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Cat. No. Product Name
  • HY-L149
    7,023 compounds

    A membrane protein is a protein molecule that is attached to or associated with the membrane of a cell or an organelle. Membrane proteins can be classified into two groups based on how the protein is associated with the membrane: integral membrane proteins and peripheral membrane proteins. In humans, about 30% genome encodes membrane proteins. Membrane proteins perform a variety of functions vital to the survival of organisms, for example, signal transduction, molecules or ion transportation, enzymatic catalysis, and intercellular communication. Membrane proteins also play important roles in drug discovery. As reported, more than 60% of current drug targets are membrane proteins.

    MCE supplies a unique collection of 7,023 compounds targeting a variety of membrane proteins. MCE Membrane Protein-targeted Compound Library can be used for membrane protein-focused screening and drug discovery.

  • HY-L150
    4,734 compounds

    Membrane receptors, also known cell surface receptors or transmembrane receptors, are transmembrane proteins embedded into the plasma membrane which play an essential role in maintaining communication between the internal processes within the cell and various types of extracellular signals. They act in cell signaling by receiving (binding to) extracellular molecules, which are also called ligands. These extracellular molecules include hormones, cytokines, growth factors, neurotransmitters, lipophilic signaling molecules such as prostaglandins, and cell recognition molecules.

    There are three kinds of membrane receptors: ion channel-linked receptors, enzyme-linked receptors and G-protein-linked receptors. They play important roles in keeping human normal physiologic processes. GPCRs and ion channels are important drug targets in drug discovery.

    MCE provides a unique collection of 4,734 compounds targeting a variety of membrane receptors. MCE Membrane reeptor-targeted Compound Library can be used for membrane receptor-focused screening and drug discovery.

  • HY-L007
    5,180 compounds

    The immune system is a host defense system comprising many biological structures and processes within an organism that protects against disease. To function properly, an immune system must detect a wide variety of agents, known as pathogens, from viruses to parasitic worms, and distinguish them from the organism's own healthy tissue. Inflammation is also the body's attempt at self-protection to remove harmful stimuli and begin the healing process. It’s part of the body's immune response. The immune system recognizes damaged cells, irritants, and pathogens, and inflammation begins the healing process. Inflammatory abnormalities are a large group of disorders that underlie a vast variety of human diseases. The immune system is often involved with inflammatory disorders, demonstrated in both allergic reactions and some myopathies, with many immune system disorders resulting in abnormal inflammation.

    MCE designs a unique collection of 5,180 compounds that are useful tool for Immunology/Inflammation research or autoimmune inflammatory diseases drug discovery.

  • HY-L099
    2,326 compounds

    MCE Targeted Diversity Library contains 2,326 compounds, covering more than 1000 targets and isoforms, such as GPCRs, Ion channel, variety of kinases, etc. 1-3 compounds with high potency and selectivity were carefully selected for each target and isoform. The bioactivity information of each compound has been clearly reported in the literatures. This library is a concise collection of small molecule compounds with comprehensive target coverage, which can be used for phenotypic screening at low cost.

  • HY-L082
    461 compounds

    A parasite is an organism that lives on or in a host organism and gets its food from or at the expense of its host. Parasites of humans include protozoans, helminths, and ecto-parasites (organisms that live on the external surface of a host). They are responsible for many diseases and are transmitted to their hosts most often through the ingestion of contaminated food, water or through the bite of an arthropod (e.g., a fly or tick), which can act as an intermediate host and as a vector. Parasitic diseases of humans are a major global health problem causing significant morbidity and mortality, especially in developing countries. Each year there are hundreds of millions of people infected with disease-causing parasites, particularly in tropical and subtropical regions of the world, resulting in an estimated one million deaths. Therefore, there is a dire need of novel anti-parasitic drugs.

    MCE has a unique collection of 461 compounds with validated anti-parasitic activity which offer researchers an opportunity to screen novel anti-parasitic targets.

  • HY-L029
    1,398 compounds

    Autophagy is a lysosomal degradation pathway that is essential for cell survival, differentiation, development, and homeostasis. The process of autophagy in mammalian cells is as follows: a portion of cytoplasm, including organelles, is enclosed by a phagophore or isolation membrane to form an autophagosome. The outer membrane of the autophagosome subsequently fuses with the endosome and then the lysosome, and the internal material is degraded. Autophagy plays a wide variety of physiological and pathophysiological roles. Defective autophagy contributes to various pathologies, including infections, cancer, neurodegeneration, aging, and heart disease.

