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keap1-nrf2-in-1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (2) Bcl-2 Family (2) Caspase (2) Cholinesterase (ChE) (2) Deubiquitinase (1) E1/E2/E3 Enzyme (1) Ferroptosis (1) HDAC (2) Heme Oxygenase (HO) (2) Interleukin Related (2) Keap1-Nrf2 (17) NF-κB (2) Quinone Reductase (1) Reactive Oxygen Species (ROS) (6) Reference Standards (2) SOD (1) TNF Receptor (3) Transferrin Receptor (1)
By Research Areas:	Cancer (7) Inflammation/Immunology (13) Metabolic Disease (5) Neurological Disease (4)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13755

Sulforaphane 65+ Cited Publications	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-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-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-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-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-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-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-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-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-124941

7-Deacetylgedunin	Keap1-Nrf2 Reactive Oxygen Species (ROS)	Inflammation/Immunology
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-P5909

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

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 .

HY-168709

Nrf2 activator 18	Keap1-Nrf2	Inflammation/Immunology
Nrf2 activator 18 (Compound 11a) is an orally active activator for *Keap1/Nrf2/HO-1* signaling pathway, that promotes the Nrf2 nuclear translocation, and enhances the antioxidant efficacy. Nrf2 activator 18 inhibits the release of IL-6 with an IC₅₀ of 4.816 μM. Nrf2 activator 18 exhibits anti-inflammatory efficacy in mouse PM2.5-induced lung injury model .

HY-161643

S21-1011	Cholinesterase (ChE) Keap1-Nrf2	Neurological Disease Inflammation/Immunology
S21-1011 is a selective inhibitor for butyrylcholinesterase (BChE), with IC₅₀ of 0.059 and 0.162 μM, for eqBChE and hBChE, respectively. S21-1011 exhibits good blood-brain barrier (BBB) permeability and good pharmacokinetic characters. S21-1011 exhibits anti-inflammatory activity through activation of *keap1-Nrf2-ARE* pathway (EC₅₀ is 23.48 μM for antioxidant element ARE activation), ameliorates cognitive impairment in murine Alzheimer’s disease model .

HY-180155

Keap1/Nrf2/ARE activator 2	Keap1-Nrf2 Cholinesterase (ChE) Interleukin Related TNF Receptor Reactive Oxygen Species (ROS) Heme Oxygenase (HO) Quinone Reductase	Neurological Disease
Keap1/Nrf2/ARE activator 2 is an activator of *Keap1/Nrf2/ARE* pathway and non-competitively inhibits AChE with an IC₅₀ of 14.79 μM and a K_i of 1.35 μM. Keap1/Nrf2/ARE activator 2 promotes Nrf2 nuclear translocation, leading to antioxidant gene upregulation and enhanced cellular defense against oxidative stress. Keap1/Nrf2/ARE activator exhibits robust neuroprotection against both H₂O₂- and Scopolamine (SCA) (HY-N0296)-induced injury in PC12 cells. Keap1/Nrf2/ARE activator 2 ameliorates memory impairment and the neuro-inflammation associated with SCA-initiated cognitive dysfunction in a zebrafish model. Keap1/Nrf2/ARE activator 2 can be used for the research of Alzheimer's disease .

HY-101140AR

KI696 isomer (Standard)	Keap1-Nrf2 Reference Standards	Metabolic Disease Inflammation/Immunology
KI696 isomer (Standard) is the analytical standard of KI696 isomer (HY-101140A). This product is intended for research and analytical applications. KI696 isomer is the less active isomer of KI696 (HY-101140). KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction .

HY-101140R

KI696 (Standard)	Keap1-Nrf2 Reference Standards	Metabolic Disease Inflammation/Immunology
KI696 (Standard) is the analytical standard of KI696 (HY-101140). This product is intended for research and analytical applications. KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction. KI696 is a potent and selective inhibitor of the KEAP1/NRF2 interaction .

Cat. No.	Product Name

HY-L109

Protein-protein Interaction Inhibitor Library	797 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 797 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.

Protein-protein Interaction Inhibitor Library

797 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 797 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.

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

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-13755

Sulforaphane 65+ Cited Publications	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-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-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 .

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 .

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 .

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keap1-nrf2-in-1

Inhibitors & Agonists

Screening Libraries

Peptides

NaturalProducts

Isotope-Labeled Compounds

Natural
Products