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Catalog No.
Product Name
Application
Product Information
Citations
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Trypsin-like Serine Protease Inhibitor
UAMC-00050 free base is a potent inhibitor of trypsin-like serine proteases. This compound exhibits significant biological activity in research focused on dry eye syndrome and ocular inflammation, providing valuable insight into therapeutic strategies for managing these conditions. -
Plasmin Activity Inhibitor
D-Val-Phe-Lys-CMK is a potent inhibitor of plasmin activity, functioning through its chloromethyl ketone moiety. This compound is utilized in research to explore mechanisms of fibrinolysis and its regulation in various pathological conditions. Applications include studies on thrombolytic therapy and the role of plasmin in tissue remodeling and cancer progression. -
Protease Inhibitor
Aureoquinone functions as a broad-spectrum protease inhibitor, targeting various proteases including trypsin, papain, thermophilic protease, collagenase, and pound-protease. It demonstrates inhibition with IC50 values of 11.4 μg/mL, 14.5 μg/mL, 17.8 μg/mL, 7.1 μg/mL, and 8.7 μg/mL, respectively. Aureoquinone is useful in research applications focused on proteolytic processes and the study of protease-related pathways. Its inhibition profiles make it a valuable tool for investigations in cellular and molecular biology. -
Plasminogen Inhibitor
Cetyl tranexamate hydrochloride is a selective inhibitor of plasminogen, functioning by blocking fibrinogen activation. This compound significantly diminishes the production of fibrinogen in keratinocytes, particularly in response to ultraviolet damage, thereby indirectly reducing melanin synthesis. Additionally, cetyl tranexamate hydrochloride targets both melanin and hemoglobin, mitigating vascular dilation and pigmentation through the inhibition of inflammatory mediators such as prostaglandins and platelet-activating factors. Its applications include the treatment of epidermal pigment disorders, including photoaging, post-inflammatory hyperpigmentation, and melasma, making it suitable for various cosmetic formulations. -
Chymotrypsin Inhibitor
Chymotrypsin-IN-1, also known as Compound TPCK, is a potent irreversible inhibitor of chymotrypsin-like serine proteases. By targeting the active site of chymotrypsin, this compound effectively inhibits enzymatic activity, making it valuable for studies related to protein digestion and regulation of proteolytic pathways. Its applications extend to biomedical research, particularly in the investigation of protease function and the development of therapeutics for conditions associated with dysregulated proteolytic activity. -
WNK Inhibitor
WNK-IN-2 is an ATP-competitive inhibitor of WNK kinases, exhibiting low selectivity for other kinases. This compound effectively modulates intracellular signaling pathways involving WNK kinases, which play crucial roles in regulating ion transport and blood pressure. WNK-IN-2 is ideal for research applications focused on elucidating the functions of WNK signaling in various physiological and pathological conditions. -
Proteinase Inhibitor
Midesteine is a proteinase inhibitor that effectively inhibits porcine pancreatic elastase, human neutrophil elastase, and bovine chymotrypsin. This compound demonstrates significant potential for research applications related to chronic obstructive pulmonary disease (COPD) and chronic bronchitis, making it a valuable tool for studying respiratory diseases and their underlying mechanisms. -
Serine Proteases Neutrophil Elastase/Proteinase-3 Inhibitor
CE-2072 is an inhibitor of serine proteases, specifically targeting neutrophil elastase and proteinase-3. This compound demonstrates significant activity in reducing HIV-1 production and p24 levels in IL-18 or NaCl-stimulated U1 monocytic cells and peripheral blood mononuclear cells. Additionally, CE-2072 effectively inhibits HIV-1 infection in permissive HeLa cells. Its ability to suppress the transcription factor NF-kB activation in U1 cells highlights its potential in HIV-1-related disease research applications. -
Serine Protease Inhibitor
Laccaridione A acts as a potent serine protease inhibitor, effectively inhibiting various proteolytic enzymes including trypsin, papain, thermophilic protease, collagenase, and zinc protease, with IC50 values of 14.7 μg/mL, 2.5 μg/mL, 18.8 μg/mL, 7.2 μg/mL, and 18.2 μg/mL, respectively. This compound is valuable for studying protease activity and regulation in biological systems, making it a useful reagent in biochemical and pharmacological research applications. Its selective inhibitory properties can aid in elucidating the roles of serine proteases in various physiological and pathological processes. -
Serine Protease Inhibitor
Laccaridione B is a potent inhibitor of serine proteases, effectively inhibiting the activity of trypsin, papain, thermophilic protease, collagenase, and zinc protease with IC50 values of 10.9 μg/mL, 5.1 μg/mL, 8.4 μg/mL, 5.7 μg/mL, and 3.0 μg/mL, respectively. Additionally, Laccaridione B demonstrates significant anti-proliferative properties against various cell lines, including L-929, K-562, and HeLa cells, with IC50 values of 2.4 μg/mL, 1.8 μg/mL, and 13.9 μg/mL, respectively. These attributes make Laccaridione B a relevant compound for research in cancer biology and protease inhibition studies. -
Serine Racemase Inhibitor
L-Serine-O-sulfate potassium is an inhibitor of serine racemase (Srr), a key enzyme involved in the synthesis of D-serine, which is implicated in various neurological processes. This compound has been shown to significantly reduce chronic constriction injury (CCI)-induced increases in nitric oxide levels, nNOS phosphorylation at Ser847, and PKC-dependent GluN1 phosphorylation at Ser896. Additionally, L-Serine-O-sulfate potassium is valuable for investigating the mechanisms of peripheral neuropathy and exploring potential therapeutic interventions. -
