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Results for "

Keap1-Nrf2

" in MCE Product Catalog:

By Targets:	Apoptosis (3) Bcl-2 Family (1) E1/E2/E3 Enzyme (1) Keap1-Nrf2 (24) NF-κB (1) NO Synthase (1) Reactive Oxygen Species (1) ROS Kinase (1)
By Research Areas:	Cancer (6) Inflammation/Immunology (16) Metabolic Disease (7) Neurological Disease (4)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Cat. No.	Product Name	Target	Research Areas

HY-150579

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

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-151362

Keap1-Nrf2-IN-14	Keap1-Nrf2 Reactive Oxygen Species	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-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-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-147517

Keap1-Nrf2-IN-9	Keap1-Nrf2	Inflammation/Immunology Neurological Disease
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-149245

Keap1-Nrf2-IN-15	Keap1-Nrf2	Inflammation/Immunology
Keap1-Nrf2-IN-15 (Compound 24a) is a potent Keap1-Nrf2 protein-protein interaction inhibitor with IC₅₀s of 77 nM and 2.5 nM in FP assay and TR-FRET assay, respectively.

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-126245A

Keap1-Nrf2-IN-1 TFA	Keap1-Nrf2	Metabolic Disease Inflammation/Immunology
Keap1-Nrf2-IN-1 TFA (compound35) is a *Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2 (Keap1-Nrf2) protein-protein interaction* inhibitor, and with an IC₅₀ of 43 nM for Keap1 protein. Keap1-Nrf2-IN-1 TFA activates Nrf2-regulated cytoprotective response and antagonizes acetaminophen-induced liver injury both in cellular and in vivo models.

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-147548

Keap1-Nrf2-IN-10	Others	Others
Keap1-Nrf2-IN-10 (compound 15) is a potent NQO1 inducer. Keap1-Nrf2-IN-10 inhibits oxidative stress by decreasing the levels of MDA, ROS, NQO1 in the liver for gamma-irradiated mice. Keap1-Nrf2-IN-10 improves the survival of gamma-irradiated mice.

HY-126245

Keap1-Nrf2-IN-1	Keap1-Nrf2	Metabolic Disease Inflammation/Immunology
Keap1-Nrf2-IN-1 is a Keap1 (Kelch-like ECH-associated protein 1)-Nrf2 (nuclear factor erythroid 2-related factor 2) protein-protein interaction inhibitor, and with an IC₅₀ of 43 nM for Keap1 protein. Keap1-Nrf2-IN-1 activates Nrf2-regulated cytoprotective response and antagonizes Acetaminophen-induced liver injury.

HY-101140

KI696	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-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-131592

Tricetin	Apoptosis Keap1-Nrf2	Cancer Inflammation/Immunology Neurological Disease
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-134205A

CBR-470-1	Keap1-Nrf2	Metabolic Disease Neurological 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-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-N10659

Praelolide	Keap1-Nrf2 NF-κB	Metabolic Disease
Praelolide is a potent *Nrf2* activator. Praelolide suppresses osteoclastogenesis and reactive oxygen species (ROS) production. Praelolide disrupts Keap1-Nrf2 protein-protein interactions by noncovalent binding to Keap1. Praelolide has the potential for the research of osteoclastogenic bone disease.

HY-110258

ML334 LH601A	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-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-110275

RA839	Keap1-Nrf2	Others
RA839 is a noncovalent small molecule binder to Keap1 with a K_d of ∼6 μM and selective activator of Nrf2 signaling. RA839 prevents the induction of both inducible nitric-oxide synthase expression and nitric oxide release in response to lipopolysaccharides in macrophages. RA839 is a selective inhibitor of the Keap1/Nrf2 interaction and a useful tool compound to study the biology of Nrf2.

HY-120371

CPUY192018	Others	Inflammation/Immunology
CPUY192018 is a potent *Keap1-Nrf2-ARE* inhibitor with an IC₅₀ of 0.63 µM. CPUY192018 exhibits induction of Nrf2-dependent gene NQO1 at 100 µM.

HY-13755A

(R)-Sulforaphane L-Sulforaphane	Keap1-Nrf2	Cancer
(R)-Sulforaphane (L-Sulforaphane) is a highly potent inducer of the *Keap1/Nrf2/ARE* pathway. (R)-Sulforaphane is a far more potent inducer of the carcinogen-detoxifying enzyme systems in rat liver and lung than the S-isomer.

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*.

Cat. No.	Product Name

HY-L037

Antioxidant Compound Library	1240 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 1240 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.

Antioxidant Compound Library

1240 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 1240 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	672 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 672 small molecule compounds that can be used in the research of NF-κB signaling pathway or high throughput screening (HTS) related drug discovery.

NF-κB Signaling Compound Library

672 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 672 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	509 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 509 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

509 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 509 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	Target	Category