Search Result

Results for "

KEAP1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Aminotransferases (Transaminases) (1) Apoptosis (8) Autophagy (3) Bcl-2 Family (3) Caspase (2) Cholinesterase (ChE) (1) COX (1) Cytochrome P450 (2) Drug Isomer (2) E1/E2/E3 Enzyme (2) Endogenous Metabolite (1) Epigenetic Reader Domain (2) Ferroptosis (5) Fungal (2) GLUT (1) Glutathione Peroxidase (1) HDAC (1) Histone Acetyltransferase (2) Influenza Virus (2) Isotope-Labeled Compounds (1) Keap1-Nrf2 (61) Lactate Dehydrogenase (2) Mitophagy (2) Necroptosis (1) NF-κB (1) NO Synthase (1) p62 (2) PROTACs (2) Reactive Oxygen Species (8) RIP kinase (1) ROS Kinase (2) Small Interfering RNA (siRNA) (3)
By Research Areas:	Cancer (35) Infection (2) Inflammation/Immunology (32) Metabolic Disease (12) Neurological Disease (6)
Click Chemistry:	Azide (1)
Oligonucleotides:	Pre-designed siRNA Sets (2) siRNAs (3)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Recombinant Proteins

Isotope-Labeled Compounds

Antibodies

Click Chemistry

Oligonucleotides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-RS07230

KEAP1 Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
KEAP1 Human Pre-designed siRNA Set A contains three designed siRNAs for KEAP1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

KEAP1 Human Pre-designed siRNA Set A KEAP1 Human Pre-designed siRNA Set A

HY-RS07231

Keap1 Mouse Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Keap1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Keap1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Keap1 Mouse Pre-designed siRNA Set A Keap1 Mouse Pre-designed siRNA Set A

HY-RS07232

Keap1 Rat Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Keap1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Keap1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Keap1 Rat Pre-designed siRNA Set A Keap1 Rat Pre-designed siRNA Set A

HY-159495

Keap1-Nrf2-IN-21	Keap1-Nrf2	Metabolic Disease Cancer
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) ^[1].

HY-170301

Keap1-IN-1	Keap1-Nrf2	Others
Keap1-IN-1 (Compound 27) is the inhibitor for *Keap1, that covalently modifys the Cys151 site in the BTB domain of KEAP1, and interfers with the interaction between Keap-Nrf. Keap1-IN-1 upregulates the mRNA expression of the antioxidant stress element (ARE)-dependent gene NQO1 with an EC₅₀* of 160 nM. Keap1-IN-1 exhibits cytotoxicity in cell U2OS with an EC₅₀ of 527 nM ^[1].

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 ^[1].

HY-P5909

Keap1-Nrf2 probe	Keap1-Nrf2	Cancer
Keap1-Nrf2 probe is a *Keap1-Nrf2* probe ^[1].

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-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 ^[1].

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 ^[1].

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 ^[1].

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 ^[1].

HY-P5480

Keap1-Nrf2-IN-16	Keap1-Nrf2	Others
Keap1-Nrf2-IN-16 is a biological active peptide. (KEAP1 binding 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 ^[1].

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 ^[1].

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 ^[1].

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 ^[1].

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 ^[1].

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 ^[1].

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 not cytotoxic activity in ARPE19 cells ^[1].

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 ^[1].

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 ^[1].

HY-157929

Keap1-Nrf2-IN-19	Keap1-Nrf2	Inflammation/Immunology Cancer
Keap1-Nrf2-IN-19 (compound 33) is an oral active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with the K_d value of 0.0014 μM. Keap1-Nrf2-IN-19 exhibits less than 50% inhibition at 30 μM against hERG and 10 μM against CYPs ^[1].

HY-147548

Keap1-Nrf2-IN-10	Reactive Oxygen Species	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 ^[1].

HY-157928

Keap1-Nrf2-IN-18	Keap1-Nrf2	Inflammation/Immunology
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 (K_D = 0.0029 μM) ^[1].

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 ^[1].

HY-P5909F

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

HY-149508

Nrf2-IN-3	Keap1-Nrf2 Reactive Oxygen Species	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 ^[1].

