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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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.
