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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
621 Results for "
Inhibitor development
" in MedChemExpress (MCE) Product Catalog:
Products (621)
621 Results for "Inhibitor development" in MCE Product Catalog:
Cat. No.: HY-L128
187 compounds
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation.
Although there are more than 600 E3 ubiquitin ligases, only several with small molecule ligands have been used for designing PROTACs, including Skp1-Cullin-F box complex containing Hrt1 (SCF), Von Hippel-Lindau tumor suppressor (VHL), Cereblon (CRBN), inhibitor of apoptosis proteins (IAPs), and mouse double minute 2 homolog (MDM2).
MCE carefully prepared a unique collection of 187 ligands for E3 ligase, which have been reported to be used in PROTAC design. MCE E3 ligase ligand library is a useful tool for PROTAC development.
Cat. No.: HY-B2035
CAS No.: 51218-49-6
Target:
Herbicide Environmental Pollutants Caspase Cytochrome P450 MDM-2/p53 Interleukin Related Reactive Oxygen Species (ROS) Apoptosis
Research Areas:
Pretilachlor is a chloroacetamide herbicide with biological activities including endocrine disruption, oxidative stress induction, apoptosis induction, and immunotoxicity. Pretilachlor exerts its effects by interfering with hormone metabolism, inducing oxidative stress, activating apoptotic pathways, and inhibiting immune functions. Pretilachlor upregulates the transcription of P53, Mdm2, and Bbc3, and increases the activities of Caspase3 and Caspase9; it upregulates the transcription of genes in the HPG/HPT axis and the activity of aromatase; it induces oxidative stress, elevates ROS levels, and upregulates CAT, SOD, and GPX. Pretilachlor downregulates the transcription of CXCL-C1C, IL-1β, and IL-8. Pretilachlor disrupts the normal physiological processes and embryonic development of fish, exhibiting significant toxicity. Pretilachlor can be used in studies related to weeding, environmental pollution, and behavioral toxicity in fish .
Cat. No.: HY-L231
25 compounds
The TCA cycle (tricarboxylic acid cycle)—is also known as the Krebs cycle or the citric acid cycle (CAC). The TCA cycle is a series of chemical reactions that release stored energy through the oxidation of acetyl-CoA in carbohydrates, fats, and proteins.
For decades, the TCA cycle has been considered as the central pathway for cell oxidative phosphorylation to produce energy and biosynthesis. Research shows that TCA cycle is associated with many diseases, especially cancer. In colon carcinoma, liver cancer and other cancers, there are mutations that lead to the imbalance of TCA cycle metabolites, indicating that TCA cycle may be related to the occurrence of cancer. Understanding the role and molecular mechanism of TCA cycle in inhibiting or promoting cancer progression will promote the development of new metabolite-based cancer treatment methods in the future.
MCE supplies a unique collection of 25 key intermediates of the TCA cycle, which can be utilized for TCA-related research and metabolomics identification studies.
Target:
Research Areas:
Bovine Factor Xa is a serine protease that plays a central role in blood coagulation, with prothrombin as its physiological substrate. Bovine Factor Xa catalyzes the conversion of prothrombin to thrombin, activates factor VIII, and hydrolyzes peptide, thioester, and amide substrates. Bovine Factor Xa cleaves protease-activated receptors 1 and 2 to activate intracellular signal transduction. Bovine Factor Xa regulates multiple cellular pathways, mediates various cellular activities, tissue remodeling and cancer cell migration, and inhibits apoptosis in some cancer cells. Bovine Factor Xa protects hippocampal neurons against glutamate-induced damage. Bovine Factor Xa participates in embryonic vascular development and regulates immune hematopoiesis; its activity is inhibited by soybean trypsin inhibitor, and cannot be enhanced by phospholipids. Bovine Factor Xa regulates immune responses and macrophage polarization, and participates in fibrosis, vascular remodeling and tumor progression through non-coagulant effects. Bovine Factor Xa can be used in research related to atherosclerosis, fibrosis, asthma, cancer, thromboinflammation, sepsis, etc .
Target:
Canine Factor Xa is a serine protease that plays a central role in blood coagulation, with prothrombin as its physiological substrate. Canine Factor Xa catalyzes the conversion of prothrombin to thrombin, activates factor VIII, and hydrolyzes peptide, thioester, and amide substrates. Canine Factor Xa cleaves protease-activated receptors 1 and 2 to activate intracellular signal transduction. Canine Factor Xa regulates multiple cellular pathways, mediates various cellular activities, tissue remodeling and cancer cell migration, and inhibits apoptosis in some cancer cells. Canine Factor Xa protects hippocampal neurons against glutamate-induced damage. Canine Factor Xa participates in embryonic vascular development and regulates immune hematopoiesis; its activity is inhibited by soybean trypsin inhibitor, and cannot be enhanced by phospholipids. Canine Factor Xa regulates immune responses and macrophage polarization, and participates in fibrosis, vascular remodeling and tumor progression through non-coagulant effects. Canine Factor Xa can be used in research related to atherosclerosis, fibrosis, asthma, cancer, thromboinflammation, sepsis, etc .
