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MeOSuc-AAPV-CMK (ElastaseInhibitor III) is an elastaseinhibitor. MeOSuc-AAPV-CMK also inhibitscathepsin G and proteinase 3.MeOSuc-AAPV-CMK blocks the cleavage of adiponectin by leukocyte elastase .
Neutrophil elastaseinhibitor 5 (compound 29) is a dual inhibitor of HNE (human neutrophil elastase) and proteinase 3 (PR3) with IC50 values of 4.91 μM and 20.69 μM, respectively. Neutrophil elastaseinhibitor 5 can be used in the study of neutrophil inflammatory diseases .
Elasnin is a selective granulocyte elastaseinhibitor. Elasnin is almost ineffective for pancreatic elastase, trypsin, chymotrypsin, thermolysin and papain .
Elafin,also known as elafin-specific inhibitor (ESI) or skin anti-leucoprotease (SKALP), is a low molecular weight inhibitor of human neutrophil elastase (HNE) and proteinase 3 in lung. Elafin is antibiotic against Pseudomonas aeruginosa and Staphylococcus aureus .
ZD-0892 is a selective and potent inhibitor of a neutrophil elastase with Kis of 6.7 and 200 nM for human neutrophil elastase and porcine pancreatic elastase, respectively.
Elastatinal is a potent and competitive inhibitor of elastase, with a Ki of 0.21 μM. Elastatinal more potently inhibits pancreatic elastase versus leucocyte elastase. Elastatinal shows no activity on human leucocyte chymotrypsin-like protease .
Elastase LasB-IN-1 (Compound 4b) has antibacterial activity. Elastase LasB-IN-1 (Compound 4b) is a selective elastase LasB inhibitor with an IC50 value of 76 nM .
MDL 101146 is an orally active neutrophil elastaseinhibitor. MDL 101146 inhibits neutrophil elastase for human with a Ki value of 25 nM. MDL 101146 can be used for the research of arthritis .
JCP174 is an inhibitor of palmitoyl protein thioesterase-1 (TgPPT1), a depalmitoylase in the parasite T. gondii . JCP174 is also an inhibitor of porcine pancreatic elastase and human leukocyte elastase .
LasB-IN-1 (compound 5f) is a potent and orally active inhibitor of LasB (IC50 = 8.7 μM). LasB-IN-1 effectively attenuates elastase production and biofilm formation by P. aeruginosa while alleviating the inflammatory response through downregulating MAPK and NF-κB pathways. LasB-IN-1 is potential to be a novel anti-infective candidate against drug-resistant infections .
Freselestat (ONO-6818) is a potent and orally active neutrophil elastaseinhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity .
SSR69071 is a potent, orally active and selective inhibitor of neutrophil elastase. SSR69071 reduces myocardial infarct size following ischemia-reperfusion injury . SSR69071 displays a higher affinity for human elastase (Ki=0.0168 nM) than for rat (Ki=3 nM), mouse (Ki=1.8 nM), and rabbit (Ki= 58 nM) elastases .
Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastaseinhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity .
FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibitsmouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect .
Secologanoside is a triterpenoid isolated from Poraqueiba sericea, weakly inhibitselastase with an IC50 of 164 μg/mL. Secologanoside is moderate cytotoxic to fibroblasts .
Ala-Ala-Pro-Val-chloromethylketone is an irreversible human neutrophil elastase (NE) inhibitor for use in the study of chronic inflammatory airway diseases .
Cyclotheonellazole A is a natural macrocyclic peptide and a potent elastaseinhibitor (IC50=0.034 nM). Cyclotheonellazole A inhibitschymotrypsin with an IC50 value of 0.62 nM .
Tiprelestat is a potent human neutrophil elastaseinhibitor. Tiprelestat has antimicrobial and anti-inflammatory activities. Tiprelestat can be used in the research of inflammation/immune disease .
GW-311616 is a potent, orally bioavailable, long duration and selective human neutrophil elastase (HNE) inhibitor with IC50 value of 22 nM and Ki value of 0.31 nM .
