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Elastase inhibitors block serine proteases that degrade elastin and other extracellular matrix proteins. Neutrophil elastase, the main target here, is stored in azurophil granules of neutrophils together with proteinase 3 and cathepsin G. After release it cleaves elastin and collagens, and it processes cytokines and cell surface receptors at sites of inflammation. During the formation of neutrophil extracellular traps (NETs), the enzyme moves to the nucleus and helps to decondense chromatin. Inhibitors are used in models of acute lung injury, cystic fibrosis and chronic obstructive pulmonary disease (COPD). Sivelestat, BAY-678 and DMP 777 are inhibitors of human neutrophil elastase. Related enzymes of the same class are listed under Serine Protease.
Secologanoside is a triterpenoid compound that acts as an elastase inhibitor, exhibiting an IC50 of 164 μg/mL. It demonstrates moderate cytotoxicity towards fibroblast cells. This compound is relevant for research applications focused on enzymatic inhibition and potential therapeutic approaches in conditions involving elastase activity.
19α-Hydroxyasiatic acid is a natural triterpenoid that functions as an elastase inhibitor. This compound demonstrates significant anti-elastase activity, making it a valuable tool in research focused on elastase-related diseases and inflammation. Its ability to modulate elastase activity positions it as a potential candidate for studying therapeutic applications in skin aging and pulmonary disorders.
Neutrophil elastase inhibitor 3 is a benzoxazinone analog that selectively inhibits neutrophil elastase (NE) with an IC50 of 80.8 nM. Its inhibitory effects are linked to the reduction of superoxide anion generation, making it a valuable tool in studying neutrophil-mediated inflammatory responses. This compound is suitable for research applications focused on inflammatory diseases and the role of neutrophil elastase in various pathological conditions.
Synonyms: AZD9668 tosylate
Alvelestat tosylate is a potent and selective inhibitor of neutrophil elastase (NE), demonstrating an affinity characterized by a pIC50 value of 7.9 nM and a Ki value of 9.4 nM. This compound plays a critical role in modulating inflammatory responses and tissue remodeling processes. It is primarily utilized in research applications focused on respiratory diseases, wherein neutrophil elastase activity contributes to pathophysiology.
Elastatinal is a potent competitive inhibitor of elastase, exhibiting a Ki of 0.21 μM. It demonstrates a higher inhibitory efficacy towards pancreatic elastase compared to leukocyte elastase, making it a valuable tool for studying elastase-related pathways. Additionally, Elastatinal does not exhibit activity against human leukocyte chymotrypsin-like protease, underscoring its specificity. This compound is suitable for research applications focused on elastase inhibition in various biological contexts.
ICI-200880 is a selective and reversible inhibitor of human neutrophil elastase (HNE). This compound demonstrates significant potential in the study of inflammatory lung diseases, particularly chronic obstructive pulmonary disease (COPD) and cystic fibrosis (CF), by modulating the activity of neutrophil elastase. Researchers may find ICI-200880 valuable for exploring therapeutic avenues in managing HNE-related pathologies.
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Pyracrenic acid is an elastase inhibitor with an IC50 of 2.42 µM, derived from the bark of Pyracantha crenulata. This compound exhibits notable DPPH free radical scavenging activity and possesses anti-inflammatory properties. It is useful in research applications focusing on elastase-related pathways and exploring therapeutic strategies for inflammation-related conditions.
Tiprelestat is a potent inhibitor of human neutrophil elastase, a key enzyme involved in inflammatory responses. This compound exhibits significant antimicrobial and anti-inflammatory activities, making it a valuable tool in the study of inflammation and immune-related diseases. Researchers can utilize Tiprelestat to explore its effects on various pathological conditions characterized by excessive elastase activity.
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(S)-MDL-101146 is a competitive and reversible inhibitor of human neutrophil elastase (HNE), exhibiting a Ki value of 25 nM. This compound effectively inhibits HNE-induced hemorrhage in experimental models, demonstrating its potential in therapeutic research. (S)-MDL-101146 is particularly relevant for studying diseases characterized by excessive elastase activity, including emphysema, rheumatoid arthritis, chronic bronchitis, cystic fibrosis, adult respiratory distress syndrome, and glomerulonephritis.
Synonyms: MDL 201,404YA
CE-1037 is a selective inhibitor of human neutrophil elastase (HNE), exhibiting a Ki value of 0.45 nM. This compound effectively prevents pulmonary hemorrhage induced by the intratracheal instillation of HNE. CE-1037 is valuable for research into pulmonary diseases, particularly chronic obstructive pulmonary disease (COPD), allowing for in-depth studies of its pathophysiology and potential therapeutic interventions.
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Roseltide rT1 is a selective inhibitor of neutrophil elastase, exhibiting an IC50 value of 0.47 μM. This compound is part of the Roseltide family (rT1-rT8) and demonstrates the ability to enhance cAMP accumulation in vitro when stimulated by neutrophil elastase. Due to its specific action on elastase, Roseltide rT1 is a valuable tool for research into diseases associated with elastase activity.