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 ^[1].

HY-162152

biKEAP1	Keap1-Nrf2	Inflammation/Immunology
biKEAP1 (compound 3) is an inhibitor targeting the dimerKEAP1. biKEAP1 binds to cellular KEAP1 dimers and releases the NRF2 protein sequestered by KEAP1, resulting in immediate activation of NRF2. biKEAP1 also promotes nuclear translocation of NRF2 and directly inhibits proinflammatory cytokine transcription. biKEAP1 can reduce acute inflammation and reduce inflammatory damage in acute inflammation models ^[1].

HY-101140

KI696 10+ 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 ^[1].

HY-P1328A

TAT-14 TFA	Keap1-Nrf2	Others
TAT-14 TFA is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 TFA has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1 ^[1].

HY-111126

K67	p62 Keap1-Nrf2	Cancer
K67 specifically inhibits the interaction between Keap1 and S₃₄₉-phosphorylated p62. K67 prevents p-p62 from blocking the binding of Keap1 and Nrf2. K67 effectively inhibits the proliferation of HCC cultures with high cellular S₃₅₁-phosphorylated p62 by restoring the ubiquitination and degradation of Nrf2 driven by Keap1 ^[1].

HY-124941

7-Deacetylgedunin	Keap1-Nrf2 Reactive Oxygen Species	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 ^[1].

HY-110258

ML334 5+ Cited Publications 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 ^[1] .

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 ^[1] .

HY-P10530

Nrf2 (69-84)	Keap1-Nrf2	Neurological Disease Inflammation/Immunology Cancer
Nrf2 (69-84) is a peptide fragment of Nrf2 protein that contains the key ETGE motif, which is an important region for binding to the Kelch domain of *Keap1* protein. Nrf2 (69-84) can be used to study the role of Nrf2 in the development and progression of diseases, especially in cancer, neurodegenerative diseases and inflammatory diseases ^[1].

HY-139620

MS83	PROTACs	Cancer
MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder.

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 ^[1] .

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 ^[1].

HY-171035

PRL-295	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 ^[1].

HY-13755

Sulforaphane 40+ Cited Publications	HDAC Keap1-Nrf2 Apoptosis Bcl-2 Family Caspase Reactive Oxygen Species	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 ^[1] .

HY-145879

Nrf2 activator-2	Keap1-Nrf2	Cancer
Nrf2 activator-2 (compound O15), a Osthole derivative, is a potent Nrf2 agonist with an EC₅₀ of 2.9 μM in 293 T cells. Nrf2 activator-2 effectively inhibits the interaction between Keap1 and Nrf2, thus showing the activation effect on Nrf2. Nrf2 activator-2 shows a marked decrease in the level of ubiquitinated Nrf2 in cells ^[1].

HY-141439

TBE 31	Keap1-Nrf2	Inflammation/Immunology Cancer
TBE 31 is a potent and orally active *NQO1* inducer with an D_m value of 1.1 nM. TBE 31 also is a potent Nrf2 activator. TBE 31 reacts with cysteines of Keap1, impairing its ability to target nuclear factor-erythroid 2 p45-related factor 2 (Nrf2) for degradation. TBE 31 shows cytoprotective effects ^[1] .

HY-112675

4-Octyl itaconate 50+ Cited Publications	Keap1-Nrf2	Inflammation/Immunology
4-Octyl Itaconate is a cell-permeable Itaconate derivative. Itaconate is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1 ^[1].

HY-120371

CPUY192018 1 Publications Verification	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 ^[1].

HY-124834

Nrf2 activator-10	Keap1-Nrf2 Apoptosis	Cancer
Nrf2 activator-10 (Compound AI-1) is a PI3K-dependent inducer for antioxidant response element (ARE) (EC₅₀ is 2.7 μM) and an activator for Nrf2. Nrf2 activator-10 modifies *Keap1, blocks Cul3-Keap1* ubiquitin ligase complex, activates the transcription of Nrf2. Nrf2 activator-10 protects cells from H₂O₂-induced apoptosis.

