elastase

Elastase LasB-IN-1 (Compound 4b), a potent and selective inhibitor of elastase LasB, exhibits antibacterial activity and has been determined to possess an IC50 value of 76 nM [1].

Elastase-IN-1 (Compound Q11) is a non-toxic elastase inhibitor with an IC 50 of 0.897 μM [1].

Tyrosinase/elastase-IN-1, a triterpenoid extracted from the leaves of Rubus fraxinifolius, exhibits inhibitory activities against both tyrosinase and elastase enzymes.

Neutrophil elastase inhibitor 4 (compound 4f) is a competitive inhibitor of human neutrophil elastase (HNE) with IC50 of 42.30 nM and Ki of 8.04 nM. It prompts apoptosis in T47D cells and inhibits the proliferation of T47D, RPMI 8226, A549, and HSF cells with respective IC50 values of 21.25, 34.17, 29.93, and 99.11 nM [1].

Porcine pancreatic elastase is a serine protease composed of a single polypeptide chain with 240 amino acid residues. It has the ability to hydrolyze polypeptides and proteins, and can induce emphysema in hamsters.

MeOSuc-AAPV-CMK (Elastase Inhibitor III) serves as an inhibitor of elastase, as well as cathepsin G and proteinase 3, and impedes leukocyte elastase-mediated cleavage of adiponectin [1].

BOS-318 is a Furin inhibitor with slowly dissociating, highly selective, and cell-pemeable characteristcs.

Acetyltrialanine is a dipeptide compound that binds at two sites on the Tb+3-pancreatic elastase complex and can be used as a nitrogen source.

2-(2-bromophenyl)-5-chloro-4H-3,1-benzoxazin-4-one is an human neutrophil elastase inhibitor.

2-CHLOROMETHYL-1,1-DIOXO-1,2-DIHYDRO-1LAMBDA*6*-BENZO[D]ISOTHIAZOL-3-ONE targets the Neutrophil elastase (human).

AZD8309 is a potent, orally available antagonist of the chemokine receptor CXCR2 that regulates neutrophil transport, significantly reduces MPO in the pancreas and lung, and decreases trypsin and elastase activity in the pancreas.AZD8309 can be used to study a range of inflammatory diseases.

BAY-678 is a human neutrophil elastase (HNE; IC50: 20 nM) inhibitor with oral bioactivity, potency and selectivity.BAY-678 is a chemical probe recommended by the Structural Genomics Consortium (SGC).

GW-311616 hydrochloride is a long duration, orally bioavailable, and selective human neutrophil elastase (HNE) inhibitor (IC50: 22 nM; Ki: 0.31 nM).

SSR69071 is a potent, orally active, and selective inhibitor of neutrophil elastase. 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 [2]. SSR69071 reduces myocardial infarct size following ischemia-reperfusion injury [1]. SSR69071 also has the potential for the treatment of chronic obstructive pulmonary diseases, asthma, emphysema, cystic fibrosis, and several inflammatory diseases.

3,4 Dichloroisocoumarin is a granzyme, cathepsin G, and neutrolphil elastase inhibitor

Coronarin, A, B, C, and D are cytotoxic prinicples from the rhizomes of Hedychium coronarium, Zingiberaceae. Coronarin A exhibits good growth inhibition activities on HUVEC proliferation, it effectively suppresses the growth factor induced tube formation

Docosyl caffeate shows moderate antioxidant activity in DPPH and ABTS scavenging assays, it also has significant anti-inflammation activity. Docosyl caffeate exhibits potent elastase inhibitory activity, with the IC50 value of 1.4 microg/mL.

(R)-3-hydroxy Myristic Acid is an antifungal compound from Lactobacillus plantarum MiLAB 14 with antioxidant, anti-elastase, and anti-urease activities and can be used in the study of fungal infections.

Decarine has high antibacterial activity against mycobacterial, gram-positive and gram-negative bacteria, and low cytotoxicity towards human macrophages.Decarine inhibits fMLP/CB-induced elastase release with IC(50) values < or = 5.53 microg/mL.

Hispanone possesses anti-inflammatory activity, it shows inhibition of superoxide anion generation and elastase release.

CH 5450 (Z-Ile-Glu-Pro-Phe-Ome) (Z-Ile-Glu-Pro-Phe-Ome) is a short peptide inhibitor of chymase in the human heart

MeOSuc-AAPA-CMK is a potent inhibitor of human neutrophil elastase (HNE) [1].

Cathepsin C-IN-6 (compound 2), an E-64c-hydrazideas-derived inhibitor of cathepsin C, possesses anti-inflammatory properties and impedes neutrophil elastase activation. This compound demonstrates potential efficacy in treating inflammatory diseases characterized by elevated neutrophil counts, such as chronic obstructive pulmonary disease (COPD) [1].

BAY-85-8501 is a selective, reversible and potent inhibitor of Human Neutrophil Elastase (HNE; IC50 of 65 pM)

Lodelaben is a human neutrophil elastase inhibitor with an IC50 and Ki of 0.5 and 1.5 μM, respectively.

Eglin c (60-63) is a sequence of a peptide that has been studied for its inhibitory activity towards human leukocyte elastase, cathepsin G, porcine pancreatic elastase and alpha-chymotrypsin.