GW-311616 is a potent, orally bioavailable, long duration and selective human neutrophil elastase (HNE) inhibitor with IC50 value of 22 nM and Ki value of 0.31 nM .
Alvelestat (tosylate) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM .
Rivulariapeptolides 1155 is a potent serine proteaseinhibitor with IC50s of 41.84, 4.94, 56.54 nM for chymotrypsin, elastase, prpteinase K, respectively .
3'-O-Methylmurraol is a coumarinthat can be found in Cnidium monnieri. 3'-O-Methylmurraol inhibits superoxide radical anion generation and elastase release .
Rivulariapeptolides 1185 is a high potent and selective serine proteaseinhibitor with IC50 values of 13.17 nM, 23.59 nM and 55.26 nM for chymotrypsin, elastase and proteinase K, respectively .
Rivulariapeptolides 1121 is a high potent and selective serine proteaseinhibitor with IC50 values of 35.52 nM, 13.24 nM and 48.05 nM for chymotrypsin, elastase and proteinase K, respectively .
Rivulariapeptolides 988 is a high potent and selective serine proteaseinhibitor with IC50 values of 95.46 nM, 15.29 nM and 85.50 nM for chymotrypsin, elastase and proteinase K, respectively .
Alvelestat (AZD9668) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM .
Lonodelestat (POL6014) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE). Lonodelestat (POL6014) has the potential for the research of cystic fibrosis (CF) .
Pyracrenic acid is an elastaseinhibitor (IC50 = 2.42 µM), can be obtained from the bark of Pyracantha crenulata. Pyracrenic acid has DPPH free radical scavenging activity and anti-inflammatory activity .
(R)-BAY-85-8501 is the less active Enantiomer of BAY-85-8501. BAY-85-8501 is a selective and potent inhibitor of Human Neutrophil Elastase (HNE), with an IC50 of 65 pM .
Lonodelestat TFA (POL6014 TFA) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE). Lonodelestat TFA has the potential for the research of cystic fibrosis (CF) .
JO146 is a Chlamydia trachomatis high temperature requirement A (CtHtrA) protease inhibitor with IC50s of 21.86 and 1.15 μM for CtHtrA and human neutrophil elastase (HNE), respectively. JO146 can be used to inhibits bacterial infections .
BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase(HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).
SP-Chymostatin B (α-MAPI) is a strong inhibitor of many proteases, including chymotrypsin, papain, chymotrypsin-like serine proteinases, chymases, and lysosomal cysteine proteinases such as cathepsins A,B,C, H, and L. SP-Chymostatin B weakly inhibits human leucocyte elastase .
ONO-EI-601 is the major metabolite of human neutrophil elastaseinhibitor ONO-5046. ONO-5046 has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19 .
Skullcapflavone I can be isolated from A. nallamalayana. Skullcapflavone I inhibitscollagenase and elastase enzyme with IC50s of 106.74 μM and 186.70 μM. Skullcapflavone I has anticancer activities by down-regulating miR-23a .
Sivelestat (EI546) is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19 .
Sivelestat (EI546) sodium is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19 .
KLK7/ELA2-IN-1 is a potent kallikrein-related peptidase 7 (KLK7) and epidermal elastase 2 (ELA2)inhibitor with IC50s of 6 nM and 55 nM, respectively (WO2009024527A1, Example 4) .
Sivelestat (EI546) sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium tetrahydrate has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19 .
BAY-678 racemate is a racemate of BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase(HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).
F-17 is a potential inhibitor of virulence factor. F-17 shows very significant inhibitory effect on biofilm, elastase, pyocyanin, and swarming motility. F-17 also shows a good binding effect on LasR and PqsR. F-17 has no obvious cytotoxicity .
BOS-318 is a potent, slowly dissociating, highly selective, and cell-permeable furininhibitor with IC50 value of 1.9 nM. BOS-318 protects ENaC from subsequent activation by neutrophil elastase. BOS-318 can be used for the rsearch for CF lung disease .
