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serine protease inhibitor
AEBSF HCl is a broad spectrum, irreversible serine protease inhibitor.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
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neutrophil elastase inhibitor
Avelestat, also known as AZD9668, is a novel, oral inhibitor of neutrophil elastase (NE).- Chen Yang, .et al. , mBio, 2024, Oct 16;15(10):e0213024 PMID: 39287443
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Neutrophil elastase inhibitor
Sivelestat sodium salt is a selective leukocyte elastase inhibitor (IC50 = 44 nM) that displays no activity at a range of other proteases. It inhibits NF-kB activation and LTB4-induced neutrophil transmigration in vitro.- Shasha He, .et al. , Nature Biomedical Engineering, 2023, 7: 281-297 PMID: 36941352
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Serine/cysteine protease inhibitor
PMSF is an irreversible serine/cysteine protease inhibitor.- Xi Yu, .et al. , Neuroreport, 2022, Nov 2;33(16):705-713 PMID: 36165031
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serine protease inhibitor
Aprotinin is a small protein serine protease inhibitor, used to reduce perioperative blood loss and transfusion.- Xi Yu, .et al. , Neuroreport, 2022, Nov 2;33(16):705-713 PMID: 36165031
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serine protease inhibitor
Nafamostat is an anticoagulant. Broad spectrum serine protease inhibitor. Reduces eosinophil infiltration, mast cell activation and airway responsiveness in a murine model of asthma.- Zeynep Demirsoy, .et al. , Chemical Engineering Journal, 2025, 516: 164066
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Serine protease inhibitor
BCX 1470 is serine protease inhibitor. BCX 1470 blocks the esterolytic and hemolytic activities of the complement enzymes Cls and factor D in vitro. -
Serine protease inhibitor
AAF-CMK is a serine protease inhibitor which irreversibly inhibits TPPII (tripeptidyl peptidase II), a giant protease which may substitute for some proteasome functions1, and reversibly inhibits Cln2 (TPPI). -
Cysteine Protease inhibitor
Leupeptin hemisulfate is a reversible inhibitor of trypsin-like and cysteine proteases such as calpain. -
Neutrophil elastase inhibitor
Sivelestat is a cell-permeable sulfanilide compound that acts as a potent, substrate-competitive, and highly specific inhibitor of neutrophil elastase (IC50 = 19-49 nM in rat, rabbit, hamster, human, and mouse leukocyte elastase). -
Neutrophil elastase inhibitor
Sivelestat sodium is a competitive inhibitor of human neutrophil elastase, also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse. -
serine proteases inhibitor
Benzamidine hydrochloride is an reversible competitive inhibitor of trypsin-like serine proteases, with Kis of 97 ?M, 21 ?M, 20 ?M and 110 ?M for uPA, trypsin, tryptase and factor Xa, respectively. -
serine protease inhibitor
Nafamostat is an anticoagulant. Broad spectrum serine protease inhibitor. Reduces eosinophil infiltration, mast cell activation and airway responsiveness in a murine model of asthma. -
serine protease inhibitor
Nafamostat hydrochloride is an anticoagulant. Broad spectrum serine protease inhibitor. Reduces eosinophil infiltration, mast cell activation and airway responsiveness in a murine model of asthma. -
PKK inhibitor
Avoralstat is an oral plasma kallikrein (PKK) inhibitor, used for the treatment of hereditary angioedema. -
PCSK9 inhibitor
SBC-110736 is a proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitor extracted from patent WO2014150395A1, Figure 1. -
serine/threonine phosphatase inhibitor
Fumonisin B1 is a fungal metabolite produced by Fusarium moniliforme, that has been shown to inhibit protein serine/threonine phosphatases (PP1, PP2A, PP2B, PP2C, and PP5/T/K/H), and is most effective with PP5. -
Kallikrein Inhibitor
Kallikrein-IN-1 is a selective inhibitor of kallikrein enzymes. By modulating kallikrein activity, this compound plays a vital role in regulating various physiological processes including blood pressure and inflammation. It is valuable for research into cardiovascular diseases and potential therapeutic approaches targeting the kallikrein-kinin system. Kallikrein-IN-1's specificity makes it an important tool for studying enzymatic pathways and their implications in disease states. -
Protease Inhibitor
Dansyl-Glu-Gly-Arg-Chloromethylketone is a potent protease inhibitor that specifically targets serine/threonine proteases. Its mechanism involves the irreversible modification of the enzyme active site, effectively blocking protease activity. This compound is valuable for research applications focusing on blood coagulation processes and the role of serine proteases in various biological systems. Its use facilitates the study of proteolytic regulation mechanisms and contributes to the understanding of protease-targeted therapies. -
Trypsin Inhibitor