Target:
Porcine Factor Xa is a serine protease that plays a central role in blood coagulation, with prothrombin as its physiological substrate. Porcine Factor Xa catalyzes the conversion of prothrombin to thrombin, activates factor VIII, and hydrolyzes peptide, thioester, and amide substrates. Porcine Factor Xa cleaves protease-activated receptors 1 and 2 to activate intracellular signal transduction. Porcine Factor Xa regulates multiple cellular pathways, mediates various cellular activities, tissue remodeling and cancer cell migration, and inhibits apoptosis in some cancer cells. Porcine Factor Xa protects hippocampal neurons against glutamate-induced damage. Porcine Factor Xa participates in embryonic vascular development and regulates immune hematopoiesis; its activity is inhibited by soybean trypsin inhibitor, and cannot be enhanced by phospholipids. Porcine Factor Xa regulates immune responses and macrophage polarization, and participates in fibrosis, vascular remodeling and tumor progression through non-coagulant effects. Porcine Factor Xa can be used in research related to atherosclerosis, fibrosis, asthma, cancer, thromboinflammation, sepsis, etc .
Target:
Porcine Factor Xa is a serine protease that plays a central role in blood coagulation, with prothrombin as its physiological substrate. Porcine Factor Xa catalyzes the conversion of prothrombin to thrombin, activates factor VIII, and hydrolyzes peptide, thioester, and amide substrates. Porcine Factor Xa cleaves protease-activated receptors 1 and 2 to activate intracellular signal transduction. Porcine Factor Xa regulates multiple cellular pathways, mediates various cellular activities, tissue remodeling and cancer cell migration, and inhibits apoptosis in some cancer cells. Porcine Factor Xa protects hippocampal neurons against glutamate-induced damage. Porcine Factor Xa participates in embryonic vascular development and regulates immune hematopoiesis; its activity is inhibited by soybean trypsin inhibitor, and cannot be enhanced by phospholipids. Porcine Factor Xa regulates immune responses and macrophage polarization, and participates in fibrosis, vascular remodeling and tumor progression through non-coagulant effects. Porcine Factor Xa can be used in research related to atherosclerosis, fibrosis, asthma, cancer, thromboinflammation, sepsis, etc .
Target:
Rat Factor Xa is a serine protease that plays a central role in blood coagulation, with prothrombin as its physiological substrate. Rat Factor Xa catalyzes the conversion of prothrombin to thrombin, activates factor VIII, and hydrolyzes peptide, thioester, and amide substrates. Rat Factor Xa cleaves protease-activated receptors 1 and 2 to activate intracellular signal transduction. Rat Factor Xa regulates multiple cellular pathways, mediates various cellular activities, tissue remodeling and cancer cell migration, and inhibits apoptosis in some cancer cells. Rat Factor Xa protects hippocampal neurons against glutamate-induced damage. Rat Factor Xa participates in embryonic vascular development and regulates immune hematopoiesis; its activity is inhibited by soybean trypsin inhibitor, and cannot be enhanced by phospholipids. Rat Factor Xa regulates immune responses and macrophage polarization, and participates in fibrosis, vascular remodeling and tumor progression through non-coagulant effects. Rat Factor Xa can be used in research related to atherosclerosis, fibrosis, asthma, cancer, thromboinflammation, sepsis, etc .
Research Areas:
5'-ODMT cEt N-Bz A Phosphoramidite (Amidite) is a nucleoside phosphoramidite monomer used to synthesize locked nucleic acid (LNA) analog oligonucleotides. It can be used as a building block of antisense oligonucleotides (ASOs) to target complementary RNA sequences. 5'-ODMT cEt N-Bz A Phosphoramidite (Amidite) locks the furanose ring into an N-type conformation through 2',4'-constrained ethyl (cEt) modification, enhancing hybridization affinity and mismatch discrimination with RNA, while significantly improving the resistance of oligonucleotides to exonuclease digestion. 5'-ODMT cEt N-Bz A Phosphoramidite (Amidite) mediates RNase H-dependent mRNA degradation or inhibits translation by forming a stable hybrid with RNA, thereby achieving gene expression regulation. 5'-ODMT cEt N-Bz A Phosphoramidite (Amidite) is mainly used in the development of antisense drugs, gene function research and oligonucleotide synthesis related to disease treatment .
