap1-Nrf2-IN-13	Keap1-Nrf2	Inflammation/Immunology Cancer
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 .

HY-W701218

Sulforaphane-d8	Reactive Oxygen Species (ROS)	Cancer
Sulforaphane-d₈ is the deuterium labeled Sulforaphane (HY-13755). Sulforaphane is an orally active inducer of the Keap1/Nrf2/ARE pathway. Sulforaphane promotes the transcription of tumor-suppressing proteins and effectively inhibits the activity of HDACs. Through the activation of the Keap1/Nrf2/ARE pathway and further induction of HO-1 expression, Sulforaphane protects the heart. Sulforaphane suppresses high glucose-induced pancreatic cancer through AMPK-dependent signal transmission. Sulforaphane exhibits both anticancer and anti-inflammatory properties .

HY-174395

CD-10	Keap1-Nrf2 Interleukin Related Heme Oxygenase (HO)	Neurological Disease
CD-10 is an orally active and BBB-penatrable *Keap1-Nrf2 protein-protein interaction (PPI) inhibitor. CD-10 binds to Keap1* with a K_D value of 193 nM. CD-10 exhibits potent anti-oxidative and anti-inflammatory effects through Keap1-Nrf2 pathway activation, evidenced by reduced levels of MDA, IL-4, IL-10 and increased expression of HO-1. CD-10 effectively alleviated anxiety and depressive behaviors and restored serum neurotransmitter levels by promoting Nrf2 nuclear translocation in the chronic unpredictable mild stress (CUMS) mouse model. CD-10 can be used for the study of depression.

HY-W505984

TPNA10168 KM05073	Keap1-Nrf2	Inflammation/Immunology
TPNA10168 is an Nrf-2 activator that activates the *Keap1-Nrf2-ARE* pathway. TPNA10168 is neuroprotective against oxidative stress-induced damage. TPNA10168 significantly reduces the transcription of inflammatory genes, including TNF-α, IL-1β, IL-6, and iNOS. TPNA10168 can be used in research on anti-inflammatory and neurological diseases .

HY-171035

PRL-295	Quinone Reductase Keap1-Nrf2 Aminotransferases (Transaminases)	Metabolic Disease
PRL-295 is an orally active inhibitor targeting *Keap1-Nrf2* interaction. PRL-295 increases the thermal stability of Keap1 and disrupts its interaction with Nrf2, thereby activating the Nrf2-dependent transcriptional target NAD(P)H:quinone oxidoreductase 1 (NQO1). PRL-295 protects against Acetaminophen (HY-66005)-induced liver injury in mice .

HY-175833

NF-κB-IN-20	NF-κB Keap1-Nrf2 Heme Oxygenase (HO) Interleukin Related TNF Receptor Reactive Oxygen Species (ROS) SOD	Inflammation/Immunology
NF-κB-IN-20 is an orally active NF-κB inhibitor. NF-κB-IN-20 directly binds to the Keap1 protein, activating the *Keap1/Nrf2/HO-1* antioxidant pathway, and simultaneously inhibiting the NF-κB inflammatory pathway, thereby synergistically reducing oxidative stress and inflammatory responses. NF-κB-IN-20 M11 inhibits the expression of IL-6, IL-1β, and TNF-α, significantly reduces the level of ROS, and restores the mitochondrial membrane potential. NF-κB-IN-20 can be used for the study of acute lung injury (ALI) .

HY-P5909

Keap1-Nrf2 probe	Keap1-Nrf2	Cancer
Keap1-Nrf2 probe is a *Keap1-Nrf2* probe .

HY-147924

Keap1-Nrf2-IN-11	Keap1-Nrf2 NO Synthase ROS Kinase	Inflammation/Immunology
Keap1-Nrf2-IN-11 (compound 6k) is a *Keap1-Nrf2* inhibitor with K_D2 value of 0.21 nM. Keap1-Nrf2-IN-11 inhibits the productions of ROS and NO and the expression of TNF-α. Keap1-Nrf2-IN-11 relieves inflammations by increasing the Nrf2 nuclear translocation. Keap1-Nrf2-IN-11 can be used for anti-inflammatory research .