Bz-D-Arg-pNA hydrochloride is a competitive inhibitor of trypsin, a serine protease involved in protein digestion and regulation. This compound effectively modulates trypsin activity, making it a valuable tool for investigating protease functions and interactions in various biological systems. Its applications extend to studying enzyme kinetics and exploring the role of trypsin in physiological and pathological processes. -
Tryptase Inhibitor
MOL-6131 is a highly selective, reversible inhibitor of tryptase, exhibiting a Ki value of 45 nM. This compound effectively reduces key features of allergic airway inflammation, including eosinophil infiltration in lung tissue, goblet cell hyperplasia, and mucus occlusion of airways. It serves as a valuable tool for research focused on respiratory diseases and allergic responses. -
FVII Inhibitor
Factor VII-IN-1 is a potent inhibitor of factor VII (FVII), exhibiting an IC50 of 1.1 μM. This compound demonstrates anticoagulant properties, making it a valuable tool for research applications focused on coagulation processes and thrombotic disorders. Factor VII-IN-1 can be utilized in studies aimed at understanding the mechanisms of blood coagulation and the development of anticoagulant therapies. -
Chymase Inhibitor
NK3201 is an orally active chymase inhibitor, demonstrating IC50 values of 2.5 nM, 1.2 nM, and 28 nM against human, dog, and hamster chymase, respectively. This compound effectively mitigates Bleomycin-induced pulmonary fibrosis and inhibits vascular proliferation in grafted veins. NK3201 serves as a valuable tool in research focused on fibroproliferative diseases and vascular complications. -
Protease Inhibitor
Leupeptin Ac-LL is a protease inhibitor derived from actinomycetes. It exhibits antiplasmin activity, making it useful in studies involving the regulation of proteolytic processes. This compound is commonly used in biochemical research to investigate protease functions and their roles in various biological pathways. -
DCLK1 inhibitor
DCLK1-IN-2 is a potent inhibitor of doublecortin-like kinase 1 (DCLK1) with an IC50 of 171.3 nM. This compound demonstrates significant antiproliferative activity against SW1990 cell lines, exhibiting an IC50 of 0.6 μM, and shows notable in vivo antitumor efficacy. DCLK1-IN-2 is suitable for research applications targeting DCLK1 in cancer biology and therapeutic development. -
Trypsin-like Serine Protease Inhibitor
UAMC-00050 is a potent inhibitor of trypsin-like serine proteases. Its mechanism of action involves the selective blockade of these enzymes, which are implicated in various inflammatory processes. UAMC-00050 is particularly useful in research focused on dry eye syndrome and ocular inflammation, providing a valuable tool for elucidating the underlying mechanisms and potential therapeutic interventions in these conditions. -
Mast Cell Tryptase Inhibitor
APC 366 hydrochloride is a selective inhibitor of mast cell tryptase, specifically targeting its enzymatic activity. This compound effectively inhibits tryptase-induced histamine release in human tonsil and lung cells, highlighting its potential role in the modulation of allergic responses and inflammation. APC 366 hydrochloride is useful for research applications focusing on allergy-related mechanisms and inflammatory pathways. -
TPP II Inhibitor
Butabindide is a potent and selective inhibitor of tripeptidyl peptidase II (TPP II), exhibiting a Ki value of 7 nM for TPP II and a significantly higher Ki of 10 μM for TPP I. This compound effectively protects cholecystokinin-8 (CCK-8) from inactivation by inhibiting TPP II activity. Butabindide is valuable for research applications focused on TPP II-related pathways and the modulation of peptide activity in biological systems. -
Urinary Trypsin Inhibitor
Urinary Trypsin Inhibitor Fragment is a proteolytic fragment of urinary trypsin inhibitor that specifically targets protease activity. This fragment has been shown to inhibit tumor cell invasion, making it valuable for studies focused on cancer progression and metastasis. Its application extends to investigating the role of proteolytic regulation in various biological processes. -
Trypsin Inhibitor
Trypsin-IN-2 is a potent and highly selective inhibitor of human trypsin, exhibiting an IC₅₀ of 8 nM. This compound is valuable for studying the role of trypsin in various biological processes, particularly in the context of pancreatic cancer research. Its specificity and efficacy make it an important tool for elucidating the mechanisms underlying trypsin-related pathologies. -
WNK1 Inhibitor
Tyrphostin 47 is a potent inhibitor of WNK1, classified as a protein tyrosine kinase inhibitor. This compound effectively suppresses the proliferation of smooth muscle cells, making it a valuable tool for studying vascular biology and related pathologies. Tyrphostin 47 is utilized in various research applications focused on cellular signaling and growth regulation. -
Serine Proteinase Inhibitor
L 658758 is a potent inhibitor of serine proteinases, primarily targeting the active site of these enzymes. This compound exhibits strong biological activity, making it valuable for studies investigating proteolytic processes and related pathways. Research applications include elucidating the role of serine proteinases in various physiological and pathological conditions, as well as in drug discovery aimed at modulating these targets. -
