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.

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.

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

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

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

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

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.

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.

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

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

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).

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

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.

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

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

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.

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.

Diminazene is a trypanocidal agent.

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

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

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.

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

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.

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

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.

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

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

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.

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].

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.

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.

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.

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

(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.

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

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

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.

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.

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).

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

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

UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (2700-fold versus plasmin and 4000-fold versus tPA).

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

ZM223 hydrochloride is an orally active, potent non-covalent inhibitor of NEDD8 activating enzyme (NAE), and with excellent anticancer activity.