FK706 is a slow-binding and competitive human neutrophil elastase inhibitor (IC50: 83 nM; Ki: 4.2 nM). FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase (IC50s: 22 nM and 100 nM, respectively). FK706 has an anti-inflammatory ef

LM-030, also known as BPR277, is a novel inhibitor of kallikrein-related peptidase 7 (KLK7) and epidermal elastase 2 (ELA2).

AZD-9819 is an inhibitor of human neutrophil elastase for potential treatment of chronic obstructive pulmonary disease (COPD).

Tiprelestat, a potent inhibitor of human neutrophil elastase, exhibits antimicrobial and anti-inflammatory properties. It is utilized in the study of inflammation and immune diseases [1].

Lonodelestat TFA (POL6014 TFA) is a potent, selective peptide inhibitor of human neutrophil elastase (hNE), demonstrating oral activity. It holds promise for cystic fibrosis (CF) research [1] [2] [3].

Suc-AAP-Abu-pNA is a specific substrate for pancreatic elastase (Km = 100 μM; Kcat/Km = 35,300 s-1 M-1 for rat pancreatic elastase; Km = 30 μM; Kcat/Km = 351,000 s- 1 M-1 for porcine pancreatic elastase).

5,7-Dihydroxy-4-methylcoumarin (Methyl-2H-Chromen-2-One) inhibits human neutrophil oxidative metabolism and elastase activity. 5,7-Dihydroxy-4-methylcoumarin has in vitro platelet antiaggregatory property. 5,7-Dihydroxy-4-methylcoumarin shows inhibition of the cyclooxygenase pathway.

SP-Chymostatin B is a potent inhibitor of many proteases, including chymotrypsin, papain, chymotrypsin-like serine proteinases, chymases, and lysosomal cysteine proteinases. It weakly inhibits human leucocyte elastase. It is effective at a final concentra

Nostopeptin B is an inhibitor of elastase.

Ono EI-601 is the main metabolite of ONO-5046, the human neutrophil elastase inhibitor .

ZD-0892 is a selective and potent inhibitor of neutrophil elastase, inhibits human neutrophil elastase and porcine pancreatic elastase, reverses advanced pulmonary vascular disease produced in rats, and can be used to study chronic obstructive pulmonary disease (COPD) and peripheral vascular disease (PVD).

Secologanoside shows anti-complementary, allelopathic, and anti-elastase activities.

Sivelestat (ONO5046) is a potent and selective inhibitor of neutrophil elastase with IC50 of 44 nM.

MMP inhibitor I is a peptide inhibitor of matrix metalloproteinase-1 (MMP-1), MMP-2, and MMP-3 (IC50s = 1.3, 30, and 150 μM, respectively). It is selective for MMP-1, MMP-2, and MMP-3 over the proteases thermolysin, urease, trypsin, α-chymotrypsin, plasmin, and elastase at concentrations up to 4 mM.

Eicosanyl caffeate has anti-ulcer and moderate antioxidant properties, it exhibits potent elastase inhibitory activity, with the IC(50) value of 0.99 microg/mL.

BAY8040 is a potent selective human neutrophilic elastase inhibitor with excellent potency and selectivity with promising pharmacokinetic characteristics.

Aristololactam IIIa demonstrates substantial inhibition of superoxide anion generation and elastase release, exhibiting IC50 values of 0.12 and 0.20 μg/mL, respectively [1].

Rivulariapeptolides 1155 is a potent serine protease inhibitor, exhibiting inhibitory concentrations (IC50s) of 41.84 nM, 4.94 nM, and 56.54 nM against chymotrypsin, elastase, and proteinase K, respectively [1].

Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent, orally active inhibitor of neutrophil elastase (Ki: 12.2 nM). quarterhydrate is more than 100-fold less active than other proteases such as trypsin, proteinase 3, pancreatic elastase, thrombin, fibrin, collagenase, histone G and murine macrophage elastase, and exhibits potent anti-inflammatory effects.

ICI 200355 is an inhibitor of human neutrophil elastase.

L 680833 is an orally active monocyclic beta-lactam human polymorphonuclear leukocyte elastase inhibitor.

JO146 is a protease inhibitor for Chlamydia trachomatis high temperature requirement A (CtHtrA) and human neutrophil elastase (HNE), with IC50 values of 21.86 μM for CtHtrA and 1.15 μM for HNE, respectively. It is effective in inhibiting bacterial infections.

Sydowinin B is a xanthone polyketide that has been found inA. sydowiiand has immunosuppressant activity.1It inhibits LPS- or concanavalin A-induced proliferation of isolated mouse splenic lymphocytes (IC50s = 19.2 and 20.8 μg/ml, respectively).2Sydowinin B inhibits superoxide generation in, and elastase release from, isolated human neutrophils induced by cytochalasin B and N-Formyl-Met-Leu-Phe with IC50values of 21.2 and 12.62 μM, respectively.3

Elafin, also referred to as elafin-specific inhibitor (ESI) or skin anti-leucoprotease (SKALP), is a protein that serves as a low molecular weight inhibitor of human neutrophil elastase (HNE) and proteinase 3, particularly in the lung. Additionally, Elafin exhibits antibacterial properties against Pseudomonas aeruginosa and Staphylococcus aureus [1] [2] [3].