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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
77 Results for "
active-site interactions
" in MedChemExpress (MCE) Product Catalog:
Products (77)
77 Results for "active-site interactions" in MCE Product Catalog:
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Sebetralstat (KVD900) is an orally active and selective plasma kallikrein inhibitor, with an IC50 of 6.0 nM and a Ki of 3.0 nM against the human target. Sebetralstat binds to the active site of plasma kallikrein, inducing a conformational flip of Trp215 to form a U-shaped conformation; its P1 group interacts with the S1 pocket through hydrophobic interactions and displacement of high-energy water molecules, independent of the Asp189 ionic bond. Sebetralstat inhibits plasma kallikrein-kinin system activation in whole plasma, rapidly relieves laryngeal and abdominal attack symptoms of hereditary angioedema (HAE-C1INH), and reduces attack severity. Sebetralstat can be used in research related to hereditary angioedema (HAE) .
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1 Cited Publications
Cat. No.: HY-P99283
CAS No.: 1312299-39-0
Synonyms: NN 7415; mAb 2021; Anti-TFPI Recombinant Antibody
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1 Cited Publications
Cat. No.: HY-N6845
CAS No.: 19275-46-8
Cat. No.: HY-W012817
CAS No.: 95-71-6
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Cat. No.: HY-157521
CAS No.: 3055162-52-9
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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 .
Cat. No.: HY-N1341
CAS No.: 54835-70-0
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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 .
Synonyms: ZGN-1061
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Aclimostat (ZGN-1061) is a methionine aminopeptidase 2 (MetAP2) inhibitor. Aclimostat exhibits anti-obesity, anti-diabetic and ovarian cancer-related activities, and does not readily distribute to the central nervous system. Aclimostat acts on the active site of MetAP2 via irreversible covalent binding, and blocks enzyme activity through interactions with His231 and His339. Aclimostat regulates gene expression, reduces fat mass, plasma glucose, insulin levels, LDL-C, hs-CRP and leptin levels, while increasing adiponectin levels. Aclimostat can be used in research related to type 2 diabetes, overweight, obesity and ovarian cancer .
Cat. No.: HY-W284558
CAS No.: 1120-01-0
Cat. No.: HY-N10423
CAS No.: 18423-69-3
Synonyms: (-)-Cubebin
Cat. No.: HY-161137
CAS No.: 3044047-98-2
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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 .
Cat. No.: HY-110147B
Purity: ≥99.0%
SSM-3 tetraTFA hydrate is a potent furin inhibitor with an EC50 of 54 nM. SSM-3 tetraTFA hydrate uses its positively charged guanidyl group to form strong electrostatic interactions with the negatively charged residues in the catalytic center of furin, thereby competitively occupying and blocking the active site. SSM-3 tetraTFA hydrate can be used in the research of anthrax and avian influenza .
Cat. No.: HY-N3057
CAS No.: 18956-15-5
Category:
Leguminosae/Fabaceae Extract Plant Flavonoids Chalcones Cajanus cajan (L.) Millsp. Extract Phenols Polyphenols Disease Research Fields Cancer
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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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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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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 .
Synonyms: 6′-Methoxyluciferin
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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 .
Cat. No.: HY-139032
CAS No.: 2204230-40-8
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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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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
