10071 Results for "

activators

" in MedChemExpress (MCE) Product Catalog:
Products (10071)

10071 Results for "activators" in MCE Product Catalog:

Cat. No.: HY-N0565S1
Doxycycline-d3 hyclate (major) is the deuterium labeled Doxycycline hyclate (HY-N0565B). Doxycycline hyclate is an orally active highly lipophilic, tissue-permeable MMP inhibitor with broad-spectrum antibacterial activity. Doxycycline hyclate is also a semi-synthetic antibiotic with chelating properties, which blocks bacterial protein synthesis and inhibits extracellular matrix degradation through interactions with zinc and calcium atoms. Doxycycline hyclate also inhibits mitochondrial biogenesis, translation, and the expression of respiratory chain proteins. Doxycycline hyclate induces apoptosis, inhibits autophagy and EMT, downregulates stem cell markers, and activates the PI3K-AKT pathway, thereby effectively inhibiting the viability and proliferation of cancer cells such as breast cancer cells. Doxycycline hyclate also promotes the survival and self-renewal of embryonic stem cells and neural stem cells, and reduces the frequency of medium changes in culture. Doxycycline hyclate has been applied in studies related to breast cancer, prostate cancer, bladder cancer, and other cancers .
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Cat. No.: HY-N1401R
CAS No.: 112246-15-8
20(R)-Ginsenoside Rh2 (Standard) is the analytical standard of 20(R)-Ginsenoside Rh2. This product is intended for research and analytical applications. 20(R)-Ginsenoside Rh2 is an orally active protopanaxadiol-type saponin with multiple biological activities. 20(R)-Ginsenoside Rh2 exerts a significant inhibitory effect on non-small cell lung cancer and liver cancer by inducing cell cycle arrest and promoting apoptosis. 20(R)-Ginsenoside Rh2 exerts anti-γ-herpesvirus effects by inhibiting viral DNA replication. 20(R)-Ginsenoside Rh2 inhibits inflammatory mediators by reducing the levels of NO, PGE2, and ROS; it can delay skin photoaging by reducing ROS and inhibiting MMP-9/2 activity. 20(R)-Ginsenoside Rh2 accelerates the recovery after muscle injury by activating the Akt1/PKB signaling pathway. 20(R)-Ginsenoside Rh2 can inhibit osteoclast formation and exert an anti-osteoporosis effect.
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Cat. No.: HY-N4118A
CAS No.: 6014-81-9
Synonyms: (-)-Cephaeline dihydrobromide; NSC 32944 dihydrobromide
Cephaeline dihydrobromide ((-)-Cephaeline dihydrobromide; NSC 32944 dihydrobromide) is a ferroptosis inducer, with broad-spectrum anticancer and antiviral activities. Cephaeline dihydrobromide induces ferroptosis (Ferroptosis) by upregulating p53, inhibiting NRF2, activating ULK3, downregulating the expressions of SLC7A11 and GPX4 in a p53-dependent manner, reducing GSH and mitochondrial membrane potential, and increasing lipid peroxidation and iron accumulation. Cephaeline dihydrobromide inhibits cancer cell proliferation, migration and tumor growth. Cephaeline dihydrobromide inhibits Ebola virus (EBOV) VLP entry and infection, with IC50 values of 3.27 μM and 22.18 μM respectively; it also inhibits Zika virus (ZIKV) NS5 RdRp activity (IC50 = 976 nM), and binds to severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) RdRp and N protein, with Kd values of 8.9 μM and 53.8 μM respectively. Cephaeline dihydrobromide can be used in studies related to breast cancer, lung cancer, COVID-19, EBOV and ZIKV infections .
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Cat. No.: HY-N5073
CAS No.: 178468-00-3
Synonyms: 4''-O-Glucosylvitexin
Vitexin-4''-O-glucoside (4''-O-Glucosylvitexin) is an orally active natural flavonoid component with multiple pharmacological effects including antioxidation, anti-inflammation, cytoprotection and anti-apoptosis. Vitexin-4''-O-glucoside regulates the MAPK signaling pathway by downregulating the phosphorylation levels of JNK and p38, thereby blocking endoplasmic reticulum stress responses. Vitexin-4''-O-glucoside alleviates oxidative stress by reducing MDA content and upregulating the activities of SOD and CAT, attenuates inflammation by downregulating the expressions of inflammatory factors TNF-α, IL-1β and IL-6, and also reduces LDH release and inhibits caspase-3 activation. Vitexin-4''-O-glucoside effectively improves drug-induced acute liver injury and exerts significant protective effects against myocardial hypoxia/reoxygenation injury. Vitexin-4''-O-glucoside can be used in studies on acute liver injury, cardiovascular diseases and myocardial hypoxia-reoxygenation injury .
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Cat. No.: HY-P1341
CAS No.: 343268-91-7
Synonyms: Orexin A (17-33) (human, mouse, rat, bovine)
OXA (17-33) (Orexin A (17-33) (human, mouse, rat, bovine)) is the shortest active orexin peptide that selectively targets OX1 (EC50=8.29 nM), with 23-fold selectivity for the OX1 receptor over the OX2 receptor. The activity of OXA (17-33) depends on the Tyr17, Leu20, Asn25, His26 residues and the spatial conformation of the α-helix. OXA (17-33) activates signaling pathways involving inositol-1,4,5-trisphosphate receptor (IP3R), phospholipase D (PL-D) and choline-Sigma-1R, thereby increasing the cytoplasmic Ca 2+ level in nucleus accumbens neurons, an effect that is blocked by Sigma-1R antagonists. OXA (17-33) serves as an important biological probe for investigating the function of the OX1 receptor. OXA (17-33) can be modified via incorporation of mixed disulfide bonds of homocysteine and cysteamine, and is widely used in studies related to insomnia and narcolepsy .
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Cat. No.: HY-P5763A
Synonyms: PNX-20 TFA
Phoenixin-20 TFA (PNX-20 TFA) is a neuropeptide that activates GPR173. Phoenixin-20 TFA inhibits LPS-induced TLR-4/MyD88/NF-κB signaling, pro-inflammatory cytokines, adhesion molecules, MMPs, and cytotoxicity. Phoenixin-20 TFA increases SIRT1 and inhibits NLRP3/ASC/caspase-1, oxidative stress, and IL-1β/IL-18. Phoenixin-20 TFA alleviates ox-LDL-induced endothelial dysfunction, monocyte adhesion, adhesion molecules, cytokines, NADPH oxidase/NOX-4, and ROS. Phoenixin-20 TFA promotes GPR173/STAT6-mediated anti-inflammatory polarization of microglia and neuroprotection. Phoenixin-20 TFA can be used in research on dental pulp infection, pulmonary arterial hypertension, atherosclerosis, neuroinflammation, anxiety, and neurodegenerative diseases .
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Cat. No.: HY-W008806S
Synonyms: OHHL-d3; N-(3-Oxohexanoyl)homoserine lactone-d3
Domaines de recherche:  

