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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
10384 Results for "
Activator
" in MedChemExpress (MCE) Product Catalog:
Products (10384)
10384 Results for "Activator" in MCE Product Catalog:
Cat. No.: HY-W016409R
CAS No.: 3943-89-3
Synonyms: Protocatechuic acid ethyl ester (Standard)
Cat. No.: HY-W021016
CAS No.: 824395-67-7
Synonyms: (S,S)-Ph-BPE
Target:
Research Areas:
(+)-1,2-Bis ((2S,5S)-2,5-diphenylphospholano)ethane ((S,S)-Ph-BPE) is a chiral bisphosphine ligand and catalyst. (+)-1,2-Bis ((2S,5S)-2,5-diphenylphospholano)ethane acts as a chiral ligand in rhodium-catalyzed reductive hydroformylation of alkenyl boronic esters, enabling enantiodivergent synthesis of chiral γ-boryl alcohols. (+)-1,2-Bis ((2S,5S)-2,5-diphenylphospholano)ethane forms chiral nickel-phosphine complexes to mediate asymmetric hydrogenation of aliphatic γ- and δ-keto acids; protons promote substrate C=O bond activation and stereoselectivity control via hydrogen bonding. (+)-1,2-Bis ((2S,5S)-2,5-diphenylphospholano)ethane forms a monodentate nickel complex, which serves as the active species for asymmetric hydrogenation of aliphatic keto acids .
Cat. No.: HY-W154247
CAS No.: 103313-38-8
IP6C is a specific inhibitor and phage sensitizer targeting type II Thoeris systems. IP6C competitively binds to histidine in the catalytic pocket of ThsB, blocks the production of the His-ADPR alarm signal and inhibits ThsA activation, thereby relieving bacterial stasis of phage replication. IP6C selectively resensitizes drug-resistant bacteria carrying type II Thoeris systems (such as Pseudomonas aeruginosa) to phage lysis, without affecting other bacteria, and shows no toxicity to mice and human cell lines. IP6C significantly improves the survival rate of infected mice, and can be used to overcome bacterial phage defense mechanisms and study Pseudomonas aeruginosa infections .
Thoeris system: (named after the Egyptian goddess of fertility and protection), is a widespread anti-phage immune defense system in bacteria and archaea. Thoeris system belongs to the "Abortion Infection (Abi)" mechanism of bacteria: when an individual bacterium detects phage invasion, it initiates a suicide program and dies, thereby blocking phage replication and spread, and protecting the surrounding bacterial population from infection.
Thoeris system: (named after the Egyptian goddess of fertility and protection), is a widespread anti-phage immune defense system in bacteria and archaea. Thoeris system belongs to the "Abortion Infection (Abi)" mechanism of bacteria: when an individual bacterium detects phage invasion, it initiates a suicide program and dies, thereby blocking phage replication and spread, and protecting the surrounding bacterial population from infection.
Cat. No.: HY-W778057
CAS No.: 1330195-40-8
Synonyms: Protocatechuic acid ethyl ester-13C3
Category:
Cat. No.: HY-L213
265 compounds
The anti-cancer drug library meticulously collects all drugs approved by FDA and other major national drug regulatory authorities for cancer treatment. These drugs cover a variety of cancer types, including but not limited to lung cancer, breast cancer, colorectal cancer, leukemia, and other common cancers. The library includes a wide range of drugs, from classic chemotherapeutic agents to cutting-edge targeted therapies and immunotherapies. It contains various types of drug compounds with different mechanisms of action. There are cytotoxic drugs that directly kill cancer cells, as well as drugs that work by modulating the tumor microenvironment, inhibiting tumor angiogenesis, and activating the immune system. This diversity provides researchers with a broad range of perspectives and options for intervention strategies.
This library can be used for basic research on cancer treatment, exploring new targets and new mechanisms of drug action; Conducting drug reuse research to look for potential therapeutic effects of existing drugs on other cancer types or diseases; Or conducting research into combination drugs to optimize cancer treatment.
MCE has collected 265 small-molecule compounds with cancer indications, which are good tools for drug repurposing.
Cat. No.: HY-L174
276 compounds
Macrophages are effector cells of the innate immune system, engulfing bacteria and secreting pro-inflammatory and antibacterial mediators. They are an important component of the first line defense against pathogens and tumor cells. In addition, macrophages play an important role in eliminating damaged cells through programmed cell death. Like all immune cells, macrophages originate from pluripotent hematopoietic stem cells in the bone marrow. Macrophages play key functions in many physiological processes beyond homeostasis and innate immunity, including metabolic function, cell debris clearance, tissue repair, and remodeling. In order to fulfill their different functional roles, macrophages can polarize into a series of phenotypes, including classic (pro inflammatory, M1) and alternative (anti-inflammatory, healing promoting, M2) activation states, as well as a wide range of regulatory phenotypes and subtypes. Macrophages exist in all vertebrate tissues and have a dual function in host protection and tissue damage, maintaining a good balance.
