48 Results for "

active-site interactions

" in MedChemExpress (MCE) Product Catalog:
Products (48)

48 Results for "active-site interactions" in MCE Product Catalog:

1
1 Cited Publications
Cat. No.: HY-P99283
CAS No.: 1312299-39-0
Synonyms: NN 7415; mAb 2021; Anti-TFPI Recombinant Antibody

Target:  

Factor Xa

Research Areas:  

Others

Concizumab is an anti-TFPI monoclonal antibody (IgG4 type) that binds to the Kunitz-type protease inhibitor (KPI) 2 structural domain of TFPI, thereby blocking the interaction of this structural domain with the FXa active site. Concizumab can be used in the study of haemophilia .
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Cat. No.: HY-W012817
CAS No.: 95-71-6
Methylhydroquinone is an orally active COX inhibitor with IC50s of 480.7 μM and 52.2 μM for ovine COX-1 and human recombinant COX-2, respectively. Methylhydroquinone has potential DNA damaging effects: 1) inhibiting COX-1 to reduce prostaglandin synthesis and exert anti-inflammatory activity; 2) inducing DNA single-strand breaks. Methylhydroquinone exerts its effects by competitively binding to the active sites of COX-1 (such as Tyr385, Met522) and non-covalent interactions .
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Cat. No.: HY-157521
CAS No.: 3055162-52-9
Target:  

Acyltransferase

AANAT-IN-1 is an arylalkylamine N-acetyltransferase (AANAT) inhibitor with a sheep AANAT IC50 of 9.9 μM. AANAT-IN-1 binds to the active site of sheep AANAT, interacting with amino acid residues via hydrogen bonds, hydrophobic interactions, ionic interactions, and water bridges, inhibiting the enzyme's catalytic activity. AANAT-IN-1 can be used for the researches of circadian rhythm-associated neuropsychiatric conditions, seasonal affective disorder, and other diseases associated with abnormally elevated melatonin levels .
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Cat. No.: HY-N1341
CAS No.: 54835-70-0
Research Areas:  

Infection

Roseoside is an inhibitor of DNA gyrase and HAV 3C protease, and also inhibits HCV NS5A/B replicase in human systems with an IC50 of 20 μM. Roseoside binds to the active site of enzymes and stabilizes the interaction by forming hydrogen bonds with key amino acid residues. Roseoside inhibits the growth of Gram-positive bacteria, Gram-negative bacteria, and Candida albicans, and interferes with HCV RNA replication in vitro by inhibiting HCV NS5A/B replicase (IC50=20 μM). Roseoside shows no cytotoxicity and serves as a research tool for studies related to bacterial infections, candidiasis, HAV and HCV .
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Cat. No.: HY-W284558
CAS No.: 1120-01-0
Sodium hexadecyl sulfate is a long-chain anionic surfactant. Sodium hexadecyl sulfate can act as an interface-regulating substance to form a soft layer on the surface of carbon nanotubes, guide proteins to adsorb in the correct orientation with active sites facing outward through electrostatic interactions, and significantly enhance the activity of immobilized enzymes. Sodium hexadecyl sulfate can replace or supplement SDS (HY-Y0316) in capillary gel electrophoresis (CGE) .
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Cat. No.: HY-N10423
CAS No.: 18423-69-3
Synonyms: (-)-Cubebin
Cubebin ((-)-Cubebin), a dibenzyl butyrolactone lignan, is an orally active AChE inhibitor. Cubebin binds to active sites of NF-κB, TNF-α, and TGF-β1 via hydrogen and hydrophobic interactions, obstructing critical residues to inhibit pro-inflammatory or renal fibrosis-related activity. Cubebin enhances p38 MAPK phosphorylation to increase tyrosinase gene expression, stimulating melanogenesis via elevated tyrosinase activity, expression, and mRNA levels. Cubebin reduces oxidative stress via enhanced endogenous antioxidant enzyme activity and inhibited lipid peroxidation, regulates lipid metabolism, improves glycemic control, and exerts renoprotective effects via reduced renal dysfunction markers and improved renal architecture. Cubebin shows antimicrobial activity. Cubebin exerts larvicidal activity against Angiostrongylus cantonensis larvae, with no cytotoxicity toward monkey or human cell lines or Caenorhabditis elegans. Cubebin can be used for the research of diabetic nephropathy, melanoma, colon adenocarcinoma, neuroangiostrongyliasis, Alzheimer’s disease (AD) and depression .
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Cat. No.: HY-161137
CAS No.: 3044047-98-2
Research Areas:  

