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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/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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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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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). -
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
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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). -
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
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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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. -
Neutrophil elastase inhibitor
Sivelestat sodium is a competitive inhibitor of human neutrophil elastase, also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse. -
PCSK9 inhibitor
SBC-110736 is a proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitor extracted from patent WO2014150395A1, Figure 1. -
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. -
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. -
14-3-3 Protein-Protein Interaction Inhibitor
(E)-FOBISIN101 is a selective inhibitor of 14-3-3 protein-protein interactions, demonstrating IC50 values of 9.3 μM and 16.4 μM for the disruption of 14-3-3ζ and 14-3-3γ binding to PRAS40, respectively. This compound also inhibits 14-3-3's interactions with Raf-1 and proline-rich AKT substrates, and it neutralizes the activating effect of 14-3-3 on exotoxin S ADP-ribosyltransferase. (E)-FOBISIN101 is valuable for research into 14-3-3-mediated pathways in cancer biology. -
VRK1 Inhibitor
VRK-IN-1 is a selective inhibitor of vaccinia-related kinase 1 (VRK1), with an IC50 value of 150 nM. This compound modulates the activity of human Ser/Thr protein kinases that are implicated in enhanced cell division and various neurological disorders. Its application in research may provide insights into cellular proliferation and potential therapeutic approaches for neurological conditions. -
WNK1 Inhibitor
WNK1-IN-1 is a selective inhibitor of WNK1, exhibiting an IC50 of 1.6 μM. It effectively inhibits the phosphorylation of OSR1 with an IC50 of 4.3 μM. This compound is relevant for studies focused on blood pressure regulation and various aspects of cancer research, making it a valuable tool for elucidating the role of WNK1 in pathophysiological processes. -
KIAA1363/AADACL1 Inhibitor
JW480 is a selective inhibitor of KIAA1363/AADACL1 that displays potent oral bioactivity, with IC50 values of 12 nM against human KIAA1363 and 20 nM against mouse KIAA1363. Its mechanism involves inhibition of lipid deacetylase activity, which suppresses HAG metabolism and reduces retinyl ester hydrolase function in hepatic stellate cells. JW480 has demonstrated significant effects in reducing MAGE lipid levels and inhibiting critical processes such as migration, invasion, and tumor growth in prostate cancer cells. Additionally, it impacts platelet function and thrombosis, making it a valuable reagent for research in prostate cancer and thrombotic disorders. -
Protease Inhibitor
Benzamidine is a competitive protease inhibitor targeting enzymes such as plasmin, trypsin, and thrombin, effectively preventing the hydrolytic cleavage of glucagon. It is primarily employed to stabilize glucagon in human plasma and blood samples during collection, storage, and analysis, thereby ensuring accurate detection outcomes in research applications. While Benzamidine can induce slight single-strand DNA breaks at elevated concentrations, it demonstrates minimal overall genotoxicity. Additionally, it may interfere with certain glucagon antisera, although it does not significantly impact the affinity of key antigen-antibody interactions at specific concentrations. -
CITK Inhibitor
C3TD879 is a potent CITK inhibitor that targets the catalytic activity of CITK with an IC50 of 12 nM. It demonstrates a strong binding affinity for full-length human CITK in cellular assays, with a NanoBRET Kd of less than 10 nM. This compound serves as a valuable chemical probe for exploring the intricate biological functions associated with CITK, making it an essential tool for research in cell signaling and cancer biology. -
Trypsin Inhibitor
SFTI-1 is a cyclic peptide that functions as a potent trypsin inhibitor, comprising 14 amino acid residues. This compound is categorized within the Bowman-Birk class of inhibitors, notable for its remarkable stability and efficacy. SFTI-1 is a valuable tool for investigating peptide drug design and can significantly enhance research related to protease activity modulation. -
HTRA1 Inhibitor
HTRA1-IN-1 is a potent and selective inhibitor of high temperature requirement A serine peptidase 1 (HTRA1) with an IC50 of 13 nM. This compound is instrumental in research related to HTRA1-associated conditions, including age-related macular degeneration (AMD), osteoarthritis, and rheumatoid arthritis. By inhibiting HTRA1, it offers potential insights into therapeutic strategies for these diseases. -
PKR Inhibitor
PKR-IN-C51 is an ATP-competitive inhibitor of the double-stranded RNA-activated protein kinase (PKR), demonstrating an IC50 of 9 μM. This compound effectively inhibits intracellular PKR activation in a dose-dependent manner in primary mouse macrophages. PKR-IN-C51 is valuable for research into PKR-mediated signaling pathways and therapeutic strategies targeting inflammatory responses. -
Serine Proteases Inhibitor
Benzamidine hydrochloride hydrate is a reversible competitive inhibitor of serine proteases, specifically targeting trypsin-like enzymes. It exhibits inhibitory constants (Kis) of 20 μM for Tryptase, 21 μM for Trypsin, 97 μM for uPA, 110 μM for Factor Xa, 320 μM for Thrombin, and 750 μM for tPA. This compound is widely utilized in biochemical research to study proteolytic processes and enzyme activity related to various physiological and pathological conditions. -
Trypsin Inhibitor
Camostat is an orally active inhibitor of trypsin, functioning by modulating proteolytic activity in various biological systems. This compound has demonstrated the ability to reduce pancreatic fibrosis in experimental models, specifically by inhibiting the proliferation and activation of pancreatic stellate cells (PSCs). Camostat serves as a valuable tool in research investigating pancreatic diseases and fibrosis-related mechanisms. -