    MCE provides a unique collection of 1,398 autophagy pathway-related compounds that is a useful tool for the research of autophagy-related regulation and diseases.

  • HY-L104
    671 compounds

    The lack of availability of appropriate medicines for children is an extensive and urgent problem. A variety of obstacles hinder children's drug development, including the limited commercial interest, lack of suitable infrastructure and competence for conducting paediatric clinical trials, difficulties in trial design, ethical worries and many others. Because of these factors, unlicensed and off-label prescribing is very common in children which may lead to safety concern.

    MCE offers a unique collection of 671 children’s medicines, all of which have been approved or studied in clinical trials for children diseases. MCE children’s drug library is a useful tool for drug repurposing to discover new children’s indications.

  • HY-L006
    2,349 compounds

    GPCRs are a large family of cell surface receptors that respond to a variety of external signals. Binding of a signaling molecule to a GPCR results in G protein activation, which in turn triggers the production of any number of second messengers. GPCRs play an important role in the human body, and increased understanding of these receptors has greatly affected modern medicine. In fact, researchers estimate that between one-third to one-half of all approved drugs act by binding to GPCRs. GPCRs are a large group of drug targets in drug discovery.

    MCE provides a unique collection of 2,349 small molecules targeting GPCRs that can be used in the screening for various GPCRs-related research and drug development projects.

  • HY-L126
    681 compounds

    Nuclear receptors (NR) are proteins found in cells that sense androgen and thyroid hormones and certain other molecules. They are ligand-activated transcription factors that participate in many aspects of human physiology and pathology, and regulate the expression of various important genes.

    Nuclear receptors have become one of the main targets in the development of new drug strategies, providing a unique type of receptors for studying a variety of human diseases, such as breast cancers, skin disorders and diabetes. 13% of U.S. Food and Drug Administration (FDA) approved drugs target nuclear receptors.

    MCE supplies a unique collection of 681 nuclear receptor inhibitors and activators, all of which have the identified inhibitory or activated effect on nuclear receptor. MCE Nuclear Receptor Library is a useful tool for drugs research related to cancer, skin disease and diabetes.

  • HY-L097
    52 compounds

    Animal disease models are used in a variety of settings in basic research, such as studies on mechanisms of disease progression and evaluation new drugs. Animal models can be broadly classified into five categories: 1) experimental, 2) spontaneous, 3) negative, 4) orphan, 5) genetically engineered. Experimental models, which are induced artificially in the laboratory, are most common. Some small molecular compounds are usually used as inducers for animal models, such as Ceruletide for inflammatory model, Azoxymethane for tumor model. These inducers are useful tool in building animal models.

    MCE offers a unique collection of 52 animal model inducers, involving inflammatory model, tumor model, nervous disease model, etc. MCE Animal Disease Model library is a powerful tool for the establishment of animal disease models.

  • HY-L146
    2,898 compounds

    Metabolism is the set of life-sustaining chemical reactions in organisms that maintain cell homeostasis. Metabolic pathways are enzyme-mediated biochemical reactions that lead to biosynthesis (anabolism) or breakdown (catabolism) of molecules including glucose metabolism, lipid metabolism and amino acid or protein metabolism within a cell or tissue. As catalysts, enzymes are crucial to metabolism as they allow a reaction to proceed more rapidly and tregulate the rate of a metabolic reaction. Due to the importance of metabolic balance in the organism, the abnormal function of metabolic enzymes often leads to the occurrence of a variety of metabolic diseases, such as diabetes, obesity, cardiovascular disease, etc.

    MCE designs a unique collection of 2,898 metabolic enzymes related small molecules, which is an important tool for studying the metabolic activities of organisms and developing drugs for metabolic diseases.

  • HY-L056
    686 compounds

    Terpenoids, also known as isoprenoids, are the most numerous and structurally diverse natural products found in many plants. Terpenoids are divided into monoterpenes, sesquiterpenes, diterpenes, sesterpenes, and triterpenes depending on its carbon units. Several studies, in vitro, preclinical, and clinical have confirmed that this class of compounds displays a wide array of very important pharmacological properties in the fight against cancer, malaria, inflammation, and a variety of infectious diseases. Naturally occurring terpenoids provide new opportunities to discover new drugs with minimum side effects.

    MCE designs a unique collection of 686 terpenoid compounds that all come from natural products. MCE Terpenoids Library is a useful tool for drug discovery that can be used for high throughput screening (HTS) and high content screening (HCS).