Cat. No.: HY-B2035R
CAS No.: 51218-49-6
Target:
Reference Standards Herbicide Cytochrome P450 Interleukin Related Apoptosis Reactive Oxygen Species (ROS) Caspase MDM-2/p53 Environmental Pollutants
Research Areas:
Pretilachlor (Standard) is the analytical standard of Pretilachlor (HY-B2035). This product is intended for research and analytical applications. Pretilachlor is a chloroacetamide herbicide with biological activities including endocrine disruption, oxidative stress induction, apoptosis induction, and immunotoxicity. Pretilachlor exerts its effects by interfering with hormone metabolism, inducing oxidative stress, activating apoptotic pathways, and inhibiting immune functions. Pretilachlor upregulates the transcription of P53, Mdm2, and Bbc3, and increases the activities of Caspase3 and Caspase9; it upregulates the transcription of genes in the HPG/HPT axis and the activity of aromatase; it induces oxidative stress, elevates ROS levels, and upregulates CAT, SOD, and GPX. Pretilachlor downregulates the transcription of CXCL-C1C, IL-1β, and IL-8. Pretilachlor disrupts the normal physiological processes and embryonic development of fish, exhibiting significant toxicity. Pretilachlor can be used in studies related to weeding, environmental pollution, and behavioral toxicity in fish .
Cat. No.: HY-P991200
Cat. No.: HY-L945
74 compounds
Sulfonyl fluoride (-SO₂F) overcomes the poor target selectivity of traditional covalent warheads that rely heavily on cysteine. With high stability and tunable electrophilicity under physiological conditions, it targets multiple nucleophilic residues including Lys, Tyr, Ser and His, offering expanded druggable space, lower off-target risks and prolonged efficacy. It is widely used in covalent inhibitors, molecular glues, PROTACs and chemical probes.
MCE has built a highly diverse sulfonyl fluoride fragment library with 1,162 structurally diverse, drug-like fragments. Designed for balanced reactivity, stability and compatibility, these molecules feature tunable electrophilicity, simple scaffolds and high derivatization potential. Combined with SuFEx click chemistry, the library enables efficient modular modification and rapid structure optimization.
Ideal for targeting non-cysteine residues, this library improves covalent screening and probe development efficiency, serving as a precise tool for early-stage covalent drug discovery and chemical biology research.
L-lysine (10 mg/kg) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity . In Vivo:L-lysine (10?mg/kg, p.o., pre-treated or post-treated, administration duration 15 days) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity in acute pancreatitis mice model . L-lysine (5 or 10?mg/kg, p.o., 45 days) ameliorates sepsis-induced acute lung injury in a lipopolysaccharide (HY-D1056)-induced mouse model .
Cat. No.: HY-L058
1,379 compounds
Glycolysis is a series of metabolic processes by which one molecule of glucose is catabolized to two molecules of pyruvate with a net gain of two ATP. Glycolysis takes place in 10 steps and catalyzed by a series of enzyme, such as hexokinase, Glucose-6-phosphate isomerase, Phosphofructokinase, etc. Glycolysis is used by all cells in the body for energy generation.
Most cancer cells exhibit increased glycolysis and use this metabolic pathway for generation of ATP as a main source of their energy supply. This phenomenon is known as the Warburg effect and is considered as one of the most fundamental metabolic alterations during malignant transformation. Because increased aerobic glycolysis is commonly seen in a wide spectrum of human cancers, development of novel glycolytic inhibitors as a new class of anticancer agents is likely to have broad therapeutic applications.
MCE provides a unique collection of 1,379 glycolysis compounds that mainly target hexokinase, glucokinase, enolase, pyruvate kinase, PDHK, etc. MCE Glycolysis Compound Library is a useful tool for glucose metabolism research and anti-cancer drug discovery.
Cat. No.: HY-L133
446 compounds
Copper is an important co-factor of all biological enzymes, but if the concentration exceeds the threshold of maintaining the homeostasis mechanism, copper will lead to cytotoxicity. This death mechanism has been named "Cuproptosis".
The mechanism of cuproptosis distinct from all other known mechanisms of regulated cell death, including apoptosis, pyroptosis, necroptosis, and ferroptosis.
Copper combine with the lipoylated components of the tricarboxylic acid cycle (TCA), leading to lipoylated protein aggregation and subsequent loss of iron-sulfur cluster proteins, ultimately resulting in protein toxicity stress and cell death. Studies have shown that the necessary factors for cuproptosis include the presence of glutathione, mitochondrial metabolism of galactose and pyruvate, and glutamine metabolism.