HY-168526

Keap1-Nrf2-IN-24	Keap1-Nrf2	Inflammation/Immunology
Keap1-Nrf2-IN-24 (compound 57) is a potent *Keap1-Nrf2* inhibitor with a K_i value of 13 nM. Keap1-Nrf2-IN-24 increases the protein expression of TRXR1 and NQO1. Keap1-Nrf2-IN-24 increases the AKR1B10 mRNA expression. Keap1-Nrf2-IN-24 shows good metabolic stability .

HY-168161

Keap1-Nrf2-IN-23	Keap1-Nrf2	Cancer
Keap1-Nrf2-IN-23 (compound 56) is an inhibitor of the Keap1–Nrf2 PPI (IC₅₀=16.0 nM). Keap1-Nrf2-IN-23 binds to Keap1 with a K_d value of 3.07 nM. Keap1-Nrf2-IN-23 has oral activity .

HY-143893

Keap1-Nrf2-IN-6	Keap1-Nrf2	Inflammation/Immunology
Keap1-Nrf2-IN-6 (compound 64) is a potent and selective Keap1-Nrf2 PPI (Keap1-Nrf2 protein−protein interaction) inhibitor with an IC₅₀ of 41 nM, K_d of 68 nM .

HY-143892

Keap1-Nrf2-IN-5	Keap1-Nrf2	Inflammation/Immunology
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, K_d of 3.7 µM .

HY-150578

Keap1-Nrf2-IN-12	Keap1-Nrf2	Inflammation/Immunology
Keap1-Nrf2-IN-12 is a potent *Keap1-Nrf2* inhibitor with an IC₅₀ value of 2.30 µM. Keap1-Nrf2-IN-12 shows metabolic stability in human liver microsomes .

HY-176146

Keap1/Nrf2/ARE activator 1	Keap1-Nrf2	Neurological Disease Inflammation/Immunology
Keap1/Nrf2/ARE activator 1 (compound HT-3) is a *Keap1/Nrf2/ARE* pathway activator. Keap1/Nrf2/ARE activator 1 exhibits antioxidant activity and neuroprotective efficacy .

HY-162096

Keap1-Nrf2-IN-17	Keap1-Nrf2	Cancer
Keap1-Nrf2-IN-17 (compound 18) is a potent inhibitor of *Keap1-Nrf2* protein-protein interaction .

HY-172598

Keap1-Nrf2-IN-28	Keap1-Nrf2	Inflammation/Immunology
Keap1-Nrf2-IN-28 (SG16) is an orally active *Keap1-Nrf2* inhibitor. Keap1-Nrf2-IN-28 shows antioxidant capability and induces the upregulation of Nrf2, HO-1, GCLM, and Akr1c1. Keap1-Nrf2-IN-28 attenuates APAP (HY-66005)-induced acute liver injury .

HY-144099

Keap1-Nrf2-IN-4	E1/E2/E3 Enzyme Apoptosis	Cancer
Keap1-Nrf2-IN-4 is a potent neddylation inhibitor. Keap1-Nrf2-IN-4 exhibits potent anti-proliferation activity against MGC-803 cells (IC₅₀=2.55 µM). Keap1-Nrf2-IN-4 blocks the migration ability and induces apoptosis of gastric cancer cells. Keap1-Nrf2-IN-4 inhibits tumor growth without obvious toxicity .

HY-146578

Keap1-Nrf2-IN-8	Keap1-Nrf2	Inflammation/Immunology
Keap1-Nrf2-IN-8 (compound 12d) is a potent Keap1-Nrf2 PPI (Keap1-Nrf2 protein−protein interaction) inhibitor with IC₅₀s of 64.5 nM and 14.2 nM for FP and TR-FRET assays, respectively. Keap1-Nrf2-IN-8 significantly increases the mRNA levels of Nrf2 downstream genes, GSTM3, HMOX2 and NQO1 .

