Serine Protease

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.

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.

Phenylmethanesulfonyl fluoride (PMSF (Phenylmethylsulfonyl fluoride)) is an enzyme inhibitor that inactivates IRC-50 arvin, subtilisin, and the fatty acid synthetase complex.

Alpha-Amyrin (alpha-Amyrine) is an inhibitor of trypsin and chymotrypsin with antineoplastic effects. alpha-Amyrin can be used in studies about acting as a hepatomodulatory.

Lodelaben (Declaben, SC-39026) is a reversible, non-competitive inhibitor of human neutrophil elastase (HNE), characterized by specificity and potency (IC50=0.5 μM, Ki=1.5 μM).

AEBSF hydrochloride (Pefabloc SC) is an irreversible inhibitor of serine proteases, such as chymotrypsin, kallikrein, thrombin, plasmin, and trypsin.

Upamostat is an inhibitor of a serine protease and is a urokinase plasminogen activator (uPA) inhibitor.

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.

(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.

Zt-12-037-01 is a ATP competitive STK19 inhibitor(IC50 values of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N),respectively).

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].

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.

AA26-9 is an effective and broad-spectrum inhibitor of serine hydrolase.

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.

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

PF-3644022 is an effective, selective, and ATP-competitive MAPKAPK2 (MK2) inhibitor (IC50: 5.2 nM and a Ki of 3 nM). PF-3644022 potently inhibits TNFα production and has an anti-inflammatory effect. PF-3644022 also inhibits MK3 and p38 regulated activated

KKI-5 acetate is a serine protease inhibitor that inhibits kallikrein and plasmin. KKI 5 may exhibit anticancer chemotherapeutic benefit and may also be used as a treatment for angioedema.

SLK STK10-IN-1 is a selective and potent inhibitor of SLK and STK10 with potential antitumor activity.

GSK-690693 is a pan-Akt inhibitor targeting Akt1 2 3 with IC50 of 2 nM 13 nM 9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.

ML281, a potent and selective STK33 inhibitor, exhibits an IC50 of 14 nM.

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

2,4-Dioxaspiro(5.5)undec-8-ene, 3-(2-furanyl)- (Ulinastatin) ,as an urinary trypsin inhibitor (UTI), is a glycoprotein that is isolated from healthy human urine or synthetically produced.

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

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.

Benzamidine hydrochloride (Benzamidine HCl) is a reversible inhibitor of serine proteases, including trypsin, plasmin, and thrombin (Ki of 35, 350, and 220 μM, respectively).

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

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

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

Demethylwedelolactone is a natural product isolated from Eclipta alba, has trypsin inhibitory effect an IC50 of 3.0 μM. it exerts anti-invasive growth effect on breast cancer cells.

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.

Alvelestat (AZD9668) is an orally bioavailable, selective, and reversible inhibitor of human neutrophil elastase (NE), exhibiting potential anti-inflammatory activity.

Diminazene is a trypanocidal agent.

UK-371804 is an effective and specific uPA inhibitor. It was selected as a candidate for further preClinicalal evaluation for the treatment of chronic dermal ulcers.

MEGA-9 (Nonanoyl-N-Methylglucamide) solubilizes membrane protein and can be used as a nonionic detergent.

Sivelestat sodium (EI 546 sodium) is a highly efficient inhibitor of human neutrophil elastase, improving sepsis-induced myocardial dysfunction by activating the PI3K AKT mTOR signaling pathway. It can be used in acute lung injury acute respiratory distress syndrome research.

ZK824190 is an orally available and selective inhibitor of urokinase plasminogen activator (uPA), with IC50 values of 237 nM for uPA, 1600 nM for tPA, and 1850 nM for Plasmin.

SC-514 (GK 01140) is a selective, orally active, ATP-competitive IKK-2 inhibitor (IC50=11.2±4.7 μM), obstructs NF-κB-dependent gene expression.

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.

BMS-363131 (BMS363131) is a potent and selective trypsin inhibitor with an IC50 value of <1.7 nM.

Patamostat HCl is a highly potent and selective small molecule protease (protease) inhibitor that inhibits trypsin, fibrinolytic enzymes, and thrombin with IC50 values of 39 nM, 950 nM, and 1.9 μM, respectively.Patamostat HCl is used in the study of acute pancreatitis.

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.

JCP174 is a depalmitoylase inhibitor that enhances Toxoplasma host-cell invasion by targeting TgPPT1.

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

Chrysophanol 8-O-glucoside and chrysophanol have mild cytotoxicity and anti-diabetic properties and can play metabolic roles in the insulin-stimulated glucose transport pathway

Feniralstat (KVD-824) is a selective and highly efficient kallikrein inhibitor. It can be used for researching immune system diseases and cardiovascular diseases.

BC 11 hydrobromide is a selective TMPRSS2 and urokinase (uPA) inhibitor.BC-11 induces diminished mitochondrial activity, promotes reactive oxygen species production, and promotes apoptosis, and can be used in the study of breast cancer.

erythro-Guaiacylglycerol-beta-O-4'-dehydrodisinapyl ether is a compound extracted from Brazilian rubber seed hulls and is an inhibitory activity against human leukocyte elastase (IC50 : 171 umol L).

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.