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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
2741 Results for "
Complexation
" in MedChemExpress (MCE) Product Catalog:
Products (2741)
2741 Results for "Complexation" in MCE Product Catalog:
Referencia número: HY-169134
Target:
Áreas de investigación:
PROTAC 20S proteasome subunit β5 degrader 1 is a PROTAC degrader targeting the 20S proteasome subunit β5, with a DC50 of 0.11 μM. PROTAC 20S proteasome subunit β5 degrader 1 forms a ternary complex with the CRBN E3 ligase, induces ubiquitination of the 20S proteasome subunit β5, and promotes its degradation via the proteasomal pathway. PROTAC 20S proteasome subunit β5 degrader 1 disrupts cell cycle progression, promotes apoptosis, and inhibits cell proliferation and migration. PROTAC 20S proteasome subunit β5 degrader 1 exhibits significant proliferation-inhibitory activity against various tumor cells, suppresses tumor growth in in vivo xenograft models, and overcomes the resistance of multiple myeloma cells to Bortezomib (HY-10227). PROTAC 20S proteasome subunit β5 degrader 1 can be used in studies related to pharyngeal cancer and drug-resistant multiple myeloma .
Referencia número: HY-187396
Target:
Áreas de investigación:
FD1-C10-CB is a PROTAC degrader targeting the BRD4 protein. FD1-C10-CB binds to FEM1B to form a ternary complex with BRD4, achieving FEM1B-dependent degradation of BRD4 via the ubiquitin-proteasome system. FD1-C10-CB binds to CD36 to mediate endocytic cellular delivery, thereby enhancing its degrading activity. FD1-C10-CB mediates protein degradation through the Cullin-dependent ubiquitin-proteasome pathway, rather than the lysosomal autophagy pathway. FD1-C10-CB induces a decrease in BRD4 protein levels, and its degrading activity is competitively inhibited by FL47 or JQ1. FD1-C10-CB can be used in the research of breast cancer and osteosarcoma .
Referencia número: HY-N10508S
No. CAS: 1637678-42-2
Referencia número: HY-N8693
No. CAS: 362472-81-9
Category:
Referencia número: HY-L934
122 compounds
CRBN, namely cereblon, is the substrate recognition subunit of the E3 ubiquitin ligase complex in the ubiquitin-proteasome system. A CRBN ligand library refers to a collection of numerous fragments that can specifically bind to the CRBN protein.
These ligands are mostly designed based on validated CRBN-binding warheads and modified through AI-driven molecular generation optimization systems. They not only include classic lenalidomide-derived structures but also cover novel non-lenalidomide scaffolds. After drug-likeness filtering, these ligands exhibit structural diversity and favorable druggable properties. They can be further optimized and modified to facilitate the development of novel molecular glue degraders, accelerate the discovery of molecular glues that induce interactions between CRBN and new substrate proteins, and enable the exploration of novel CRBN substrates for identifying previously unknown CRBN-binding proteins.
MCE compiles 122 fragments that can specifically bind to the CRBN protein, with molecular weights ranging from 200 to 500. Compounds developed based on the library ligands target multiple disease targets such as cancer and autoimmune diseases, further advancing the development of Molecular Glues and PROTACs therapeutic agents.
Referencia número: HY-L105S
867 compounds
Peptides, composed of amino acids, serve as crucial building blocks for proteins and have gained significant attention in drug development over the past decade. The advancements in production, modification, and analytical technologies have led to a surge in the potential applications of peptides in medicine. Peptides offer a number of advantages over small molecule drugs, including: greater target specificity and efficacy, more predictable metabolic profiles, easier delivery to where they are needed in the body, and fewer side effects. Peptides are increasingly appearing in all branches of medicine as components of innovative drugs, imaging agents, diagnostic agents, and other complex drugs such as peptide-drug conjugates. To date, more than 80 peptide drugs have been approved to treat a variety of diseases, including microbial infections, obesity, anti-diabetes, and cancer, as well as to develop cell targeting platforms and improve cell penetration properties.