HY-168065

Keap1-Nrf2-IN-22	Keap1-Nrf2	Inflammation/Immunology
Keap1-Nrf2-IN-22 (compound 19) is a *Keap1-Nrf2* inhibitor， with a K_D2 value of 42.2 nM for Keap1. Keap1-Nrf2-IN-22 can be used for the study of acute lung injury (ALI) and cerebral ischemia/reperfusion (I/R) injury .

HY-170761

KEAP1-NRF2 PPI-IN-1	Keap1-Nrf2	Cancer
KEAP1-NRF2 PPI-IN-1 (compound 23) is an inhibitor targeting the *KEAP1-NRF2* interaction. KEAP1-NRF2 PPI-IN-1 has IC₅₀ values of 136 nM and 62 nM in the DNA damage assays of human TK6 and insect SF9 cell lines, respectively .

Cat. No.	Product Name

HY-L037

Antioxidant Compound Library

2,332 compounds

Oxidative stress is an imbalance of free radicals and antioxidants in the body, which can lead to cell and tissue damage. Oxidative stress can be responsible for the induction of several diseases, both chronic and degenerative, as well as speeding up body aging process and cause acute pathologies. Antioxidants are a class of compounds able to counteract oxidative stress and mitigate its effects on individuals’ health, gained enormous attention from the biomedical research community. Antioxidants have long been substantial and amenable therapeutic arsenals for multifarious diseases such as AD and cancer.

MCE Antioxidant Compound Library contains 2,332 compounds that act as antioxidants for high throughput screening (HTS) and high content screening (HCS). This library is a useful tool for discovery new antioxidants and oxidative stress research.

HY-L014

NF-κB Signaling Compound Library

1,670 compounds

Nuclear factor-κB (NF-κB)/Rel proteins include NF-κB2 p52/p100, NF-κB1 p50/p105, c-Rel, RelA/p65, and RelB. These proteins function as dimeric transcription factors that regulate the expression of genes and influence a broad range of biological processes including innate and adaptive immunity, inflammation, stress responses, B-cell development, and lymphoid organogenesis. NF-κB plays a key role in regulating the immune response to infection. In addition, activation of the NF-κB pathway is involved in the pathogenesis of chronic inflammatory diseases, such as asthma, rheumatoid arthritis, and inflammatory bowel disease. Incorrect regulation of NF-κB has been linked to cancer, inflammatory and autoimmune diseases, septic shock, viral infection, and improper immune development.

MCE owns a unique collection of 1,670 small molecule compounds that can be used in the research of NF-κB signaling pathway or high throughput screening (HTS) related drug discovery.

HY-L109

Protein-protein Interaction Inhibitor Library

782 compounds

Protein protein interactions (PPI) have pivotal roles in life processes. The studies showed that aberrant PPI are associated with various diseases, including cancer, infectious diseases, and neurodegenerative diseases. The classic drug targets are usually enzymes, ion channels, or receptors, the PPI indicate new potential therapeutic targets. Therefore, targeting PPI is a new direction in treating diseases and an essential strategy for the development of new drugs.

However, the design of modulators targeting PPI still faces tremendous challenges, such the difficult PPI interfaces for the drug design, lack of ligands reference, lack of guidance rules for the PPI modulators development and high-resolution PPI proteins structures.

With the development of high-throughput technology, high-throughput screening is also gradually used for the identification of PPI inhibitors, but the compound library used for conventional target screening is not very effective in screening PPI inhibitors. To improve screening efficiency, MCE carefully selected 782 PPI inhibitors and mainly targeting MDM2-p53, Keap1-Nrf2, PD-1/PD-L1, Myc-Max, etc. MCE Protein-protein Interaction Inhibitor Library is a useful tool for PPI drug discovery and related research.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-13755