HY-156065

S217879	Keap1-Nrf2	Metabolic Disease
S217879 is a highly potent and selective NRF2 activator. S217879 disrupts the KEAP1-NRF2 interaction leading to robust NRF2 pathway activation. S217879 can be used for non-alcoholic steatohepatitis (NASH) research ^[1].

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 ^[1].

HY-W009731

Dibenzoylmethane	Keap1-Nrf2	Metabolic Disease Cancer
Dibenzoylmethane, a minor ingredient in licorice, activates Nrf2 and prevents various cancers and oxidative damage. Dibenzoylmethane, an analog of curcumin, results in dissociation from Keap1 and nuclear translocation of Nrf2 ^[1].

Cat. No.	Product Name

HY-L037

Antioxidant Compound Library

1,739 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 1,739 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

957 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 957 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

656 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 656 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	Research Area

HY-P1328

TAT-14 1 Publications Verification	Keap1-Nrf2	Others
TAT-14 is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1 ^[1].

HY-P5909

Keap1-Nrf2 probe	Keap1-Nrf2	Cancer
Keap1-Nrf2 probe is a *Keap1-Nrf2* probe ^[1].

HY-P5480

Keap1-Nrf2-IN-16	Keap1-Nrf2	Others
Keap1-Nrf2-IN-16 is a biological active peptide. (KEAP1 binding activity)

HY-P5909F

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

HY-P1328A

TAT-14 TFA	Keap1-Nrf2	Others
TAT-14 TFA is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 TFA has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1 ^[1].

HY-P10530

Nrf2 (69-84)	Keap1-Nrf2	Neurological Disease Inflammation/Immunology Cancer
Nrf2 (69-84) is a peptide fragment of Nrf2 protein that contains the key ETGE motif, which is an important region for binding to the Kelch domain of *Keap1* protein. Nrf2 (69-84) can be used to study the role of Nrf2 in the development and progression of diseases, especially in cancer, neurodegenerative diseases and inflammatory diseases ^[1].

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-13755

Sulforaphane 40+ Cited Publications	Structural Classification Natural Products other families Classification of Application Fields Source classification Plants Inflammation/Immunology Disease Research Fields	HDAC Keap1-Nrf2 Apoptosis Bcl-2 Family Caspase Reactive Oxygen Species
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 ^[1] .

HY-W009731

Dibenzoylmethane	Structural Classification Classification of Application Fields Leguminosae Ketones, Aldehydes, Acids Source classification Metabolic Disease Plants Glycyrrhiza uralensis Fisch. Disease Research Fields	Keap1-Nrf2
Dibenzoylmethane, a minor ingredient in licorice, activates Nrf2 and prevents various cancers and oxidative damage. Dibenzoylmethane, an analog of curcumin, results in dissociation from Keap1 and nuclear translocation of Nrf2 ^[1].

HY-131592

Tricetin 1 Publications Verification	Flavonols Flavonoids Cupressaceae Classification of Application Fields Neurological Disease Thuja occidentalisLinn. Source classification Plants Disease Research Fields Inflammation/Immunology	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 ^[1].

HY-N0005

Curcumin Maximum Cited Publications 79 Publications Verification Diferuloylmethane; Natural Yellow 3; Turmeric yellow	Structural Classification Classification of Application Fields Anti-aging Source classification Plants Food Research Microorganisms Sunscreen Phenols Polyphenols Pigments Cosmetic Research Curcuma longa Disease Research Fields Zingiberaceae Cancer	Histone Acetyltransferase Epigenetic Reader Domain Keap1-Nrf2 Autophagy Mitophagy Influenza Virus Ferroptosis
Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.

HY-13755A

(R)-Sulforaphane L-Sulforaphane	Structural Classification Natural Products other families Classification of Application Fields Source classification Plants Disease Research Fields Cancer	Keap1-Nrf2 Bcl-2 Family Caspase Reactive Oxygen Species 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 ^[1] .

HY-124941

7-Deacetylgedunin	Structural Classification Natural Products Toona sinensis (A. Juss.) Roem. Source classification Plants Meliaceae	Keap1-Nrf2 Reactive Oxygen Species
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 ^[1].