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. -
Serine/Threonine Kinase Inhibitor
Tilpisertib fosmecarbil is a potent inhibitor of serine/threonine kinases, demonstrating significant anti-inflammatory activity. This compound is valuable for research focused on inflammatory pathways and related signaling mechanisms. Its application may extend to studies investigating various diseases associated with dysregulated kinase activity. -
WNK Inhibitors
STOCK2S-26016 is a selective inhibitor of the WNK (With No K) signaling pathway, targeting WNK4 and WNK1 with IC50 values of 16 μM and 34.4 μM, respectively. This compound exhibits potential biological activity in the modulation of blood pressure regulation and hypertension-related research applications. Its specificity for WNK kinases makes it a valuable tool for studying the physiological and pathological roles of WNK signaling in various cellular processes. -
Tryptase Inhibitor
CRA-2059 is a highly selective tryptase inhibitor with a Ki of 620 pM for recombinant human tryptase-β (rHTβ). This compound demonstrates potent inhibition of tryptase activity, making it a valuable tool for research focused on allergic responses and tissue remodeling. Its specificity for tryptase positions CRA-2059 as an important reagent in studies of inflammatory diseases and related therapeutic development. -
TMPRSS6 Inhibitor
TMPRSS6-IN-1 is a potent inhibitor of TMPRSS6 (Matriptase-2), a type II transmembrane serine protease (TTSP). Inhibition of TMPRSS6 has been shown to alleviate symptoms associated with conditions such as hemochromatosis and beta thalassemia in preclinical models. This compound is valuable for studies targeting iron metabolism and therapeutic strategies aimed at managing related disorders. -
HtrA Serine Protease Inhibitor
JO146 is a selective inhibitor of the Chlamydia trachomatis high-temperature requirement A (CtHtrA) serine protease, exhibiting IC50 values of 21.86 μM for CtHtrA and 1.15 μM for human neutrophil elastase (HNE). This compound effectively inhibits the proteolytic activity associated with bacterial infections, making it a valuable tool for research into Chlamydia pathogenesis and potential therapeutic interventions. Its ability to target HtrA highlights its relevance in studies focused on bacterial virulence factors and protease biology. -
Protease Inhibitor
(Rac)-Telmesteine is a protease inhibitor that functions as an enzyme stabilizer. This compound is utilized in various applications, including enhancing the stability of proteases in detergents and cleaning agents. Its role as an enzyme stabilizer makes it applicable in research focused on enzyme activity and formulation development in the detergent industry. -
TMPRSS6 Inhibitor
MD5 is a selective inhibitor of TMPRSS6, demonstrating an IC50 of 22 nM and a Ki of 3.4 nM for recombinant human TMPRSS6. It shows limited inhibition of Matriptase, with an IC50 of 352 nM and a Ki of 99.2 nM, and a weak effect on thrombin (Ki of 120 nM). Due to its favorable target specificity and initial drug-like properties, MD5 is suitable for research into iron overload diseases, including hereditary hemochromatosis and β-thalassemia. -
Tryptase Inhibitor
AMG-126737 is a highly selective oral inhibitor of human mast cell tryptase, exhibiting a Ki value of 90 nM. This compound effectively suppresses both early and late-phase bronchoconstriction in sheep models. AMG-126737 is an important tool in the research of asthma and allergic diseases, enabling investigations into novel therapeutic strategies for these conditions. -
FXIIa Inhibitor
Thrombin inhibitor 7 is a selective inhibitor of Factor XIIa (FXIIa) with an IC50 value of 28 nM, demonstrating strong potency. It exhibits minimal activity against Factor XIa (FXIa) with an IC50 value exceeding 132 µM. This compound's low cytotoxicity makes it suitable for various biochemical studies and therapeutic research focused on coagulation pathways. -
Plasminogen Activator Inhibitor
PAI-1, or Plasminogen Activator Inhibitor-1, is a critical regulator of fibrinolysis, functioning primarily as an inhibitor of tissue-type (tPA) and urokinase-type (uPA) plasminogen activators. As a member of the Ser Protease inhibitor superfamily, PAI-1 exhibits significant antiprotease activity. This reagent is widely utilized in research applications related to thrombosis, tissue remodeling, and cancer metastasis, providing valuable insights into the mechanisms underlying these complex biological processes. -
TNIK Inhibitor
TNIK-IN-4 is a selective inhibitor of TNIK (TRAF2 and NCK interacting kinase) with an IC50 of 0.61 μM. It demonstrates significant inhibitory activity against the colorectal cancer cell line HCT116, making it a valuable tool for studying TNIK's role in oncogenic signaling pathways. This reagent is suited for research applications focused on cancer biology and targeted therapeutic development. -
Serine Protease Inhibitor
Alpha 1 Antichymotrypsin, Human Plasma is a serine protease inhibitor involved in various physiological processes. Its presence in amyloid lesions is associated with Alzheimer’s disease, making it a significant marker in neurodegenerative research. This reagent is valuable for studies focused on Alzheimer's disease pathophysiology and related therapeutic investigations. -
Protease Inhibitor
Patamostat hydrochloride is a highly effective protease inhibitor, targeting trypsin, plasmin, and thrombin with IC50 values of 39 nM, 950 nM, and 1.9 μM, respectively. It demonstrates potential in suppressing the pathogenesis and progression of acute pancreatitis, making it a valuable tool for research focused on protease-related diseases and therapeutic interventions.
