4086 Results for "

acid-responsive structural modulator

" in MedChemExpress (MCE) Product Catalog:
Products (4086)

4086 Results for "acid-responsive structural modulator" in MCE Product Catalog:

16
16 Cited Publications
Art. -Nr.: HY-109037
CAS. Nr.: 1642288-47-8
Reinheit:  99.94%
Synonyms: MYK461; SAR439152
Target:  

Myosin

Forschungsgebiete:  

Cardiovascular Disease

Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.
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16
16 Cited Publications
Art. -Nr.: HY-19620
CAS. Nr.: 1562338-42-4
Synonyms: LMI070; NVS-SM1
Forschungsgebiete:  

Cancer

Branaplam (LMI070; NVS-SM1) is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model .
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16
16 Cited Publications
Art. -Nr.: HY-19620A
CAS. Nr.: 1562338-39-9
Synonyms: LMI070 hydrochloride; NVS-SM1 hydrochloride
Forschungsgebiete:  

Cancer

Branaplam (LMI070; NVS-SM1) hydrochloride is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam hydrochloride inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam hydrochloride elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model .
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14
14 Cited Publications
Art. -Nr.: HY-N0322E
CAS. Nr.: 57-88-5
Cholesterol (synthetic) is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol (synthetic) plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol (synthetic) is also an endogenous estrogen-related receptor α (ERRα) agonist .
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14
14 Cited Publications
Art. -Nr.: HY-N0322D
CAS. Nr.: 57-88-5
Cholesterol (from plant) is the major sterol in mammals. It is making up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol (from plant) plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins . Cholesterol (from plant) is also an endogenous estrogen-related receptor α (ERRα) agonist .
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14
14 Cited Publications
Art. -Nr.: HY-12688A
CAS. Nr.: 864167-45-3
Reinheit:  ≥98.0%
Succinyl phosphonate trisodium salt is a α-Ketoglutarate Dehydrogenase Complex (KGDHC) modulator with neuroprotective activity. Succinyl phosphonate trisodium salt protects this complex, reduces cellular succinyl-CoA concentration, downregulates protein succinylation levels, and inhibits the activity of the α-ketoglutarate dehydrogenase complex. Succinyl phosphonate trisodium salt corrects hypoxic or ethanol-induced behavioral impairments, modulates exploratory behavior and emotional stress responses, and improves hypoxia tolerance. Succinyl phosphonate trisodium salt reduces glutamate excitotoxicity, restores the activity of the α-ketoglutarate dehydrogenase complex, reverses the changes in glutamate dehydrogenase and glutamine synthetase activities induced by β-amyloid (Amyloid-β), modulates cognitive function, and prevents β-amyloid-induced neuronal damage. Succinyl phosphonate trisodium salt improves microglial senescence, alleviates neuroinflammation, reactive oxygen species (ROS) production, lipid peroxidation, and the expression of proinflammatory cytokines. Succinyl phosphonate trisodium salt can be used in the research of Alzheimer's disease, aging-related neuroinflammation, and Parkinson's disease .
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13
13 Cited Publications
Art. -Nr.: HY-12594
CAS. Nr.: 1216941-48-8
Reinheit:  99.87%
Synonyms: ABT-450; Veruprevir
Target:  

HCV Protease HCV SARS-CoV

Forschungsgebiete:  

Infection

Paritaprevir (ABT-450) is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Paritaprevir is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir can be enhanced by Ritonavir (a CYP450 inhibitor) .
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12
12 Cited Publications
Art. -Nr.: HY-101291
CAS. Nr.: 1323403-33-3
Reinheit:  99.54%
Synonyms: CC-220
Iberdomide (CC-220) is an orally active and potent cereblon (CRBN) E3 ligase modulator (CELMoD) with an IC50 of ~150 nM for cereblon-binding affinity. Iberdomide, a derivative of Thalidomide (HY-14658), has antitumor and immunostimulatory activities .
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11
11 Cited Publications
Art. -Nr.: HY-17537
CAS. Nr.: 1216665-49-4
Target:  

IRE1

Forschungsgebiete:  