HY-N10313

Dehydrobruceine B	Structural Classification 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* ^[1].

HY-W009731R

Dibenzoylmethane (Standard)	Structural Classification Leguminosae Ketones, Aldehydes, Acids Source classification Plants Glycyrrhiza uralensis Fisch.	Keap1-Nrf2
Dibenzoylmethane (Standard) is the analytical standard of Dibenzoylmethane. This product is intended for research and analytical applications. Dibenzoylmethane, a minor ingredient in licorice, activates Nrf2 and prevents various cancers and oxidative damage. Dibenzoylmethane, an analog of curcumin, results in dissociation from Keap1 and nuclear translocation of Nrf2 ^[1].

HY-N8160

Dehydrocurdione	Classification of Application Fields Terpenoids Sesquiterpenes Source classification Plants Curcuma phaeocaulis Valeton Disease Research Fields Inflammation/Immunology Zingiberaceae	Keap1-Nrf2 Reactive Oxygen Species
Dehydrocurdione, a zedoary-derived sesquiterpene, induces heme oxygenase *(HO)-1, an antioxidative enzyme, in RAW 264.7 macrophages. Dehydrocurdione interacts with Keap1*, resulting in Nrf2 translocation followed by activation of the HO-1 E2 enhancer. Dehydrocurdione suppresses lipopolysaccharide-induced NO release, a marker of inflammation. Anti-inflammatory activity ^[1] .

HY-N0005R

Curcumin (Standard)	Structural Classification Microorganisms Source classification Phenols Polyphenols Plants Curcuma longa Zingiberaceae	Histone Acetyltransferase Epigenetic Reader Domain Keap1-Nrf2 Autophagy Mitophagy Influenza Virus Ferroptosis
Curcumin (Standard) is the analytical standard of Curcumin. This product is intended for research and analytical applications. Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.

HY-N0394R

L-Cystine (Standard)	Structural Classification Human Gut Microbiota Metabolites Microorganisms Source classification Amino acids Endogenous metabolite	Endogenous Metabolite Ferroptosis ROS Kinase Keap1-Nrf2
L-Cystine (Standard) is the analytical standard of L-Cystine. This product is intended for research and analytical applications. L-Cystine, the extracellular form of L-Cysteine (HY-Y0337), is a nutritionally dispensable semiessential sulfur-containing amino acid, occurring in proteins of plants and animals. L-Cystine induces Nrf2 protein elevation in a Keap1 (HY-P75897)-dependent manner and activates Nrf2 transcription factor. L-cystine can elicit cytoprotection by reducing ROS generation and protecting against oxidant- or doxorubicin-induced apoptosis. The reduced reabsorption of L-Cystine in renal tubules and its poor solubility in urine are the important causes of cystine precipitation and cystine crystal formation eventually leading to kidney stones. L-Cystine combined with L-theanine (HY-15121) enhances the production of antigen-specific IgG by increasing glutathione (GSH) levels and T helper 2 (Th2) mediated responses in mice. L-Cystine is promising for research of cystinuria and cystinosis ^[1]

HY-19543

Brusatol 25+ Cited Publications NSC 172924	Structural Classification Simaroubaceae Classification of Application Fields Terpenoids Source classification Diterpenoids Plants Disease Research Fields Brucea javanica (L.) Merr. Cancer	Keap1-Nrf2 Apoptosis
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 ^[1]. Brusatol increases cellular apoptosis .

Species:	Human (4) Mouse (1)
Tag:	His (3) SUMO (1) Tag Free (2) GST (1)
Source:	Sf9 insect cells (3) P. pastoris (1) E. coli (1)

Cat. No.	Compare	Product Name	Species	Source

HY-P75897

	KEAP1 Protein, Human (sf9) Kelch-like ECH-associated protein 1; Cytosolic inhibitor of Nrf2; KEAP1; KEAP1	Human	Sf9 insect cells
	KEAP1 in the BCR E3 ubiquitin ligase complex complex regulates cellular responses to oxidative stress by ubiquitinating NFE2L2/NRF2. As an oxidative stress sensor, KEAP1 normally promotes NFE2L2/NRF2 degradation. KEAP1 Protein, Human (sf9) is the recombinant human-derived KEAP1 protein, expressed by Sf9 insect cells , with tag free. The total length of KEAP1 Protein, Human (sf9) is 623 a.a..

