Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
18 Results for "
keap1-nrf2-in-1
" in MedChemExpress (MCE) Product Catalog:
Products (18)
18 Results for "keap1-nrf2-in-1" in MCE Product Catalog:
77
3
3 Cited Publications
Target:
Research Areas:
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 .
2
2 Cited Publications
Synonyms: L-Sulforaphane
2
Research Areas:
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 .
Cat. No.: HY-173444
CAS No.: 2989934-63-4
Target:
Research Areas:
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 .
Cat. No.: HY-W701218
CAS No.: 836682-32-7
Cat. No.: HY-175833
Target:
NF-κB Keap1-Nrf2 Heme Oxygenase (HO) Interleukin Related TNF Receptor Reactive Oxygen Species (ROS) SOD
Research Areas:
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) .
Cat. No.: HY-W505984
CAS No.: 957942-34-6
Synonyms: KM05073
Target:
Research Areas:
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 .
Cat. No.: HY-176146
Target:
Research Areas:
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 .
Cat. No.: HY-124941
CAS No.: 10314-90-6
Cat. No.: HY-P5909
CAS No.: 2430031-36-8
Target:
Research Areas:
Cat. No.: HY-170761
CAS No.: 3108079-75-7
Target:
Research Areas:
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.: HY-168709
Target:
Research Areas:
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 .
Cat. No.: HY-161643
CAS No.: 2671859-87-1
Target:
Research Areas:
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 .
Cat. No.: HY-180155
CAS No.: 3105470-83-2
Target:
Keap1-Nrf2 Cholinesterase (ChE) Interleukin Related TNF Receptor Reactive Oxygen Species (ROS) Heme Oxygenase (HO) Quinone Reductase
Research Areas:
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 Ki 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 .
Cat. No.: HY-187219
Research Areas:
CX-Se13 is an orally active pulmonary fibrosis inhibitor with anti-inflammatory and antioxidant activities. CX-Se13 regulates the Keap1/Nrf2/HO-1/NQO1, YAP/TAZ-TEAD, NF-κB p65 and TGF-β/Smads signaling pathways. CX-Se13 activates the cellular antioxidant defense system, restores redox balance, alleviates inflammatory responses, reduces collagen deposition, decreases pro-inflammatory cytokine levels and inhibits pathological progression. CX-Se13 can be used in studies related to pulmonary fibrosis .
Cat. No.: HY-L109
807 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 807 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.
- 1
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
