serine protease

Aprotinin (Traskolan) is a broad-spectrum serine protease (BPTI) inhibitor that inhibits the activity of a number of different esterases and proteases. Aprotinin is an antifibrinolytic agent used to minimize hemorrhage during complex surgical procedures.

Leupeptin hemisulfate is a protease inhibitor with cell membrane-permeable, reversible, competitive, and oral activities. Leupeptin hemisulfate inhibits the activity of Cathepsin B, Cathepsin H, and Cathepsin L, and blocks fusion of amphipathic lysosomes. Leupeptin hemisulfate also has anti-inflammatory activity.

Proteinase K (Protease K) is a non-specific serine protease that can tolerate changes in SDS, urea, pH (4-12), salt concentration, and temperature. Proteinase K hydrolyzes a wide range of peptide bonds and is used for protein digestion.

Evolocumab is an inhibitor of the humanized monoclonal antibody PCSK9. It binds to circulating PCSK9 protein, resulting in inhibition of PCSK9 binding to LDLR. It can be used in studies of hypercholesterolemia and atherosclerotic cardiovascular disease.

ZD-0892 is a selective and potent inhibitor of neutrophil elastase, targeting human neutrophil elastase and porcine pancreatic elastase with Kis of 6.7 nM and 200 nM, respectively.

BCX 1470 inhibits the esterolytic activity of factor D and C1s (IC50: 96 nM and 1.6 nM), demonstrating 3.4- and 200-fold greater efficacy compared to trypsin, respectively.

BCX 1470 hydrochloride is a potent serine protease inhibitor with anti-inflammatory activity that inhibits the ester hydrolysis and haemolytic activity of factor D and C1s, and can be used to study oedema.

Pirodomast is a thromboxane A (TXA2) synthase inhibitor. Pirodomast inhibits leukotriene (LT) D4, C4, E4 formation and thromboxane B2 (TXB2) activity, but is weakly or ineffectively antagonistic to guinea pig bronchospasm induced by histamine, methacholine, serotonin, LTC4, or platelet-activating factor. Pirodomast is a potential antiallergic compound. Pirodomast had only weak relaxant activity on guinea pig trachea in vitro. Pirodomast is a potential antiallergic compound that inhibits the protein hydrolyzing activity of trypsin in vitro, prevents antigen-induced immediate and late asthmatic responses in allergic sheep in vivo, and inhibits antigen-induced airway hyperresponsiveness to histamine and carbachol in allergic sheep.

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, displaying higher affinity for human elastase (Ki = 0.0168 nM) compared to rat (Ki = 3 nM), mouse (Ki = 1.8 nM), and rabbit (Ki = 58 nM) elastases [2]. It reduces myocardial infarct size following ischemia-reperfusion injury [1] and has potential for treating chronic obstructive pulmonary diseases, asthma, emphysema, cystic fibrosis, and various inflammatory diseases.

Ono-3307 mesylate is a protease inhibitor with inhibitory effects on a variety of proteases.Ono-3307 mesylate has significant protective effects against liver injury in rats and inhibits the deposition of radiofibrillar proteins in the kidneys and lungs.PF-184298 is a protease inhibitor with potential antioxidant effects in plasma and adipose tissue.PF-184298 can be used in the study of pancreatitis.

Patamostat mesylate (E-3123) is a potent protease inhibitor with IC50 values of 39 nM for trypsin, 950 nM for plasmin, and 1.9 μM for thrombin. This compound demonstrates promising potential in suppressing the pathogenesis and development of acute pancreatitis.

TNIK-IN-2 is an inhibitor Traf2- and Nck-interacting protein kinase (TNIK, IC50 = 1.33 μM)) which is a downstream signal protein of the Wnt/β-catenin pathway.

Patamostat (E-3123) is a potent protease inhibitor that effectively inhibits trypsin, plasmin, and thrombin with IC50 values of 39 nM, 950 nM, and 1.9 µM, respectively. Research suggests it might suppress the pathogenesis and development of acute pancreatitis [1] [2].

Amiloride hydrochloride (Amiloride HCl) is an effective sodium channel blocker of epithelial.

Gabexate mesylate (FOY) is a serine proteinase inhibitor used therapeutically in the treatment of pancreatitis, disseminated intravascular coagulation (DIC), and as a regional anticoagulant for hemodialysis. The drug inhibits the hydrolytic effects of thrombin, plasmin, and kallikrein, but not of chymotrypsin and aprotinin.

PMSF (Phenylmethylsulfonyl fluoride) is an irreversible inhibitor of serine/cysteine protease and is often used in the preparation of cell lysates.

Ceritinib (LDK378) is an ALK tyrosine kinase inhibitor (IC50=200 pM) with selective, ATP-competitive, and oral activity. Ceritinib also inhibits IGF-1R, InsR, and STK22D (IC50=8/7/23 nM). Ceritinib has antitumor activity.

Sivelestat sodium tetrahydrate (ONO5046 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.

Camostat mesylate (FOY-S980) is a trypsin-like protease inhibitor and inhibits airway epithelial sodium channel (ENaC) function.

Nafamostat mesylate (FUT-175), a synthetic serine protease inhibitor, has been used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis.

Elastase from porcine pancreas is a serine protease derived from the porcine pancreas, consisting of 240 amino acid residues. It has the ability to hydrolyze proteins and peptides, can induce emphysema in hamsters, and is commonly used to establish animal models of chronic obstructive pulmonary disease (COPD).

4-Aminobenzamidine dihydrochloride (p-Aminobenzamidine dihydrochloride) is a strong trypsin inhibitor and a relatively weak inhibitor of urokinase type plasminogen activator (uPA) (K i =82 μM). 4-Aminobenzamidine can inhibit growth of a human prostate tumor in SCID mice [1] [2].