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Neutrophil elastase-IN-7 is an effective inhibitor of human neutrophil elastase (HNE), exhibiting an IC50 value of 0.54 μM. This compound also demonstrates notable inhibitory activity against various coagulation proteins, including thrombin (IC50: 8.2 μM), FXa (IC50: 12.7 μM), FXIa (IC50: 1.2 μM), and FXIIIa (IC50: 5.7 μM). Neutrophil elastase-IN-7 is suitable for investigating inflammation, innate immune responses, and tissue remodeling in biological research.
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MDL 101146 is a potent orally active inhibitor of neutrophil elastase, with a Ki value of 25 nM. This compound effectively suppresses neutrophil elastase activity, making it suitable for investigating inflammatory conditions such as arthritis. Its ability to modulate proteolytic enzymes offers valuable insights into therapeutic strategies for diseases characterized by excessive elastase activity.
ICI 186756 is a selective inhibitor of human neutrophil elastase, demonstrating competitive inhibition at the enzyme's active site. This compound effectively reduces elastase activity, which may mitigate enzyme-induced pulmonary alterations and has shown potential in modulating lung lesions in hamsters. Its application is particularly relevant in research on inflammatory lung diseases and therapeutic strategies targeting elastase-related pathologies.
Elastase-IN-1 is a potent inhibitor of elastase, exhibiting an IC50 value of 0.897 µM. This compound demonstrates non-toxic properties, making it suitable for various biological studies. Its ability to selectively inhibit elastase activity is valuable in research applications targeting diseases associated with elastase overactivity, such as emphysema and certain inflammatory conditions.
(R)-MDL-101146 is a competitive and reversible inhibitor targeting human neutrophil elastase (HNE), with a Ki value of 25 nM. This compound demonstrates significant inhibition of HNE-induced hemorrhage in preclinical models, highlighting its potential in respiratory and inflammatory diseases. Research applications include emphysema, rheumatoid arthritis, chronic bronchitis, cystic fibrosis, adult respiratory distress syndrome, and glomerulonephritis.
Cyclotheonellazole A is a natural macrocyclic peptide that acts as a potent inhibitor of elastase and chymotrypsin. It exhibits an IC50 of 0.034 nM for elastase and 0.62 nM for chymotrypsin, indicating its high efficacy in modulating these enzymes. This compound is valuable for research into inflammatory processes and potential therapeutic applications related to protease activity.
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AZD-9819 is a potent inhibitor of neutrophil elastase, an enzyme implicated in the pathogenesis of various inflammatory diseases. Its effective inhibition of HNE makes it a valuable tool in the study of chronic obstructive pulmonary disease (COPD) and related pulmonary conditions. Researchers can utilize AZD-9819 to explore the therapeutic potential of targeting neutrophil elastase in mitigating inflammation and tissue damage within the lungs.
L 659286 is a potent inhibitor of human polymorphonuclear leukocyte elastase (PMN elastase), with a reported Ki of 0.4 μM. This compound is utilized in research to investigate the role of elastase in lung injury mechanisms, particularly through its effects observed in model systems such as hamsters after intratracheal administration. Its specificity and efficacy make it a valuable tool for studying elastase-related pathologies.
BAY-8040 is a pyrimidopyridazine derivative that serves as a potent inhibitor of human neutrophil elastase (HNE). This compound has been shown to reduce cardiac remodeling and improve cardiac function in a rat model of pulmonary arterial hypertension induced by Monocrotaline (HY-N0750). BAY-8040 holds promise for research into inflammatory and cardiopulmonary pathologies.
HLE-IN-1 is a potent inhibitor of human leukocyte elastase (HLE) with an inhibitory constant (Ki) of 1.8 nM. This compound effectively modulates elastase activity, making it a valuable tool in the study of emphysema and inflammatory pulmonary conditions. Its specificity for HLE supports its application in research focused on lung diseases and therapeutic interventions targeting elastolytic enzymes.
Nostopeptin B is a cyclic dipeptide that functions as an inhibitor of elastase and chymotrypsin. Isolated from the marine organism N. minutum (NIES-26), Nostopeptin B features the unique amino acid 3-amino-6-hydroxy-2-piperidone (Ahp), which demonstrates significant inhibitory activity against these serine proteases. This compound is valuable for research applications involving protein degradation and inflammatory processes.
L-684248 is an inhibitor of human leukocyte elastase (HLE), acting through the formation of a covalent bond with the enzyme's active site. This interaction effectively mitigates HLE activity, demonstrating potential utility in anti-inflammatory and anti-tumor research applications. Its role in modulating elastase activity makes it a valuable tool for studies related to inflammatory pathways and cancer biology.
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