MCE designs a unique collection of 867 peptide compounds. HY-L105S is a peptide compound library that can be provided with solution form based on HY-L105, and can be applied to peptides-based drug development.
Referencia número: HY-L142
159 compounds
Tuberculosis (TB), usually caused by bacteria (Mycobacterium tuberculosis), is an infectious disease that mainly affects the lungs. According to the statistics of the World Health Organization (WHO), 10 million people suffer from tuberculosis every year, and 1.5 million people die of tuberculosis every year, which makes tuberculosis the number one killer of infectious diseases.
Tuberculosis can be cured through the standard 6-month course of treatment of four kinds of antibiotics. Common drugs include rifampicin and isoniazid. In some cases, TB bacteria do not respond to standard drugs, that is, patients with drug-resistant tuberculosis. The treatment of drug-resistant tuberculosis takes longer and is more complex. In the face of the resurgence of tuberculosis in the world and the rapid emergence of multi drug resistant tuberculosis, it is very important to develop new anti-tuberculosis drugs or new clinical treatment schemes for existing anti mycobacterium drugs.
MCE supplies a unique collection of 159 compounds with clear anti-tuberculosis activity. MCE Anti-tuberculosis Compound Library is a useful tool for anti-tuberculosis related research and anti-tuberculosis drug development
Referencia número: HY-L034
7,771 compounds
Aging is a complex biological process characterized by functional decline of tissues and organs, structural degeneration, and reduced adaptability and resistance, all of which contribute to an increase in morbidity and mortality caused by multiple chronic diseases, such as Alzheimer's disease, cancer, and diabetes. Many theories, which fall into two main categories: programmed and error theories, have been proposed to explain the process of aging, but neither of them appears to be fully satisfactory. The programmed theories imply that aging relies on specific gene regulation, and the error theories emphasize the internal and environmental damages accumulated to living organisms. The damage theories proposed the nine hallmarks that were generally considered to contribute to the aging process: genomic instability, telomere attrition, epigenetic alterations, loss of proteostasis, deregulated nutrient-sensing, mitochondrial dysfunction, cellular senescence, stem cell exhaustion, and altered intercellular communication.
MCE Anti-Aging Compound Library contains 7,771 compounds, mainly targeting Sirtuin, mTOR, IGF-1R, AMPK, p53, Telomerase, Mitophagy, Mitochondrial Metabolism, COX, Cytochrome P450, Oxidase, etc. This library is a useful tool for anti-aging research.
Referencia número: HY-112847B
No. CAS: 1212012-37-7
Synonyms: (E/Z)-Sulfo-N-succinimidyl oleate sodium
Áreas de investigación:
(E/Z)-Sulfosuccinimidyl oleate sodium is the racemate of (E)-Sulfosuccinimidyl oleate sodium and (Z)-Sulfosuccinimidyl oleate sodium. Sulfosuccinimidyl oleate sodium (Sulfo-N-succinimidyl oleate sodium) is a long-chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate sodium is a potent and irreversible inhibitor of the mitochondrial respiratory chain. Sulfosuccinimidyl oleate sodium binds to the CD36 receptor on the surface of microglial cells. Sulfosuccinimidyl oleate sodium exhibits anti-inflammatory effects .
Referencia número: HY-126051
No. CAS: 1381782-08-6
Synonyms: (-)-Viriditoxin
Category:
Referencia número: HY-184209
Áreas de investigación:
Antifungal agent-163 is an antifungal agent. Antifungal agent-163 inhibits the activity of coenzyme Q-cytochrome C reductase (CoQ-Ccr), thereby disrupting electron transport in the mitochondrial respiratory chain. Antifungal agent-163 induces intracellular ROS accumulation, causes cell membrane damage, and impairs mitochondrial function in *Sublineola* cells. Antifungal agent-163 exhibits control effects against fungal plant diseases. Antifungal agent-163 can be used in the research of sorghum anthracnose .