BAY-677 is an inactive control for BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase(HNE), with an IC50 of 20 nM . BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC) .
Cathepsin C-IN-6 (compound 2) is a E-64c-hydrazideas based inhibitor of cathepsin C with anti-inflammatory activity. Cathepsin C-IN-6 inhibts activation of neutrophil elastase,exhibits potential efficacy in inflammatory diseases with high neutrophil load (e.g.,chronic obstructive pulmonary disease) .
Tamarixetin 3-O-β-d-apiofuranosyl-(1 → 2)-β-d-galactopyranoside (compound 4) is an inhibitor of collagenase and elastase with potential anti-inflammatory activity. Tamarixetin 3-O-β-d-apiofuranosyl-(1 → 2)-β-d-galactopyranoside can be isolated from the methanol extract of the Balkan endemic species Astragalus thracicus Griseb. .
HCH6-1 is a potent and competitive dipeptide antagonist of Formyl peptide receptor 1 (FPR1). HCH6-1 inhibits chemotaxis, superoxide anion generation, and elastase release in human neutrophils specifically activated by fMLF (an FPR1 agonist). HCH6-1 has protective effects against acute lung injury (ALI) in vivo and can be used for the research of FPR1-involved inflammatory lung diseases .
5-O-Demethylnobiletin (5-Demethylnobiletin), a polymethoxyflavone isolated from Citrus jambhiri Lush., is a direct inhibition of 5-LOX (IC50=0.1 μM), without affecting the expression of COX-2. 5-O-Demethylnobiletin (5-Demethylnobiletin) has anti-inflammatory activity, inhibits leukotriene B (4)(LTB4) formation in rat neutrophils and elastase release in human neutrophils with an IC50 of 0.35 μM .
MeOSuc-AAPV-CMK (ElastaseInhibitor III) is an elastaseinhibitor. MeOSuc-AAPV-CMK also inhibitscathepsin G and proteinase 3.MeOSuc-AAPV-CMK blocks the cleavage of adiponectin by leukocyte elastase .
Elafin,also known as elafin-specific inhibitor (ESI) or skin anti-leucoprotease (SKALP), is a low molecular weight inhibitor of human neutrophil elastase (HNE) and proteinase 3 in lung. Elafin is antibiotic against Pseudomonas aeruginosa and Staphylococcus aureus .
Ala-Ala-Pro-Val-chloromethylketone is an irreversible human neutrophil elastase (NE) inhibitor for use in the study of chronic inflammatory airway diseases .
Tiprelestat is a potent human neutrophil elastaseinhibitor. Tiprelestat has antimicrobial and anti-inflammatory activities. Tiprelestat can be used in the research of inflammation/immune disease .
Lonodelestat (POL6014) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE). Lonodelestat (POL6014) has the potential for the research of cystic fibrosis (CF) .
Lonodelestat TFA (POL6014 TFA) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE). Lonodelestat TFA has the potential for the research of cystic fibrosis (CF) .
KLK7/ELA2-IN-1 is a potent kallikrein-related peptidase 7 (KLK7) and epidermal elastase 2 (ELA2)inhibitor with IC50s of 6 nM and 55 nM, respectively (WO2009024527A1, Example 4) .
CH 5450 (Z-Ile-Glu-Pro-Phe-Ome) is a selective short peptide human cardiac chymaseinhibitor. CH-5450 inhibits the action of rat MAB elastase 2 on substrate Ang I with an IC50 value of 49 µM and N-succinyl-Ala-Ala-Pro-Phe-p-nitroanilide with an IC50 value of 4.8 µM .
Secologanoside is a triterpenoid isolated from Poraqueiba sericea, weakly inhibitselastase with an IC50 of 164 μg/mL. Secologanoside is moderate cytotoxic to fibroblasts .
Elastatinal is a potent and competitive inhibitor of elastase, with a Ki of 0.21 μM. Elastatinal more potently inhibits pancreatic elastase versus leucocyte elastase. Elastatinal shows no activity on human leucocyte chymotrypsin-like protease .