cGKII Inhibitor
AP-C2 is a selective inhibitor of guanosine 3',5'-cyclic monophosphate-dependent protein kinase II (cGKII), exhibiting a pIC50 value of 5.2. This compound effectively modulates cGKII activity, making it a valuable tool in investigating cGMP signaling pathways. It is particularly relevant for research focused on cardiovascular biology and renal function, where cGKII plays a crucial role in cellular signaling. -
Kallikrein Inhibitor
Kallikrein-IN-2 is a selective inhibitor of kallikrein, a serine protease involved in the kinin-generating cascade. By modulating kallikrein activity, this compound plays a significant role in regulating blood pressure, inflammation, and pain signaling. Kallikrein-IN-2 is valuable for research applications focused on cardiovascular diseases, inflammatory disorders, and pain management studies, providing insights into the therapeutic potential of targeting the kallikrein-kinin system. -
CRNSP Inhibitor
Z-APF-CMK is a selective inhibitor of the Ca2+-regulated nuclear scaffold protease (CRNSP). It exhibits potent inhibition of CRNSP activity, which plays a crucial role in nuclear signaling and cellular regulation. This compound is invaluable for research applications focused on delineating the function of CRNSP in various cellular processes and its implications in disease mechanisms. -
Protease Inhibitor
Patamostat mesylate is a potent protease inhibitor that primarily targets trypsin, plasmin, and thrombin, exhibiting IC50 values of 39 nM, 950 nM, and 1.9 μM, respectively. This compound demonstrates significant inhibitory activity, which may play a role in modulating the pathogenesis and progression of acute pancreatitis. Its diverse protease inhibition profile positions Patamostat mesylate as a valuable tool for research into protease-related diseases and therapeutic strategies. -
DCLK1 Inhibitor
DCLK1-IN-5 is a selective DCLK1 inhibitor with an IC50 of 179.7 nM. It effectively mitigates lipopolysaccharide-induced inflammation by inhibiting DCLK1-mediated IKKβ phosphorylation. Research has demonstrated that DCLK1-IN-5 provides protective effects in mouse models against inflammation-induced lung injury and sepsis, making it valuable for studies exploring inflammatory pathways and potential therapeutic interventions. -
Aspartic Proteinases Inhibitor
CP 81282 is a tripeptide inhibitor of aspartic proteinases, demonstrating potent activity with an IC50 of 1 nM against human renin and 11 nM against endopeptidase. This compound is particularly relevant for research focused on hypertension, providing valuable insights into the regulation of blood pressure and related cardiovascular conditions. -
Tryptase Inhibitor
BMS-354326 is a potent tryptase inhibitor with an IC50 of 1.8 nM, demonstrating exceptional selectivity towards tryptase and minimal activity against most other serine proteases. This compound is valuable for research focused on asthma and various inflammatory diseases, facilitating the exploration of tryptase's role in these conditions. BMS-354326 provides a useful tool for investigating the implications of tryptase inhibition in therapeutic strategies. -
Tryptase Inhibitor
BMS-363131 is a selective inhibitor of tryptase, exhibiting an IC50 of less than 1.7 nM. It demonstrates hydrolytic stability at physiological pH levels (7 and 9). BMS-363131 has been shown to attenuate asthma symptoms in guinea pig models, making it a valuable tool for studying respiratory diseases and therapeutic interventions. -
Serine Proteases Inhibitor
VD4162 is a macrocyclic inhibitor targeting serine proteases, demonstrating enhanced potency against TMPRSS2 (IC50 = 3.7 nM), HGFA (IC50 = 3.3 nM), matriptase (IC50 = 2.9 nM), and hepsin (IC50 = 0.54 nM). This compound is valuable for cancer research, providing insights into the role of serine proteases in tumor progression and potential therapeutic interventions. -
Tryptase Inhibitor
JNJ-27390467 is a highly selective inhibitor of human β-tryptase, exhibiting an IC50 of 3.6 nM and a Ki of 3.7 nM. With approximately 5000-fold selectivity over trypsin, this compound demonstrates significant biological activity in animal models of airway inflammation. JNJ-27390467 is ideally suited for research applications related to allergic asthma, providing a valuable tool for exploring therapeutic avenues in respiratory conditions. -
Trypsin-like Serine Proteases Inhibitor
APC-6860 is a potent inhibitor of trypsin-like serine proteases, exhibiting inhibition constants (Ki) of 0.21 μM for urokinase (uPA) and 0.44 μM for trypsin. It selectively inhibits tissue-type plasminogen activator (tPA) with an impressive selectivity ratio of 80 compared to uPA. APC-6860 demonstrates Ki values of 0.1 μM for human urokinase and 0.082 μM for murine urokinase, making it a valuable tool in cancer research and related studies focused on protease activity.