MCE designs a unique collection of 276 macrophage related compounds. It is a good tool to be used for research on Inflammation, cancer and other diseases.
Cat. No.: HY-L014
1,801 compounds
Nuclear factor-κB (NF-κB)/Rel proteins include NF-κB2 p52/p100, NF-κB1 p50/p105, c-Rel, RelA/p65, and RelB. These proteins function as dimeric transcription factors that regulate the expression of genes and influence a broad range of biological processes including innate and adaptive immunity, inflammation, stress responses, B-cell development, and lymphoid organogenesis. NF-κB plays a key role in regulating the immune response to infection. In addition, activation of the NF-κB pathway is involved in the pathogenesis of chronic inflammatory diseases, such as asthma, rheumatoid arthritis, and inflammatory bowel disease. Incorrect regulation of NF-κB has been linked to cancer, inflammatory and autoimmune diseases, septic shock, viral infection, and improper immune development.
MCE owns a unique collection of 1,801 small molecule compounds that can be used in the research of NF-κB signaling pathway or high throughput screening (HTS) related drug discovery.
Cat. No.: HY-L136
1,525 compounds
Coagulation, also known as clotting, is the process in which blood changes from a liquid to a solid gel to form a blood clot. Thrombin, which is accurately and evenly generated in the injured part of blood vessels, is a key effector enzyme of the blood coagulation system and participates in many important biological processes, such as platelet activation, fibrinogen conversion to fibrin network, coagulation feedback amplification, etc. At the same time, to avoid the accidental formation of thrombus in the body, there is also an anticoagulant mechanism that inhibits blood coagulation.
Normal coagulation mechanism represents a balance between the pro-coagulant pathway in the injured site and anti-coagulant pathway beyond it. The blood coagulation system may be out of balance during the perioperative period or critical illness, which may lead to thrombosis or excessive bleeding. Therefore, the physiological study of coagulation balance is an important basis for clinical diagnosis and treatment of the abnormal coagulation process.
MCE supplies a unique collection of 1,525 compounds targeting key proteins in coagulation and anti-coagulation system. MCE Coagulation and Anti-coagulation Compound Library is a useful tool for study the mechanism of coagulation and anticoagulation.
Cat. No.: HY-L166
1,751 compounds
Ion channel is a membrane-binding enzyme whose catalytic site is an ion conduction pore, which is opened and closed in response to specific environmental stimuli (voltage, ligand concentration, membrane tension, temperature, etc.). Ion channel provide pores for the passive diffusion of ions on the biofilm. Due to their high selectivity for ion, ion channel are generally classified as sodium (Na+ ), potassium (K+ ), calcium (Ca2+ ), chloride (Cl- ), and non-specific cation channel. Ion channel is an important contributor to cell signal transduction and homeostasis. In addition to electrical signal transduction, ion channel also have many functions: regulating vascular smooth muscle contraction, maintaining normal cell volume, regulating glandular secretion, protein kinase activation, etc. Therefore, dysfunction of ion channel can lead to many diseases, and its mechanism research is particularly important.
MCE designs a unique collection of 1,751 small molecules related to ion channel, mainly targeting Na+ channel, K+ channel, Ca2+ channel, GABA receptor, iGluR, etc. It is an essential tool for research of cardiovascular diseases, Nervous system diseases and other diseases.
Cat. No.: HY-L036
1,618 compounds
Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.
MCE covalent inhibitor library contains 1,618 small molecules including identified covalent inhibitors and other bioactive molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, Sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.
Cat. No.: HY-116115
CAS No.: 1233715-33-7
Synonyms: 17-Oxo-DPA; 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-DPA
Research Areas:
17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid (17-Oxo-DPA; 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-DPA) is an electrophilic oxo-derivative (EFOX) of the docosahexaenoic acid (DHA) (HY-B2167). 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid is generated during inflammation by COX-2-catalyzed mechanism in activated macrophages. 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid acts as an agonist for PPARγ and a modulator for NF-κB signaling pathway, inhibits the production of pro-inflammatory cytokines and nitric oxide, and exhibits anti-inflammatory efficacy .