Neurological Disease

LQFM215 is a proline transporter (PROT) inhibitor. LQFM215 inhibits proline transport by competitively binding to the active site of PROT. LQFM215 effectively reduces hyperlocomotion and enhances social interaction .
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Cat. No.: HY-176892
CAS No.: 574-77-6
Research Areas:  

Neurological Disease

Papaveroline is a Fyn tyrosine kinase inhibitor, Na +,K +-ATPase inhibitor with an IC50 of 0.20 mM, Mg 2+-ATPase inhibitor, K +-activated pNPPase inhibitor with an IC50 of 1.51 mM, and apoptosis inducer . Papaveroline binds to the active site of Fyn tyrosine kinase and forms stable interactions with pocket amino acid residues . Papaveroline induces cell apoptosis, produces pycnotic and fragmented cell nuclei, and does not reduce intracellular ATP levels . Papaveroline is a dopamine-derived neurotoxin candidate associated with the pathogenesis of Parkinson's disease . Papaveroline can be used in the research of Alzheimer's disease and Parkinson's disease .
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Cat. No.: HY-139031
CAS No.: 2204229-64-9
Purity:  98.80%
Research Areas:  

Endocrinology

ALDH1A2-IN-1 is an active site-directed reversible ALDH1A2 inhibitor (IC50=0.91 μM; Kd=0.26 μM) with several hydrophobic interactions .
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Cat. No.: HY-136300
CAS No.: 2009343-14-8
Purity:  99.21%
PHD-1-IN-1 is an orally active and potent HIF prolylhydroxylase domain-1 (PHD-1) inhibitor with an IC50 of 0.034 μM. PHD-1-IN-1 has a unique monodentate binding interaction with the active site Fe 2+ ion and induces the formation of an "Arg367-out" pocket .
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Cat. No.: HY-115749
CAS No.: 24404-90-8
Purity:  99.93%
Synonyms: 6′-Methoxyluciferin
Target:  

Fluorescent Dye

Research Areas:  

Others

D-Luciferin 6′-methyl ether (6′-Methoxyluciferin; compound 19a) is a potent luciferase from the North American firefly Photinus pyralis (PpyLuc) inhibitor with an IC50 of 0.1 µM. D-Luciferin 6′-methyl ether, a D-luciferin analog, shows non-specific interactions at ATP- and luciferin-binding sites of the PpyLuc active site .
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Cat. No.: HY-139032
CAS No.: 2204230-40-8
Research Areas:  

Others

CM121 is an active site-directed reversible ALDH1A2 inhibitor (IC50=0.54 μM;Kd=1.1 μM) with a variety of hydrophobic interactions .
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Cat. No.: HY-121020
CAS No.: 83162-82-7
Arcapillin is a flavonoid that can be isolated from Artemisia capillaris Thunb. Arcapillin induces dose-dependent relaxation of ileum and pulmonary artery smooth muscle, causes slight urinary bladder smooth muscle contraction at highest tested concentrations. Arcapillin binds to the active site of SARS-CoV-2 Mpro via interactions with Gln139, His163, and His164, exhibits antiviral activity against SARS-CoV-2 and MERS-CoV. Arcapillin can be used for the research of gastrointestinal disorders, COVID-19, and Middle East respiratory syndrome (MERS) .
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Cat. No.: HY-161514
CAS No.: 2982794-86-3
Target:  