Sulforaphane Maximum Cited Publications 69 Publications Verification	Natural Products other families Classification of Application Fields Plants Inflammation/Immunology Disease Research Fields Source Classification	HDAC Keap1-Nrf2 Apoptosis Bcl-2 Family Caspase Reactive Oxygen Species (ROS)
Sulforaphane is an orally active inducer of the *Keap1/Nrf2/ARE* pathway. Sulforaphane promotes the transcription of tumor-suppressing proteins and effectively inhibits the activity of HDACs. Through the activation of the Keap1/Nrf2/ARE pathway and further induction of HO-1 expression, Sulforaphane protects the heart. Sulforaphane suppresses high glucose-induced pancreatic cancer through AMPK-dependent signal transmission. Sulforaphane exhibits both anticancer and anti-inflammatory properties .

HY-N0147

Rutaecarpine 5+ Cited Publications RutecarpINe	Alkaloids Structural Classification Classification of Application Fields Evodia rutaecarpa (Juss.) Benth. Rutaceae Plants Disease Research Fields Indole Alkaloids Source Classification Cancer	COX Keap1-Nrf2
Rutaecarpine, an alkaloid of Evodia rutaecarpa, is an inhibitor of COX-2 with an IC₅₀ value of 0.28 μM. Rutaecarpine can target and activate the NRF2/HO-1 pathway to reduce craniofacial injury. Rutaecarpine sttenuates oxidative stress-induced traumatic brain injury (TBI) and reduces secondary injury via the PGK1/KEAP1/NRF2 signaling pathway. Rutaecarpine can cross the blood-brain barrier (BBB).

HY-113298

Citraconic acid 4 Publications Verification Methylmaleic acid	Structural Classification Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Other Diseases Endogenous metabolite Disease Research Fields Source Classification	NOD-like Receptor (NLR) Keap1-Nrf2 Reactive Oxygen Species (ROS)
Citraconic acid (Methylmaleic acid) is an orally active inhibitor targeting the NLRP3 inflammasome and *Keap1-Nrf2* pathway. Citraconic acid reduces reactive oxygen species (ROS) generation by inhibiting succinate dehydrogenase (SDH) activity. Citraconic acid also modifies the conformation of Keap1 protein, relieves its inhibition of Nrf2, promotes antioxidant gene expression, and inhibits NLRP3 activation and the release of pro-inflammatory factors such as IL-1β and IL-18. Citraconic acid has anti-inflammatory and antioxidant activities, can reduce oxidative stress and cell pyroptosis, improve tissue damage, and can be used for the research of inflammation-related diseases such as acute renal ischemia-reperfusion injury. Citraconic acid is an isomer of Itaconic acid (HY-Y052) .

HY-13755A

(R)-Sulforaphane 2 Publications Verification L-Sulforaphane	Natural Products other families Classification of Application Fields Plants Disease Research Fields Source Classification Cancer	Keap1-Nrf2 Bcl-2 Family Caspase Reactive Oxygen Species (ROS) NF-κB
(R)-Sulforaphane (L-Sulforaphane) is a orally active, potent inducer of the Keap1/Nrf2/ARE pathway, exhibiting antioxidant and anticancer activities. (R)-Sulforaphane primarily functions by upregulating phase II detoxifying enzymes in cells, aiding in the removal of carcinogens and combating oxidative stress. (R)-Sulforaphane is capable of modulating gene expression, influencing various signaling pathways, including Nrf2, NF-κB, and AP-1. (R)-Sulforaphane can be used in studies of tumor biology, antioxidant defense mechanisms, as well as inflammation and immune responses .