Cancer

APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain .
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11
11 Cited Publications
Art. -Nr.: HY-B1588
CAS. Nr.: 5697-56-3
Carbenoxolone is a blood-brain barrier-permeable Pannexin1 inhibitor, gap junction (Gap junction) blocker, and β-amyloid 42 inhibitor. Carbenoxolone modulates voltage-gated currents of wild-type and mutant Panx1, and inhibits stimulus-activated Panx1 channel function. Carbenoxolone interacts with stable residues of β-amyloid 42 peptides, fibrils and oligomers, thereby inhibiting their aggregation. Carbenoxolone alleviates liver fibrosis. Carbenoxolone exerts neuroprotective and nootropic effects. Carbenoxolone can be used in studies related to Alzheimer's disease and liver fibrosis .
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10
10 Cited Publications
Art. -Nr.: HY-N2371
CAS. Nr.: 20380-11-4
Synonyms: 27-OHC
27-Hydroxycholesterol (27-OHC) is a selective estrogen receptor modulator and an agonist of the liver X receptor.
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10
10 Cited Publications
Art. -Nr.: HY-N0281
CAS. Nr.: 486-35-1
Synonyms: 7,8-Dihydroxycoumarin
Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1β, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
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10
10 Cited Publications
Art. -Nr.: HY-B0113
CAS. Nr.: 73590-58-6
Synonyms: H 16868
Omeprazole (H 16868) is an orally active H +,K +-ATPase inhibitor and a proton pump inhibitor. Omeprazole competitively inhibits CYP2C19, CYP3A4, and CYP2C9 activity. Omeprazole inhibits gastric acid secretion and can be used for acid-related gastrointestinal disorders. Omeprazole inhibits pancreatic cancer cell proliferation, induces apoptosis, autophagosome accumulation (elevated LC3-I and LC3-II levels), oxidative stress, and cytogenetic imbalance, modulates lysosomal transport, reduces inflammatory cytokines. Omeprazole alters small intestinal morphology and magnesium absorption, and induces gastric mucosa morphologic changes. Omeprazole also has neuroprotective and antibacterial effects .
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10
10 Cited Publications
Art. -Nr.: HY-B0113A
CAS. Nr.: 95510-70-6
Synonyms: H 16868 sodium
Omeprazole (H 16868) sodium is an orally active H +,K +-ATPase inhibitor and a proton pump inhibitor. Omeprazole sodium competitively inhibits CYP2C19, CYP3A4, and CYP2C9 activity. Omeprazole sodium inhibits gastric acid secretion and can be used for acid-related gastrointestinal disorders. Omeprazole sodium inhibits pancreatic cancer cell proliferation, induces apoptosis, autophagosome accumulation (elevated LC3-I and LC3-II levels), oxidative stress, and cytogenetic imbalance, modulates lysosomal transport, reduces inflammatory cytokines. Omeprazole sodium alters small intestinal morphology and magnesium absorption, and induces gastric mucosa morphologic changes. Omeprazole sodium also has neuroprotective and antibacterial effects .
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9
9 Cited Publications
Art. -Nr.: HY-B1221
CAS. Nr.: 530-78-9
Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
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9
9 Cited Publications
Art. -Nr.: HY-N0029
CAS. Nr.: 81525-13-5
Forsythoside B is a phenylethanoid glycoside isolated from Forsythia suspensa (Thunb.) Vahl, a Chinese folk medicinal plant for treating inflammatory diseases and promoting blood circulation. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
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9
9 Cited Publications
Art. -Nr.: HY-104037
CAS. Nr.: 2055536-64-4
Reinheit:  99.14%
Synonyms: LYC-55716
Target:  

ROR

Forschungsgebiete:  

Cancer

Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival .
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9
9 Cited Publications
Art. -Nr.: HY-115670
CAS. Nr.: 866924-39-2
Reinheit:  99.30%
Target:  

MMP

Forschungsgebiete:  

Inflammation/Immunology Cancer

GW280264X is the mixed ADAM10/TACE (ADAM17) metalloproteinases inhibitor. GW280264X potently blocks TACE (ADAM17) and ADAM10 with IC50s of 8.0 nM and 11.5 nM, respectively . ADAM10 and 17 modulate the immunogenicity of glioblastoma-initiating cells .
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9
9 Cited Publications
Art. -Nr.: HY-162288
CAS. Nr.: 3036029-72-5
Target:  

DNA/RNA Synthesis

Forschungsgebiete:  

Cancer

FAZ-3532 is a G3BP inhibitor (Kd = 0.54 μM) which binds to the NTF2L nsP3 binding pocket in G3BP1. FAZ-3532 disrupts the co-condensation of RNA, G3BP1, and caprin 1. FAZ-3532 inhibits G3BP-driven stress granule formation. FAZ-3532 can be studied as a powerful tool to probe the biology of stress granules and a promising interventions designed to modulate stress granule formation .
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9
9 Cited Publications
Art. -Nr.: HY-N1445
CAS. Nr.: 482-35-9
Synonyms: Isoquercetin; Quercetin 3-glucoside
Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway . Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies .
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