Xanthine Oxidase

Research Areas:  

Metabolic Disease

Xanthine oxidase-IN-15 (Compound 6c) is a selective inhibitor of Xanthine oxidase (XO) (IC50=0.13 μM). Xanthine oxidase-IN-15 inhibits XO catalysis by forming a stable interaction with the active site of XO. Xanthine oxidase-IN-15 is mainly used in the study of hyperuricemia and gout .
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Cat. No.: HY-115749A
CAS No.: 646450-23-9
Synonyms: (Rac)-6′-Methoxyluciferin sodium
D-Luciferin 6′-methyl ether (6′-Methoxyluciferin; compound 19a) sodium is a potent luciferase from the North American firefly Photinus pyralis (PpyLuc) inhibitor with an IC50 of 0.1 μM. D-Luciferin 6′-methyl ether, a D-luciferin analog, shows non-specific interactions at ATP- and luciferin-binding sites of the PpyLuc active site .
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Cat. No.: HY-W012817R
CAS No.: 95-71-6
Methylhydroquinone (Standard) is the analytical standard of Methylhydroquinone. This product is intended for research and analytical applications. Methylhydroquinone is an orally active COX inhibitor with IC50s of 480.7 μM and 52.2 μM for ovine COX-1 and human recombinant COX-2, respectively. Methylhydroquinone has potential DNA damaging effects: 1) inhibiting COX-1 to reduce prostaglandin synthesis and exert anti-inflammatory activity; 2) inducing DNA single-strand breaks. Methylhydroquinone exerts its effects by competitively binding to the active sites of COX-1 (such as Tyr385, Met522) and non-covalent interactions[1][2].
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Cat. No.: HY-W284558S
CAS No.: 2708287-31-2
Sodium hexadecyl sulfate-d33 is the deuterium labeled Sodium hexadecyl sulfate. Sodium hexadecyl sulfate is a long-chain anionic surfactant. Sodium hexadecyl sulfate can act as an interface-regulating substance to form a soft layer on the surface of carbon nanotubes, guide proteins to adsorb in the correct orientation with active sites facing outward through electrostatic interactions, and significantly enhance the activity of immobilized enzymes. Sodium hexadecyl sulfate can replace or supplement SDS (HY-Y0316) in capillary gel electrophoresis (CGE) .
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Cat. No.: HY-159481
SDH-IN-17 (compound C32), a hydrazide-containing flavonol derivative, is a potent succinate dehydrogenase (SDH) inhibitor with an IC50 of 8.42 μM. SDH-IN-17 can occupy the active site and form strong interactions with the key residues of SDH. SDH-IN-17 exhibits antifungal activity against Rhizoctonia solani (EC50=0.170 μg/mL). SDH-IN-17 disrupts the normal growth of hyphae by affecting the structural integrity of the cell membrane and cellular respiration. SDH-IN-17 has the potential for plant disease control research .
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Cat. No.: HY-170557
Research Areas:  

Cancer

Topoisomerase IIα-IN-10 (Compound 13r) is an inhibitor of Topoisomerase IIα. It binds to the active site of DNA when complexed with Topoisomerase IIα, and this binding is stabilized through interactions with DNA base pairs and amino acid residues. Topoisomerase IIα-IN-10 can induce Apoptosis by intercalating DNA and inhibiting Topoisomerase IIα, thereby disrupting the mitochondrial membrane potential and inhibiting the growth of HCT116 cell lines, with an IC50 of 4.37 μM against HCT116 cells. Topoisomerase IIα-IN-10 can be used for research in the field of cancer treatment .
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Cat. No.: HY-181141
AChE/MAO-B-IN-8 is an acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B) inhibitor with IC50 values of 0.72 and 0.19 μM. AChE/MAO-B-IN-8 interactions with AChE and MAO-B active-site amino acid residues. AChE/MAO-B-IN-8 can be used for the research of Alzheimer’s disease .
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