Cat. No.: HY-117573
CAS No.: 1438280-73-9
Research Areas:
1Z105 is an orally active TLR4/MD2 agonist, immunostimulant and vaccine adjuvant. 1Z105 activates NF-κB via the MyD88/TRIF pathway in a CD14-independent manner, with EC50 values of 0.63 µM and 0.77 µM for inducing IL-6 and IL-12 in mBMDCs, respectively. 1Z105 promotes dendritic cell maturation, antigen uptake and cross-presentation; when used alone, it induces Th2-IgG1, while combined with the TLR7 agonist 1V270, it synergistically induces balanced Th1/Th2 responses and provides low-reactogenic protection against homologous, heterologous and heterosubtypic influenza. 1Z105 prevents LPS (HY-D1056A1)- and galactosamine-induced liver injury as well as autoantibody-driven arthritis in mice. 1Z105 can be used in studies related to influenza virus infection, inflammation, and LPS/galactosamine-induced liver injury .
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
NYX-2925 is an orally active, blood-brain barrier-permeable NMDAR modulator, with EC50 values of 55 pM, 28 fM, 11 pM and 55 pM against NR2A, NR2B, NR2C and NR2D, respectively . NYX-2925 enhances synaptic plasticity, long-term potentiation, metaplasticity, structural plasticity, learning ability, memory capacity and circadian rhythm amplitude. NYX-2925 regulates the signaling pathways of Src kinase, EIF2, mTOR, CDK5 and protein kinase A (PKA). NYX-2925 increases the levels of PSD-95, GluA1, activated Src and synaptic GluN2B . NYX-2925 is used in the research of neuropathic pain, fibromyalgia, painful diabetic peripheral neuropathy, post-traumatic stress disorder, cognitive impairment, depression, age-related cognitive decline and NMDAR-mediated central nervous system diseases .
Cat. No.: HY-137055
CAS No.: 1171824-96-6
PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function.
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-L908
1,244 compounds
Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.
MCE Lead-like Covalent Screening Library offers a valuable resource of 1,049 lead-like compounds with commonly used covalent warheads. These warheads, such as acrylamide, activated terminal alkyne, acyloxymethyl ketone, and boronic acid, are capable of reacting with specific amino acid residues, including cysteine, lysine, serine, and histidine. The inclusion of these reactive warheads in the library allows researchers to explore the potential of covalent inhibition, a powerful approach in drug discovery.
Cat. No.: HY-L135
3,540 compounds
With the progress of modern cancer therapy, the life of cancer patients has been extended. However, after initial treatment and recovery, the development of secondary tumors often leads to cancer recurrence. Cancer stem cells are a small number of cells that tumor growth and reproduction depend on.
Cancer stem cells have strong self-renewal ability, which is the direct cause of tumor occurrence. In addition, cancer stem cells also have the ability to differentiate into different cell types, playing a crucial role in tumor metastasis and development. Chemotherapy and radiotherapy induced DNA damage and apoptosis are common cancer treatments. However, cancer stem cells can effectively protect cancer cells from apoptosis by activating DNA repair ability. Cancer stem cells are regarded as the key "seed" of tumor occurrence, development, metastasis and recurrence. Since its first discovery in leukemia in 1994, cancer stem cells have been considered a promising therapeutic target for cancer treatment.
MCE supplies a unique collection of 3,540 compounds targeting key proteins in cancer stem cells. MCE Cancer Stem Cells Compound Library is a useful tool for cancer stem cells related research and anti-cancer drug development.
Cat. No.: HY-P703465
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: TRMT112; AD-001; HSPC152; HSPC170; Multifunctional methyltransferase subunit TRM112-like protein; tRNA methyltransferase 112 homolog; TRM112; HTrm112; TRMT11-2; TRNA Methyltransferase Activator Subunit 11-2; TRM112-Like Protein; TRNA Methyltransferase 11-2 Homolog; TRNA Methyltransferase 11-2 Homolog (S. Cerevisiae); TRNA Methyltransferase Subunit 11-2; HEMK2; N-6 Adenine-Specific DNA Methyltransferase 1 (Putative); Prev. C21orf127; Methylarsonite Methyltransferase N6AMT1; Prev. N6AMT1; Lysine N-Methyltransferase 9; PRED28; Methyltransferase N6AMT1; KMT9; Methyltransferase HEMK2; HemK Methyltransferase Family Member 2; M.HsaHemK2P; N6AMT; N-6 Adenine-Specific DNA Methyltransferase 1; MTQ2; Chromosome 21 Open Reading Frame 127; PrmC; N6-DNA-Methyltransferase; HemK Methyltransferase 2, ETF1 Glutamine And Histone H4 Lysine; Protein N(5)-Glutamine Methyltransferase
Species:
Human
Source:
E. coli
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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