  • HY-L094
    2,007 compounds

    The health benefits deriving from the consumption of certain foods have been common knowledge. All foods are made up of chemical substances. Chemicals in foods are largely harmless and often desirable. At present, numerous researchers have been focused on the beneficial role played by certain food components in the close relationship between food intake and health status. For example, polyphenols, a common class of compounds among foods, are well-known antioxidants, which may play a role in the prevention of several diseases including type 2 diabetes, cardiovascular diseases, and some types of cancer.

    MCE supplies a unique collection of 2,007 compounds from variety of foods. All compounds are with specific food source(s). MCE Food-Sourced Compound Library is the useful tool to discover molecules with pharmaceutical activity from foods.

  • HY-L059
    1,271 compounds

    Programmed cell death pathways, including apoptosis, pyroptosis and necroptosis, are regulated by unique sets of host proteins that coordinate a variety of biological outcomes. Pyroptosis is a highly inflammatory form of programmed cell death that occurs most frequently upon infection with intracellular pathogens and is likely to form part of the antimicrobial response. This process promotes the rapid clearance of various bacterial, viral, fungal and protozoan infections by removing intracellular replication niches and enhancing the host's defensive responses. Pyroptosis has been widely studied in inflammatory and infection disease models. Recently, there are growing evidences that pyroptosis also plays an important role in the development of cancer, cardiovascular diseases and Metabolic disorder, etc.

    MCE designs a unique collection of 1,271 pyroptosis-related compounds mainly focusing on the key targets in the pyroptosis signaling pathway and can be used in the research of pyroptosis signal pathway and related diseases.

  • HY-L172
    82 compounds

    Immunity refers to the ability of the body to resist the invasion of pathogenic microorganisms and resist a variety of diseases. Immunocompromised will inevitably lead to a series of diseases. Immunopotentiator are a class of compounds that enhance immune function and induce immune response. Immunopotentiator can activate the proliferation and differentiation of one or more kinds of immune active cells in the body, promote the secretion of lymphocytes, and then enhance the immune function of the body. Immunopotentiator are mainly used in the treatment of tumors, infectious diseases and immunodeficiency diseases. In addition, immunopotentiator are often used as adjuvants in combination with vaccine antigens to enhance the immunogenicity of vaccines.

    MCE designs a unique collection of 82 compounds with definite or potential Immunopotentiating effect, mainly targeting the NOD-like Receptor (NLR), Toll-like Receptor (TLR), NF-κB, etc. It is an effective tool for development and research of anti-cancer, anti-infectious diseases and anti-immunodeficiency diseases compounds.

  • HY-L121
    313 compounds

    5-HT receptors, also called Serotonin receptors, are a group of G protein-coupled receptors (GPCRs) and ligand-gated ion channels (LGICs) found in the central and peripheral nervous systems. These receptors are now classified into seven families, 5-HT1–7, comprising a total of 14 structurally and pharmacologically distinct mammalian 5-HT receptor subtypes. The 5-HT receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, mood, nausea, sleep, andthermoregulation. The serotonin receptors are the target of a variety of pharmaceutical drugs, including many antidepressants, antipsychotics, anorectics, antiemetics, gastroprokinetic agents, antimigraine agents, hallucinogens, and entactogens.

    MCE 5-HT Receptor Compound Library consists of 313 5-HT receptor inhibitors and activators, which can be used for neuropsychiatric disorders drugs discovery.

  • HY-L127
    36 compounds

    Orthopoxvirus is a genus of viruses in the family Poxviridae and subfamily Chordopoxvirinae. The orthopoxvirus genus consists of 12 viruses including variola virus, vaccinia virus (VV), cowpox viruses (CV), monkeypox virus, and camelpox virus. Smallpox has been eradicated worldwide in 1980, but some other orthopoxvirus, such as monkeypox virus, are still threats to human health.

    There are not many drugs available for orthopoxvirus treatment. The only product currently available for treatment of complications of Orthopoxvirus infection is vaccinia immunoglobulin (VIG). In 2021, brincidofovir was approved by FDA for the treatment of smallpox and tecovirimat was approved by EMA for the treatment of monkeypox in 2022. A few active compounds including interferon and interferon inducers, and a variety of nucleosides or nucleotides have been reported to have activity against orthopoxvirus.

    MCE carefully prepared a unique collection of 36 compounds reported with the anti- orthopoxvirus activity which can be used for drug screening and other research about orthopoxvirus.