HY-N0806

Sweroside 3 Publications Verification	Monophenols Classification of Application Fields Labiatae Lespedeza tomentosa (Thunb.) Siebold ex Maxim. Phenols Metabolic Disease Plants Disease Research Fields	Keap1-Nrf2 AMPK Sirtuin NF-κB NOD-like Receptor (NLR) Pyroptosis Apoptosis Autophagy PARP
Sweroside is an iridoid glycoside that targets multiple targets, including the Keap1/Nrf2 axis, NLRP3 inflammasome, SIRT1, NF-κB, AMPK/mTOR pathway, and caspase family. Sweroside promotes Nrf2 nuclear translocation by competitively binding to Keap1. Sweroside also inhibits oxidative stress and NLRP3-mediated pyroptosis by activating Nrf2, inhibits NF-κB inflammatory pathway by activating SIRT1, and promotes autophagy and induces caspase-dependent apoptosis via the AMPK/mTOR pathway. Sweroside has antioxidant, anti-inflammatory, anti-apoptotic, and lipid metabolism regulating activities, and can be used in the research of myocardial ischemia-reperfusion injury, leukemia, acute lung injury, non-alcoholic fatty liver disease, and other fields .

HY-113162

Bovinic acid 1 Publications Verification	Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Metabolic Disease Endogenous metabolite Disease Research Fields Source Classification	Keap1-Nrf2 Ferroptosis Reactive Oxygen Species (ROS) SOD
Bovinic acid is an orally active anti-inflammatory agent. Bovinic acid inhibits oxidative stress and ferroptosis by regulating the *Keap1-Nrf2* signaling pathway. Bovinic acid exerts hepatoprotective effects against alcohol-associated liver disease. Bovinic acid can be used for the research of alcohol-associated liver disease .

HY-131592

Tricetin 1 Publications Verification	Flavonols Flavonoids Cupressaceae Thuja occidentalisLinn. Neurological Disease Classification of Application Fields Plants Inflammation/Immunology Disease Research Fields Source Classification	Apoptosis Keap1-Nrf2
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-N10313

Dehydrobruceine B	Natural Products Microorganisms Source Classification	Bcl-2 Family Keap1-Nrf2 Apoptosis
Dehydrobruceine B, a quassinoid, can be isolated from Brucea javanica. Dehydrobruceine B shows a synergistic effect with Cisplatin (HY-17394) to induce apoptosis via mitochondrial method. Dehydrobruceine B increases apoptosis-inducing factor (AIF) and Bax expression and suppresses *Keap1-Nrf2* .

HY-124941

7-Deacetylgedunin	Natural Products Toona sinensis (A. Juss.) Roem. Plants Meliaceae Source Classification	Keap1-Nrf2 Reactive Oxygen Species (ROS)
7-Deacetylgedunin is an activator of *Keap1/Nrf2/HO-1. 7-Deacetylgedunin alleviates mice mortality induced by LPS. 7-Deacetylgedunin inhibits Keap1* expression and suppresses macrophage proliferation. 7-Deacetylgedunin suppresses inflammation in vivo and in vitro .

HY-N0147R

Rutaecarpine (Standard) RutecarpINe (Standard)	Alkaloids Structural Classification Evodia rutaecarpa (Juss.) Benth. Rutaceae Plants Indole Alkaloids Source Classification	Reference Standards COX Keap1-Nrf2
Rutaecarpine (Standard) is the analytical standard of Rutaecarpine. This product is intended for research and analytical applications. Rutaecarpine, an alkaloid of Evodia rutaecarpa, is an inhibitor of COX-2 with an IC₅₀ value of 0.28 μM. Rutaecarpine can target and activate the NRF2/HO-1 pathway to reduce craniofacial injury. Rutaecarpine sttenuates oxidative stress-induced traumatic brain injury (TBI) and reduces secondary injury via the PGK1/KEAP1/NRF2 signaling pathway. Rutaecarpine can cross the blood-brain barrier (BBB).