Infection Inflammation/Immunology

N-(3-Oxohexanoyl)-L-homoserine lactone-d3 (OHHL-d3) is the deuterated-labeled N-(3-Oxohexanoyl)-L-homoserine lactone (HY-W008806). N-(3-Oxohexanoyl)-L-homoserine lactone (OHHL; N-(3-Oxohexanoyl)homoserine lactone) is a specific agonist of LuxR-type transcription factor CarR with a Kd of 1.8 μM. N-(3-Oxohexanoyl)-L-homoserine lactone activates CarR by inducing protein multimerization, promoting its binding to target DNA sequences in the carR-carA intergenic region, thereby upregulating the transcription of carbapenem biosynthesis genes. N-(3-Oxohexanoyl)-L-homoserine lactone acts as a quorum sensing signal molecule, enabling bacteria to coordinate the production of carbapenem antibiotics in a cell density-dependent manner. N-(3-Oxohexanoyl)-L-homoserine lactone is used to study bacterial quorum sensing mechanisms, especially the secondary metabolism and virulence factor regulatory pathways of Erwinia carotovora and Yersinia enterocolitica .
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Cat. No.: HY-W008806S1
Synonyms: OHHL-d2; N-(3-Oxohexanoyl)homoserine lactone-d2
Domaines de recherche:  