  • HY-L032
    22,500 compounds

    Fragment-based drug discovery (FBDD) is well suited for discovering both drug leads and chemical probes of protein function; it can cover broad swaths of chemical space and allows the use of creative chemistry. Fragment-based drug discovery is well-established in industry and has resulted in a variety of drugs entering clinical trials, with two, vemurafenib and venetoclax, already approved. FBDD also has key attractions for academia. Notably, it is able to tackle difficult or novel targets for which no chemical matter may be found in existing HTS collections.

    MCE designs a unique collection of 22,500 fragment compounds, all of which obey a heuristic rule called the “Rule of Three (RO3) ”, in which molecular weight ≤300 Da, the number of hydrogen bond donors (H-donors) ≤3, the number of hydrogen bond acceptors (H-acceptors) is ≤3 and cLogP is ≤3. This library is an important source of lead-like drugs.

  • HY-L153
    4,566 compounds

    Covalent inhibitors are small molecules that can bind specifically to target proteins through covalent bonds and inhibit their biological functions. Although for a long time, covalent targeting has been playing a subordinate role in drug discovery, with an increasing number of reports on successful clinical applications of such drugs, the potential of these agents is now being acknowledged. Currently, cysteine is the most common covalent amino acid residue in a variety of covalent drugs, and various warheads have been developed that can react with cysteine, providing the key building blocks for covalent drugs to form covalent bonds.

    To meet the development needs of covalent inhibitors targeting cysteine, MCE has designed a unique collection of 4,566 compounds with different covalent warheads that target cysteine. The MCE Cysteine Targeted Covalent Library is designed using the following covalent warheads: Acrylamides, Propiolic acid ester, Dimethylamine functionalized acrylamides, Chloroacetamides, Acrylonitrile, 2-Cyanoacrylamide, Aziridine, Haloacetamide, etc.

  • HY-L012
    4,567 compounds

    Metabolism is the set of life-sustaining chemical reactions in organisms. Metabolic pathways are enzyme-mediated biochemical reactions that lead to biosynthesis (anabolism) or breakdown (catabolism) of natural product small molecules within a cell or tissue. Acting as catalysts, enzymes are crucial to metabolism - they allow a reaction to proceed more rapidly - and they also allow the regulation of the rate of a metabolic reaction. Proteases are used throughout an organism for various metabolic processes. Proteases control a great variety of physiological processes that are critical for life, including the immune response, cell cycle, cell death, wound healing, food digestion, and protein and organelle recycling. Imbalances in metabolic activities have been found to be critical in a number of pathologies, such as cardiovascular diseases, inflammation, cancer, and neurodegenerative diseases.

    MCE designs a unique collection of 4,567 Metabolism/Protease-related small molecules that act as a useful tool for drug discovery of metabolism-related diseases.

  • HY-L068
    522 compounds

    Flavonoids are an important class of natural products; particularly, they belong to a class of plant secondary metabolites having a polyphenolic structure, widely found in fruits, vegetables and certain beverages. Flavonoids can be subdivided into different subgroups depending on the carbon of the C ring on which the B ring is attached and the degree of unsaturation and oxidation of the C ring. These subgroups are: flavones, flavonols, flavanones, flavanonols, flavanols or catechins, anthocyanins and chalcones. Flavonoids are now considered as an indispensable component in a variety of nutraceutical, pharmaceutical, medicinal and cosmetic applications. This is attributed to their anti-oxidative, anti-inflammatory, anti-mutagenic and anti-carcinogenic properties coupled with their capacity to modulate key cellular enzyme function. Naturally occurring flavonoids are known to have biological activities for use as drugs, for example, in diseases like cancer, Alzheimer’s disease (AD), atherosclerosis, etc.

    MCE offers a unique collection of 522 natural flavonoid compounds which is a useful tool for drug discovery as an important source of lead compounds.

  • HY-L179
    43 compounds

    Radiotherapy is a common treatment for various cancers, and more than 50% of cancer patients require radiotherapy during the disease treatment. With advances in radiation technology and a better understanding of tumor biology, the efficacy of radiation therapy has gradually improved, and more and more patients have benefited from it. However, even with the use of advanced radiotherapy techniques, there are still many malignant tumor cells with low sensitivity to radiation, leading to the radiation effect is not ideal. To solve this problem, radiosensitizers have received more and more attention. Radiosensitizer is a kind of drug that can enhance the radiosensitivity of tumor cells and improve the effect of radiotherapy. Radiation sensitizers act in a variety of ways, such as killing hypoxic cells, enhancing DNA damage, inhibiting DNA damage repair, and blocking cell cycle progression, making tumor cells more susceptible to radiation damage and death than surrounding normal cells.