Referencia número: HY-161806
Target:
Áreas de investigación:
ZXH-8-004 is a DENV E PROTAC degrader with a DC50 value of 0.21 µM in Huh7.5 cells. ZXH-8-004 induces CRBN- and proteasome-dependent degradation of intracellular dengue virus envelope protein. ZXH-8-004 inhibits envelope-mediated membrane fusion during viral entry and reduces the production of infectious dengue virus particles. ZXH-8-004 can be used in studies related to dengue virus infection, Zika virus infection, Japanese encephalitis virus infection, West Nile virus infection, and yellow fever virus infection .
Referencia número: HY-183075
No. CAS: 1648720-01-7
Target:
Áreas de investigación:
ND-011458 is an Antibacterial agent, a QcrB inhibitor, and also an inhibitor of cytochrome bcc:aa3 oxidase function. ND-011458 binds to the QcrB subunit of cytochrome bcc:aa3 oxidase. ND-011458 inhibits ATP formation. When used in combination with Clofazimine (HY-B1046), ND-011458 exhibits bactericidal activity against Mycobacterium abscessus. ND-011458 can be used in studies related to Mycobacterium abscessus pulmonary infections .
Referencia número: HY-186268
No. CAS: 3034180-15-6
Áreas de investigación:
BRD4 ligand-Linker Conjugate 8 is a Target Protein Ligand-Linker Conjugate that can be used in studies related to PROTAC synthesis. BRD4 ligand-Linker Conjugate 8 is applicable for the synthesis of BD-7148 (HY-186267) .
Target:
Áreas de investigación:
BD-9136 is a selective BRD4 PROTAC degrader with a DC50 of 1.2 nM, and exhibits a selectivity of ≥1000-fold over BRD2 and BRD3. BD-9136 preferentially forms a ternary complex with the BD1 domain of BRD4, and downregulates the expression of B7-H4 by disrupting the PR-P300-BRD4 axis. BD-9136 depletes BRD4 protein in tumor tissues, inhibits tumor growth, reduces B7-H4 protein expression, increases CD8+ T cell infiltration, and enhances tumor sensitivity to anti-PD-L1. Degradation of BRD4 by BD-9136 rescues the erythroid differentiation block induced by LSD1 inhibition, and transient administration restores erythroid output while retaining HbF induction. BD-9136 causes no adverse effects in mice at effective doses. BD-9136 can be used in studies related to acute myeloid leukemia, acute lymphoblastic leukemia and breast cancer .
Referencia número: HY-162775
No. CAS: 50566-97-7
Target:
Áreas de investigación:
TST1N-224 is a potent response regulator VraRC inhibitor. TST1N-224 can disrupt VraRC-DNA complex formation (IC50=60.2 μM). TST1N-224 exhibits interference with VraRC binding to its cognate DNA through a fast-on-fast-off binding mechanism (KD=23.4 μM). TST1N-224 predominantly interacts with the α9- and α10-helixes of the DNA-binding domain of VraR. TST1N-224 inhibits the growths of S. aureus (SA; MIC>126 μM), Methicillin-resistant S. aureus (MRSA; MIC>126 μM), and Vancomycin-intermediate S. aureus (VISA; MIC=63 μM). TST1N-224, an antimicrobial agent, evidently enhances the susceptibility of VISA to both Vancomycin (HY-B0671) and Methicillin (HY-B0974) .
Referencia número: HY-179560
Áreas de investigación:
PMV6-PEG4-BI2536 is an RIPTAC-like bifunctional molecule that promotes the formation of the p53 Y220C-PLK1 ternary complex (EC50 = 1.4 μM). PMV6-PEG4-BI2536 causes PLK1 mislocalization and inhibits PLK1 activity, inducing G2/M phase arrest and apoptosis in p53 Y220C-mutant cells, while sparing cells with wild-type TP53. PMV6-PEG4-BI2536 can be used in research on uterine, gastric, pancreatic, prostate, and breast cancers harboring the p53 Y220C mutation. PMV6-PEG4-BI2536 is composed of PMV6 (a p53 Y220C mutant-binding ligand), PEG4 (a linker), and BI2536 (HY-159493) (a PLK inhibitor) .
