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Keap1-Nrf2 protein-protein interaction (PPI)

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) Heme Oxygenase (HO) (1) Interleukin Related (1) Keap1-Nrf2 (12)
By Research Areas:	Cancer (3) Inflammation/Immunology (10) Neurological Disease (4)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-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-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-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 .

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 IC₅₀*s 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-173187

Keap1-Nrf2-IN-27	Keap1-Nrf2	Inflammation/Immunology
Keap1-Nrf2-IN-27 (compound 1C) is a inhibitor of **Keap1-Nrf2 protein-protein interaction (PPI) with K_D2** value of 0.119 μM. Keap1-Nrf2-IN-27 suppresses the expression of pro-inflammatory cytokine TNF-α and IL-6 in the LPS-induced RAW264.7 cell model .

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) .

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-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 .

Cat. No.	Product Name

HY-L109

Protein-protein Interaction Inhibitor Library	672 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 672 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

672 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 672 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.

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

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