    MCE designs a unique collection of 43 compounds with definite reported radiosensitization. It can be used for drug combination research in anti-cancer treatment.

  • HY-L047
    888 compounds

    The endocrine system is a chemical messenger system comprising feedback loops of the hormones released by internal glands of an organism directly into the circulatory system, regulating distant target organs. Hormones are chemicals that serve to communicate between organs and tissues for physiological regulation and behavioral activities. Hormones affect distant cells by binding to specific receptor proteins in the target cell, resulting in a change in cell function.

    The endocrine system is concerned with the integration of developmental events proliferation, growth, and differentiation, and the psychological or behavioral activities of metabolism, growth and development, tissue function, sleep, digestion, respiration, excretion, mood, stress, lactation, movement, reproduction, and sensory perception caused by hormones. Irregulated hormone release, inappropriate response to signaling or lack of a gland can lead to endocrine disease.

    MCE offers a unique collection of 888 endocrinology related compounds targeting varieties of hormone receptors such as thyroid hormone receptor, TSH receptor, GNRH receptor, adrenergic receptor, etc. MCE Endocrinology Compound Library is a useful tool for the discovery of endocrinology drugs.

  • HY-L129
    39 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. Therefore, PROTACs execute their functions by degrading the target proteins rather than inhibiting them, which has a great superiority in overcoming resistance caused by target mutation or overexpression. To date, PROTAC technology has been applied to a variety of targets, including AR, ER, BTK, BET, and BCR-ABL to overcome resistance.

    MCE carefully prepared a unique collection of 39 ligands for target proteins, which have been reported to be used in PROTAC design. MCE Target Protein Ligand Library is a useful tool for PROTAC development.

  • HY-L020
    362 compounds

    The developmental proteins Hedgehog, Notch and Wnt are key regulators of cell fate, proliferation, migration and differentiation in several tissues. Their related signaling pathways are frequently activated in tumors, and particularly in the rare subpopulation of cancer stem cells. The Wnt signaling pathway is a conserved pathway in animals. Deregulated Wnt signaling has catastrophic consequences for the developing embryo and it is now well appreciated that defective Wnt signaling is a causative factor for a number of pleiotropic human pathologies, including cancer. Hedgehog signaling pathway is linked to tumorigenesis and is aberrantly activated in a variety of cancers. The Notch signaling pathway is a highly conserved cell signaling system present in most animals. It plays an important role in cell-cell communication, and further regulates embryonic development.

    MCE designs a unique collection of 362 Wnt/Hedgehog/Notch signaling pathway-related small molecules. Wnt/Hedgehog/Notch Compound Library serves as a useful tool for stem cell research and anti-cancer drug screening.

  • HY-L154
    3,182 compounds

    Covalent inhibitors are small molecules that can bind specifically to target proteins through covalent bonds and inhibit their biological functions. Although for a long time, covalent targeting has been playing a subordinate role in drug discovery, with an increasing number of reports on successful clinical applications of such drugs, the potential of these agents is now being acknowledged. Currently, cysteine is the most common covalent amino acid residue in a variety of covalent drugs, and various warheads have been developed that can react with cysteine, providing the key building blocks for covalent drugs to form covalent bonds.

    To meet the development needs of covalent inhibitors targeting cysteine, MCE has designed a unique collection of 3,182 fragments with different covalent warheads that target cysteine. The MCE Cysteine Targeted Covalent Fragment Library is designed using the following covalent warheads: Acrylamides, Propiolic acid ester, Dimethylamine functionalized acrylamides, Chloroacetamides, Acrylonitrile, 2-Cyanoacrylamide, Aziridine, Haloacetamide, etc. All fragments are pre-filtered with the Rule of Three restrictions which can be used for fragment-based covalent drug development.

  • HY-L181
    20,505 compounds

    Bioactive small molecules are important sources of lead compounds and effective tools for drug screening. Because the target of active small molecules is clear, it is conducive to the study of mechanism. In addition, due to the large structural differences between the individual active molecules, it is easier to obtain a greater variety of lead compounds.

    MCE integrates the Bioactive Compound Library (HY-L001) and Novel Bioactive Compound Library (HY-L111) to form the Bioactive Compound Library Max. Bioactive Compound Library Max contains novel active small molecules, molecules that have entered the clinical stage and the market, and small molecules that have been verified by cell experiments or biochemical experiments, which fundamentally expands the number of compound libraries in the library and improves the structural diversity, and is an effective tool to start drug screening and mechanism research.