Targeted regulation of cuproptosis is a potential choice to treat cancer, rheumatoid arthritis, and other diseases. For example, up-regulation of LIPT1 may inhibit the occurrence and development of tumors by destroying TCA in mitochondria and then inducing cuproptosis.
MCE supplies a unique collection of 446 cuproptosis-related compounds, all of which act on the targets or signaling pathways related to cuproptosis and may have in inhibitory or activated effect on cuproptosis. MCE Cuproptosis Library is a useful tool for drug research related to cancer, rheumatoid arthritis, and other diseases.
Cat. No.: HY-P992056
Cat. No.: HY-W587733
CAS No.: 1662-06-2
Synonyms: 17,20β-P; 17,20β-DHP
Research Areas:
17α,20β-Dihydroxy-4-pregnen-3-one (17,20β-P; 17,20β-DHP) acts as the maturation-inducing hormone (MIH) in salmonid fish and rainbow trout. 17α,20β-Dihydroxy-4-pregnen-3-one binds to oocyte-specific plasma membrane receptors and pertussis toxin-sensitive inhibitory G proteins in fish, inhibits Adenylate Cyclase and reduces intracellular cAMP via the membrane receptor-G protein coupling pathway, thereby initiating downstream signal transduction. 17α,20β-Dihydroxy-4-pregnen-3-one induces de novo synthesis of cyclin B, mediates the translation of cyclin B mRNA and the phosphorylation of cdc2, and promotes the production of maturation-promoting factor (MPF). 17α,20β-Dihydroxy-4-pregnen-3-one drives meiotic maturation of fish oocytes. 17α,20β-Dihydroxy-4-pregnen-3-one is applicable for development-related research .
Cat. No.: HY-L249
6,182 compounds
Protein lactylation, an emerging post-translational modification identified in recent years, plays a critical role in linking cellular metabolic reprogramming, epigenetic regulation, and signaling networks. Based on a systematic framework encompassing lactate metabolism, lactylation, and downstream signaling pathways, this compound library comprehensively targets multiple regulatory layers, including histone modification enzymes (such as p300 and HDACs), key glycolytic enzymes (such as PKM2, LDHA, and GAPDH), transcriptional regulators (such as STAT3, HMGB1, and p53), as well as central signaling pathway nodes including HIF-1α, NF-κB, and PI3K-AKT-mTOR. This integrated design enables a comprehensive representation of the regulatory roles of lactylation across the “metabolism–epigenetics–signaling” axis.
MCE has assembled a collection of 6,182 known bioactive compounds and potential functional molecules, making this library suitable for a wide range of applications, including high-throughput drug screening, inhibitor identification, and mechanistic studies. It can be used to systematically evaluate the functional roles of lactylation in biological processes such as tumor metabolism, immune regulation, and inflammatory responses, and to efficiently identify small-molecule candidates with regulatory potential, thereby facilitating the development of innovative therapeutics targeting the interplay between metabolism and epigenetic regulation.
Cat. No.: HY-L073
394 compounds
Hepatitis C virus (HCV) is a hepatotropic enveloped positive- strand RNA virus (family Flaviviridae) that infects the parenchymal cells of the liver. HCV infection is a significant public health burden. Globally, an estimated 71 million people have chronic hepatitis C virus infection. A significant number of those who are chronically infected will develop cirrhosis or liver cancer. To date, there is no vaccine against HCV, and combination pegylated alpha interferon (pIFN-) and ribavirin, the main standard-of-care treatment for HCV, is effective in only a subset of patients and is associated with a wide spectrum of toxic side effects and complications. More recently, new therapeutic approaches that target essential components of the HCV life cycle have been developed, including direct-acting antiviral (DAA) that specifically block a viral enzyme or functional protein and host-targeted agents (HTA) that block interactions between host proteins and viral components that are essential to the viral life cycle. However, the genetic diversity of HCV viruses and the stage of liver disease (i.e., cirrhosis) are revealing themselves as obstacles for effective, pan-genotypic treatments. There still exists a need for the discovery and development of new HCV inhibitors. In particular, since the future of HCV therapy will likely consist of a cocktail approach using multiple inhibitors that target different steps of infection, new antivirals targeting all steps of the viral infection cycle.
MCE offers a unique collection of 394 compounds with identified and potential anti-HCV activity. MCE Anti- Hepatitis C Virus Compound Library is a useful tool for discovery new anti-HCV drugs and other anti-infection research.
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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