Referencia número: HY-181413
No. CAS: 3093642-25-9
Áreas de investigación:
PROTAC EZH2 Degrader-44 (compound 60) is a highly efficient PROTAC degrader targeting the EZH2-PRC2 complex. By recruiting the CRBN E3 ligase and relying on the proteasome system, PROTAC EZH2 Degrader-44 simultaneously induces the degradation of core components EZH2, SUZ12 and EED, thereby significantly reducing the levels of H3K27me3 and CARM1. PROTAC EZH2 Degrader-44 exerts antiproliferative effects through a dual mechanism: on the one hand, it triggers mitochondrial dysfunction leading to decreased membrane potential; on the other hand, it strongly promotes apoptosis by regulating Bcl-2 family proteins (upregulating Bax, Caspase-3 and PARP, and downregulating Bcl-2). PROTAC EZH2 Degrader-44 exhibits only extremely low cytotoxicity in human normal mammary epithelial, liver and kidney cells, showing a favorable safety window. PROTAC EZH2 Degrader-44 is an ideal tool molecule for exploring the mechanisms of targeted therapy for triple-negative breast cancer .
Referencia número: HY-W1143867
No. CAS: 2226-71-3
Áreas de investigación:
4’-Phosphopantetheine is an orally active coenzyme A (CoA) precursor. 4’-Phosphopantetheine is membrane-permeable and acts as a CoA precursor, a prosthetic group, and a reactive oxygen species (ROS) inhibitor. 4’-Phosphopantetheine binds covalently to rat liver fatty acid synthase, modifies the conserved serine residue in the PKS/NRPS carrier protein domain, and serves as a substrate for CoA synthase and PPAT. 4’-Phosphopantetheine undergoes non-catalytic exchange on rat liver fatty acid synthase, with a faster turnover rate than that of the enzyme complex, and restores intracellular CoA levels in cells with impaired de novo biosynthesis. 4’-Phosphopantetheine rescues phenotypes induced by CoA deficiency, normalizes PKAN-related biomarkers, restores mitochondrial enzyme activity, and alleviates vascular endothelial damage. 4’-Phosphopantetheine shows biological stability in serum, acts as a prosthetic group and degradation product of ACP, and inhibits the formation of atherosclerotic plaques. 4’-Phosphopantetheine can be used in the research of brain iron accumulation neurodegenerative diseases, pantothenate kinase-associated neurodegeneration, CoASY protein-associated neurodegenerative diseases, coronary heart disease, and atherosclerosis .
Referencia número: HY-L246
1,039 compounds
Tonifying traditional Chinese medicines occupy a central position in the traditional medical system, with their core value lying in the regulation of the body's functional state. Modern pharmacological studies have confirmed that these medicinal materials and their monomeric components possess multiple biological activities, including bidirectional immune regulation, anti-aging and lifespan extension, neuroprotection and cognitive enhancement, as well as hematopoietic and metabolic regulation. According to the traditional Chinese medicine theory of “strengthening the body’s resistance and consolidating the foundation”, tonifying medicines are mainly classified into four major categories: Qi-tonifying, Blood-tonifying, Yin-tonifying, and Yang-tonifying. This compound library strictly follows this classification system for compound collection.
Monomeric compounds derived from traditional Chinese medicines demonstrate excellent drug-like properties. They naturally possess structural diversity and clearly defined pharmacological activities, which help improve screening success rates and make them ideal tools for studying multi-target synergistic effects. This library contains 1,039 compounds, providing a material basis for investigating synergistic interactions among compounds (network pharmacology) and facilitating the development of multi-target therapeutic strategies for complex diseases such as cancer, neurodegenerative disorders, and metabolic syndrome.
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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