HY-113298R

Citraconic acid (Standard) Methylmaleic acid (Standard)	Structural Classification Microorganisms Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	Reference Standards NOD-like Receptor (NLR) Keap1-Nrf2 Reactive Oxygen Species (ROS)
Citraconic acid (Methylmaleic acid) (Standard) is the analytical standard of Citraconic acid (HY-113298). This product is intended for research and analytical applications. Citraconic acid is an orally active inhibitor targeting the NLRP3 inflammasome and *Keap1-Nrf2* pathway. Citraconic acid reduces reactive oxygen species (ROS) generation by inhibiting succinate dehydrogenase (SDH) activity. Citraconic acid also modifies the conformation of Keap1 protein, relieves its inhibition of Nrf2, promotes antioxidant gene expression, and inhibits NLRP3 activation and the release of pro-inflammatory factors such as IL-1β and IL-18. Citraconic acid has anti-inflammatory and antioxidant activities, can reduce oxidative stress and cell pyroptosis, improve tissue damage, and can be used for the research of inflammation-related diseases such as acute renal ischemia-reperfusion injury. Citraconic acid is an isomer of Itaconic acid (HY-Y052) .

HY-N0806R

Sweroside (Standard)	Structural Classification Monophenols Labiatae Lespedeza tomentosa (Thunb.) Siebold ex Maxim. Phenols Plants	Reference Standards Keap1-Nrf2 AMPK Sirtuin NF-κB NOD-like Receptor (NLR) Pyroptosis Apoptosis Autophagy PARP
Sweroside (Standard) is the analytical standard of Sweroside (HY-N0806). This product is intended for research and analytical applications. Sweroside is an iridoid glycoside that targets multiple targets, including the Keap1/Nrf2 axis, NLRP3 inflammasome, SIRT1, NF-κB, AMPK/mTOR pathway, and caspase family. Sweroside promotes Nrf2 nuclear translocation by competitively binding to Keap1. Sweroside also inhibits oxidative stress and NLRP3-mediated pyroptosis by activating Nrf2, inhibits NF-κB inflammatory pathway by activating SIRT1, and promotes autophagy and induces caspase-dependent apoptosis via the AMPK/mTOR pathway. Sweroside has antioxidant, anti-inflammatory, anti-apoptotic, and lipid metabolism regulating activities, and can be used in the research of myocardial ischemia-reperfusion injury, leukemia, acute lung injury, non-alcoholic fatty liver disease, and other fields .

HY-N17603

Ginnalin A AcertannIN	Structural Classification Sapindaceae Phenols Polyphenols Acer tataricum subsp. ginnala (Maximowicz) Wesmael Plants Source Classification	Keap1-Nrf2 p62 Heme Oxygenase (HO)
Ginnalin A (Acertannin) is a Nrf2 activator. Ginnalin A shows antiproliferative activity against HCT116, SW480 and SW620 cells with IC₅₀ values of 24.8, 22.0, and 39.7 μM, respectively. Ginnalin A can induce cancer cells S phase arrest. Ginnalin A can activate the *p62-Keap1-Nrf2* signaling pathway, significantly upregulate the mRNA and protein expression of Nrf2, HO-1, and NQO1, and promote the transport of Nrf2 from the cytoplasm to the nucleus. Ginnalin A can be used for the research of colon cancer .

Cat. No.	Product Name	Chemical Structure

HY-W701218

Sulforaphane-d8

Sulforaphane-d₈ is the deuterium labeled Sulforaphane (HY-13755). Sulforaphane is an orally active inducer of the Keap1/Nrf2/ARE pathway. Sulforaphane promotes the transcription of tumor-suppressing proteins and effectively inhibits the activity of HDACs. Through the activation of the Keap1/Nrf2/ARE pathway and further induction of HO-1 expression, Sulforaphane protects the heart. Sulforaphane suppresses high glucose-induced pancreatic cancer through AMPK-dependent signal transmission. Sulforaphane exhibits both anticancer and anti-inflammatory properties .

Cat. No.	Product Name		Classification

HY-159495

Keap1-Nrf2-IN-21		Azide
Keap1-Nrf2-IN-21 (compound 4d) is a glucose metabolism inhibitor with antitumor activity. Keap1-Nrf2-IN-21 inhibits glycolytic activity of cancer cells by targeting the glycolytic pathway, especially by affecting the *Keap1-Nrf2* signaling pathway, thereby inhibiting tumor growth. Keap1-Nrf2-IN-21 exhibits cytotoxicity against the HEC1A cell line (IC₅₀=2.60 μM) .

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