    MCE can provide a library of 20,505 mitophagy compounds, which can be used for drug development and mechanism research in cancer, immunity, infection and other hot research fields.

  • HY-L062
    1,828 compounds

    Neurotransmitter (NT) receptors, also known as neuroreceptors, are a broadly diverse group of membrane proteins that bind neurotransmitters for neuronal signaling. There are two major types of neurotransmitter receptors: ionotropic and metabotropic. Ionotropic receptors are ligand-gated ion channels, meaning that the receptor protein includes both a neurotransmitter binding site and an ion channel. The binding of a neurotransmitter molecule (the ligand) to the binding site induces a conformational change in the receptor structure, which opens, or gates, the ion channel. The term “metabotropic receptors” is typically used to refer to transmembrane G-protein-coupled receptors. Metabotropic receptors trigger second messenger-mediated effects within cells after neurotransmitter binding.

    In some neurological diseases, the neurotransmitter receptor itself appears to be the target of the disease process. Many neuroactive drugs act by modifying neurotransmitter receptors. A better understanding of neurotransmitter receptor changes in disease may lead to improvements in therapy.

    MCE designs a unique collection of 1,828 compounds targeting a variety of neurotransmitter receptors. MCE Neurotransmitter Receptor Compound Library is a useful tool for neurological diseases drug discovery.

  • HY-L038
    1,463 compounds

    Stem cells, which are found in all multi-cellular organisms, can divide and differentiate into diverse special cell types and can self-renew to produce more stem cells. To be useful in therapy, stem cells must be converted into desired cell types as necessary which is called induced differentiation or directed differentiation. Understanding and using signaling pathways for differentiation is an important method in successful regenerative medicine. Small molecules or growth factors induce the conversion of stem cells into appropriate progenitor cells, which will later give rise to the desired cell type. There is a variety of signal molecules and molecular families that may affect the establishment of germ layers in vivo, such as fibroblast growth factors (FGFs); the wnt family or superfamily of transforming growth factors β (TGFβ) and bone morphogenetic proteins (BMP). Unfortunately, for now, a high cost of recombinant factors is likely to limit their use on a larger scale in medicine. The more promising technique focuses on the use of small molecules. These small molecules can be used for either activating or deactivating specific signaling pathways. They enhance reprogramming efficiency by creating cells that are compatible with the desired type of tissue. It is a cheaper and non-immunogenic method.

    MCE Differentiation Inducing Compound Library contains a unique collection of 1,463 compounds that act on signaling pathways for differentiation. These compounds are potential stimulators for induced differentiation. This library is a useful tool for researching directed differentiation and regenerative medicine.

  • HY-L045
    2,572 compounds

    Oxygen homeostasis regulation is the most fundamental cellular process for adjusting physiological oxygen variations, and its irregularity leads to various human diseases, including cancer. Hypoxia is closely associated with cancer development, and hypoxia/oxygen-sensing signaling plays critical roles in the modulation of cancer progression.

    Hypoxia-inducible factor 1 (HIF-1) is a transcription factor that functions as a master regulator of oxygen homeostasis. A variety of HF-1 target genes have been identified thus far which encode proteins that play key roles in critical developmental and physiological processes including angiogenesis/vascular remodeling, erythropoiesis, glucose transport, glycolysis, iron transport, and cell proliferation/survival.

    HIF-1 is a heterodimeric transcription factor consisting of a constitutively expressed β-subunit and an oxygen-regulated α-subunit. The unique feature of HIF-1 is the regulation of HIF-1α expression and activity based upon the cellular O2 concentration. Under normoxic conditions, hydroxylation of HIF-1α on these different proline residues is essential for HIF proteolytic degradation by promoting interaction with the von Hippel-Lindau tumor-suppressor protein (pVHL) through hydrogen bonding to the hydroxyproline-binding pocket in the pVHL β-domain. As oxygen levels decrease, hydroxylation of HIF decreases; HIF-1α then no longer binds pVHL, and becomes stabilized, allowing more of the protein to translocate to the cell’s nucleus, where it acts as a transcription factor, upregulating (often within minutes) the production of proteins that stimulate blood perfusion in tissues and thus tissue oxygenation.

    MCE offers a unique collection of 2,572 oxygen sensing related compounds targeting HIF/HIF Prolyl-Hydroxylase, MAPK/ERK, PI3K/AKT signaling pathways, etc. MCE Oxygen Sensing Compound Library is a useful tool to study hypoxia, oxidative stress and discover new anti-cancer drugs.

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