HY-P75899

	KEAP1 Protein, Human (sf9, His-GST) Kelch-like ECH-associated protein 1; Cytosolic inhibitor of Nrf2; KEAP1; KEAP1	Human	Sf9 insect cells
	KEAP1 in the BCR E3 ubiquitin ligase complex complex regulates cellular responses to oxidative stress by ubiquitinating NFE2L2/NRF2. As an oxidative stress sensor, KEAP1 normally promotes NFE2L2/NRF2 degradation. KEAP1 Protein, Human (sf9, His-GST) is the recombinant human-derived KEAP1 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. The total length of KEAP1 Protein, Human (sf9, His-GST) is 623 a.a., with molecular weight of ~109 kDa.

HY-P702829

	KEAP1 Protein, Mouse (His, SUMO) Kelch-like ECH-associated protein 1; Cytosolic inhibitor of Nrf2; KEAP1; KEAP1	Mouse	E. coli
	KEAP1 in the BCR E3 ubiquitin ligase complex complex regulates cellular responses to oxidative stress by ubiquitinating NFE2L2/NRF2. As an oxidative stress sensor, KEAP1 normally promotes NFE2L2/NRF2 degradation. KEAP1 Protein, Mouse (His, SUMO) is the recombinant human-derived KEAP1 protein, expressed by E. coli , with N-6*His, N-SUMO.

HY-P701249

	KEAP1 Protein, Human (P.pastoris, His) 1 Publications Verification Kelch-like ECH-associated protein 1; Cytosolic inhibitor of Nrf2; KEAP1; KEAP1	Human	P. pastoris
	KEAP1 in the BCR E3 ubiquitin ligase complex complex regulates cellular responses to oxidative stress by ubiquitinating NFE2L2/NRF2. As an oxidative stress sensor, KEAP1 normally promotes NFE2L2/NRF2 degradation. KEAP1 Protein, Human (P.pastoris, His) is the recombinant human-derived KEAP1 protein, expressed by P. pastoris , with N-6*His labeled tag. The total length of KEAP1 Protein, Human (P.pastoris, His) is 624 a.a., with molecular weight of 71.7 kDa.

HY-P75897Y

	KEAP1 Protein, Human (sf9, solution) Kelch-like ECH-associated protein 1; Cytosolic inhibitor of Nrf2; KEAP1; KEAP1	Human	Sf9 insect cells
	KEAP1 in the BCR E3 ubiquitin ligase complex complex regulates cellular responses to oxidative stress by ubiquitinating NFE2L2/NRF2. As an oxidative stress sensor, KEAP1 normally promotes NFE2L2/NRF2 degradation. KEAP1 Protein, Human (sf9) is the recombinant human-derived KEAP1 protein, expressed by Sf9 insect cells , with tag free. The total length of KEAP1 Protein, Human (sf9) is 623 a.a., with molecular weight of ~64 kDa.

Compare Products


Products	In-stock - + Add to Cart
Cat. No.
Species
Source
Tag
Accession
Gene ID
Molecular Weight
Purity
Endotoxin Level
Biological Activity
Appearance
Formulation
Storage & Stability
Shipping
Free Sample	Yes No
Size	* This product has been "discontinued". Optimized version of product available: / In-stock - + Add to Cart Get quote

Cat. No.	Product Name	Chemical Structure

HY-112675S

4-Octyl itaconate-13C5-1
4-Octyl itaconate- ¹³C₅-1 is ¹³C-labeled 4-Octyl itaconate (HY-112675). Itaconate is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1.

Cat. No.	Compare	Product Name	Application	Reactivity

HY-P80732

	Keap1 Antibody 1 Publications Verification INrf2; KLHL19	WB, IHC-P	Human, Mouse
	Keap1 Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 70 kDa, targeting to Keap1. It can be used for WB,IHC-P assays with tag free, in the background of Human, Mouse.