Infection Inflammation/Immunology

N-(3-Oxohexanoyl)-L-homoserine lactone-d2 (OHHL-d2) is the deuterated-labeled N-(3-Oxohexanoyl)-L-homoserine lactone (HY-W008806). N-(3-Oxohexanoyl)-L-homoserine lactone (OHHL; N-(3-Oxohexanoyl)homoserine lactone) is a specific agonist of LuxR-type transcription factor CarR with a Kd of 1.8 μM. N-(3-Oxohexanoyl)-L-homoserine lactone activates CarR by inducing protein multimerization, promoting its binding to target DNA sequences in the carR-carA intergenic region, thereby upregulating the transcription of carbapenem biosynthesis genes. N-(3-Oxohexanoyl)-L-homoserine lactone acts as a quorum sensing signal molecule, enabling bacteria to coordinate the production of carbapenem antibiotics in a cell density-dependent manner. N-(3-Oxohexanoyl)-L-homoserine lactone is used to study bacterial quorum sensing mechanisms, especially the secondary metabolism and virulence factor regulatory pathways of Erwinia carotovora and Yersinia enterocolitica .
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Cat. No.: HY-W013403S
CAS No.: 362049-50-1
2'-Deoxy-2'-fluorouridine-d2 is the deuterium labeled 2'-Deoxy-2'-fluorouridine . 2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
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Cat. No.: HY-W016409R
CAS No.: 3943-89-3
Synonyms: Protocatechuic acid ethyl ester (Standard)
Ethyl 3,4-dihydroxybenzoate (Standard) (Protocatechuic acid ethyl ester (Standard)) is the analytical standard of Ethyl 3,4-dihydroxybenzoate (HY-W016409). This product is intended for research and analytical applications. Ethyl 3,4-dihydroxybenzoate (Protocatechuic acid ethyl ester) is an orally effective, blood-brain barrier-permeable, competitive prolyl hydroxylase (PHD) inhibitor that inhibits the hydroxylation modification of hypoxia-inducible factor (HIF) by PHD. Ethyl 3,4-dihydroxybenzoate stabilizes HIF-1α by inhibiting PHD, activates downstream pathways to induce autophagy and apoptosis of tumor cells, and regulates inflammatory responses, inhibits the NF-κB pathway, improves vascular permeability, and promotes osteoblast differentiation. Ethyl 3,4-dihydroxybenzoate has anti-tumor, anti-hypoxic injury, and bone metabolism regulation effects. It can also be used in the research of cardiovascular protection (such as reducing myocardial ischemic damage), bone tissue engineering (promoting osteogenesis/inhibiting osteoclast differentiation), and prevention and treatment of high-altitude cerebral edema .
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Cat. No.: HY-W021016
CAS No.: 824395-67-7
Synonyms: (S,S)-Ph-BPE
Domaines de recherche:  

Others

(+)-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 .
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Cat. No.: HY-W154247
CAS No.: 103313-38-8
Target:  

Bacterial

Domaines de recherche:  

Infection

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.
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Cat. No.: HY-W778057
CAS No.: 1330195-40-8
Synonyms: Protocatechuic acid ethyl ester-13C3
Ethyl 3,4-Dihydroxybenzoate- 13C3 (Protocatechuic acid ethyl ester- 13C3) is the 13C-labeled Ethyl 3,4-dihydroxybenzoate (HY-W016409). Ethyl 3,4-dihydroxybenzoate (Protocatechuic acid ethyl ester) is an orally effective, blood-brain barrier-permeable, competitive prolyl hydroxylase (PHD) inhibitor that inhibits the hydroxylation modification of hypoxia-inducible factor (HIF) by PHD. Ethyl 3,4-dihydroxybenzoate stabilizes HIF-1α by inhibiting PHD, activates downstream pathways to induce autophagy and apoptosis of tumor cells, and regulates inflammatory responses, inhibits the NF-κB pathway, improves vascular permeability, and promotes osteoblast differentiation. Ethyl 3,4-dihydroxybenzoate has anti-tumor, anti-hypoxic injury, and bone metabolism regulation effects. It can also be used in the research of cardiovascular protection (such as reducing myocardial ischemic damage), bone tissue engineering (promoting osteogenesis/inhibiting osteoclast differentiation), and prevention and treatment of high-altitude cerebral edema .
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Cat. No.: HY-Y0148R
CAS No.: 1679-53-4
Synonyms: NSC 15139 (Standard); 10-HDAA (Standard)
10-Hydroxydecanoic acid (Standard) is the analytical standard of 10-Hydroxydecanoic acid. This product is intended for research and analytical applications. 10-Hydroxydecanoic acid (10-HDAA) is a saturated fatty acid derived from 10-hydroxy-trans-2-decenoic acid, which can be isolated from royal jelly. 10-Hydroxydecanoic acid exhibits various biological activities, including anti-inflammatory, insecticidal, anti-malarial, and anti-Leishmania properties, as well as enhancing antigen-specific immune responses. The anti-inflammatory effects of 10-Hydroxydecanoic acid are primarily mediated by inhibiting the activation of NF-κB and the translation of interferon regulatory factor 1 (IRF-1), which reduces the production of interleukin 6 (IL-6) and nitric oxide (NO) in inflammatory cells. Additionally, 10-Hydroxydecanoic acid alleviates neuroinflammatory responses through the p53-autophagy pathway and the p53-NLRP3 pathway. Finally, 10-Hydroxydecanoic acid enhances antigen-specific immune responses by promoting the effective uptake of antigens by microfold cells[1][2][3][4][5].
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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.