Rivulariapeptolides 1155 is a potent serine proteaseinhibitor with IC50s of 41.84, 4.94, 56.54 nM for chymotrypsin, elastase, prpteinase K, respectively .
3'-O-Methylmurraol is a coumarinthat can be found in Cnidium monnieri. 3'-O-Methylmurraol inhibits superoxide radical anion generation and elastase release .
Rivulariapeptolides 1185 is a high potent and selective serine proteaseinhibitor with IC50 values of 13.17 nM, 23.59 nM and 55.26 nM for chymotrypsin, elastase and proteinase K, respectively .
Rivulariapeptolides 1121 is a high potent and selective serine proteaseinhibitor with IC50 values of 35.52 nM, 13.24 nM and 48.05 nM for chymotrypsin, elastase and proteinase K, respectively .
Rivulariapeptolides 988 is a high potent and selective serine proteaseinhibitor with IC50 values of 95.46 nM, 15.29 nM and 85.50 nM for chymotrypsin, elastase and proteinase K, respectively .
Pyracrenic acid is an elastaseinhibitor (IC50 = 2.42 µM), can be obtained from the bark of Pyracantha crenulata. Pyracrenic acid has DPPH free radical scavenging activity and anti-inflammatory activity .
Tamarixetin 3-O-β-d-apiofuranosyl-(1 → 2)-β-d-galactopyranoside (compound 4) is an inhibitor of collagenase and elastase with potential anti-inflammatory activity. Tamarixetin 3-O-β-d-apiofuranosyl-(1 → 2)-β-d-galactopyranoside can be isolated from the methanol extract of the Balkan endemic species Astragalus thracicus Griseb. .
5-O-Demethylnobiletin (5-Demethylnobiletin), a polymethoxyflavone isolated from Citrus jambhiri Lush., is a direct inhibition of 5-LOX (IC50=0.1 μM), without affecting the expression of COX-2. 5-O-Demethylnobiletin (5-Demethylnobiletin) has anti-inflammatory activity, inhibits leukotriene B (4)(LTB4) formation in rat neutrophils and elastase release in human neutrophils with an IC50 of 0.35 μM .
The leukocyte elastase inhibitor/SERPINB1 protein is an important neutrophil serine protease inhibitor that regulates innate immune responses by protecting cells from cytoplasmic proteases during stress. It inhibits various neutrophil proteases, including elastase and chymotrypsin, and blocks GZMH activity intracellularly. Leukocyte elastase inhibitor/SERPINB1 Protein, Pig (His, myc) is the recombinant pig-derived Leukocyte elastase inhibitor/SERPINB1 protein, expressed by E. coli , with N-His, C-Myc labeled tag. The total length of Leukocyte elastase inhibitor/SERPINB1 Protein, Pig (His, myc) is 378 a.a., with molecular weight of ~50.0 kDa.
Serpin B1 protein is an important neutrophil serine protease inhibitor that regulates innate immune responses by protecting cells from cytoplasmic proteases during stress. It inhibits various neutrophil proteases, including elastase and chymotrypsin, and blocks GZMH activity intracellularly. Serpin B1 Protein, Human (HEK293, His) is the recombinant human-derived Serpin B1 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of Serpin B1 Protein, Human (HEK293, His) is 379 a.a., with molecular weight of ~44.0 kDa.
Elafin/Trappin-2, a skin-specific inhibitor of neutrophil and pancreatic elastase, safeguards tissues against elastase-mediated proteolysis. Its inhibitory range extends to the alpha-4-beta-2/CHRNA2-CHRNB2 nicotinic acetylcholine receptor. Elafin/Trappin-2 also weakly inhibits Kv11.1/KCNH2/ERG1 and transient receptor potential cation channel subfamily V member 1 (TRPV1), as reported in studies. Elafin/Trappin-2 Protein, Human (HEK293, His) is the recombinant human-derived Elafin/Trappin-2 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of Elafin/Trappin-2 Protein, Human (HEK293, His) is 95 a.a., with molecular weight of 13-15 kDa.
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