Matriptase Inhibitor
Matriptase-IN-2 is a selective inhibitor of matriptase, a serine protease implicated in cartilage matrix degradation associated with osteoarthritis. With a Ki value of 5 nM, this secondary amide compound effectively inhibits matriptase activity, thereby preventing cartilage degradation. Matriptase-IN-2 is designed for research applications focused on understanding the role of matriptase in osteoarthritis pathology and potential therapeutic strategies. -
Serine/Threonine Kinase Inhibitor
Tilpisertib is a selective serine/threonine kinase inhibitor that targets key signaling pathways involved in cellular proliferation and survival. It has demonstrated significant antitumor activity, making it a valuable tool for cancer research and drug development. This compound is particularly useful for studying mechanisms of resistance in cancer therapies and evaluating the therapeutic potential of kinase inhibition in various tumor models. -
proteinase K inhibitor
MeOSuc-AAPF-CMK is a potent inhibitor of proteinase K, acting through the binding of its active site. This compound is primarily utilized in biochemical research to study protein degradation and enzyme inhibition mechanisms. Its effectiveness in blocking proteinase K activity makes it a valuable tool for investigating proteolytic pathways and cellular processes involving protein turnover. -
Hepsin Inhibitor
Hepln-13 is a selective Hepsin inhibitor, demonstrating an IC50 of 0.33 μM. Its potency and oral bioavailability make it a valuable tool for investigating the role of Hepsin in metastatic prostate cancer. Researchers can employ Hepln-13 to explore therapeutic strategies targeting Hepsin-mediated pathways in cancer progression. -
TNIK Inhibitor
TNIK-IN-1 is a potent inhibitor of Traf2 and Nck-interacting kinase (TNIK), exhibiting an IC50 of 65 nM. This compound demonstrates significant antitumor activity and is valuable for research investigating the role of TNIK in cancer progression and proliferation. Applications include studying TNIK-mediated signaling pathways and exploring its potential as a therapeutic target in oncology. -
Sperm Acrosin Inhibitor
4-Nitrophenyl 4-guanidinobenzoate hydrochloride is a potent inhibitor of sperm acrosin, a serine protease involved in fertilization. Its mechanism of action facilitates the inhibition of acrosin activity, crucial for sperm-egg fusion. Additionally, this compound acts as a substrate for trypsin, making it valuable for biochemical studies in protease activity and regulation. Researchers can utilize it in studies focused on reproductive biology and enzyme kinetics. -
Mast Cell Tryptase Inhibitor
APC 366 is a selective inhibitor of mast cell tryptase, exhibiting a Ki of 7.1 μM. This compound effectively inhibits antigen-induced early and late asthmatic responses, as well as bronchial hyperresponsiveness in sheep models of allergic asthma. APC 366 serves as a valuable tool for research in asthma pathophysiology and the development of therapeutic strategies targeting mast cell activity. -
TNIK Inhibitor
TNIK-IN-7 is a selective inhibitor of Traf2 and Nck-interacting kinase (TNIK), exhibiting an IC50 of 11 nM. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its specificity for TNIK allows for the exploration of signaling pathways involved in tumor progression and offers potential insights into targeted therapies for various cancers. -
Serine/threonine Kinase Inhibitor
Tilpisertib fosmecarbil TFA is the trifluoroacetic acid salt form of Tilpisertib, a potent inhibitor of serine/threonine kinases. This compound exhibits significant anti-inflammatory activity, making it valuable for research applications focused on inflammatory pathways and related diseases. Its mechanism of action allows for detailed exploration of kinase-related signal transduction processes in cellular models. -
Protease Inhibitor
Patamostat is a potent protease inhibitor targeting trypsin, plasmin, and thrombin, with IC50 values of 39 nM, 950 nM, and 1.9 μM, respectively. This compound has demonstrated potential in suppressing the pathogenesis and development of acute pancreatitis. Its efficacy in inhibiting critical proteolytic enzymes makes Patamostat a valuable tool for research into protease-related disorders and therapeutic interventions. -
Matriptase Inhibitor
Matriptase-IN-2 free base is a potent matriptase inhibitor, exhibiting a Ki of 5 nM. This compound has significant potential for research applications focused on disorders of the musculoskeletal system. It provides a valuable tool for investigating the role of matriptase in various biological processes and therapeutic interventions. -
TNIK Inhibitor
PF-794 is a selective and potent inhibitor of Traf2- and Nck-interacting kinase (TNIK), exhibiting an IC50 of 39 nM. This ATP-competitive compound specifically targets the TNIK family, leading to a reduction in endogenous p120-catenin phosphorylation in cellular models. PF-794 is utilized in research related to psychiatric disorders, providing a valuable tool for studying the underlying mechanisms of these conditions. -
TAO Kinase Inhibitor
TAO Kinase Inhibitor 2 targets TAO Kinase and exhibits inhibitory activity with an IC50 range of 50 to 500 nM. Additionally, this compound inhibits KIAA1361 and JIK within the same IC50 range. Its selectivity and potency make it a valuable tool for studying the role of TAO Kinase and its related pathways in various biological contexts and disease models. -
Protease Inhibitor
[Des-Pro2]-Bradykinin is a potent protease inhibitor that effectively prevents the degradation of methionine enkephalin. By inhibiting proteolytic enzymes, it enhances the stability and activity of enkephalins, which are important neuropeptides involved in pain modulation and stress response. This reagent is valuable for studies focused on neurobiology, pain research, and peptide pharmacology. -
HGF-activating Serine Proteases Inhibitor
VD2173 is a macrocyclic peptide inhibitor specifically targeting HGF-activating serine proteases, including matriptase and hepsin. Demonstrating potent inhibition, VD2173 serves as a valuable tool for investigating the role of these proteases in various biological processes. Its use in research on lung cancer can elucidate mechanisms of tumor progression and potential therapeutic interventions.

