Serine Protease

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  1. 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.
  2. 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.
  3. Subtillsin Substrate

    Fluorescent Substrate for Subtilisin is designed to specifically detect the enzymatic activity of subtilisin, a bacterial serine protease. This substrate provides a sensitive and quantifiable method to evaluate subtilisin activity in various biological assays. It is suitable for applications in enzyme activity studies and protease-related research.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. Serine Protease

    Complement factor D is a serine protease that plays a critical role in the complement system by activating C3 convertase through the specific cleavage of complement Factor B. This enzyme is essential for modulating immune responses and is promising for research in autoimmune diseases, such as paroxysmal nocturnal hemoglobinuria and C3 glomerulopathy, as well as conditions like age-related macular degeneration and thrombotic microangiopathies. Its study can provide insights into the underlying mechanisms of these diseases and potentially guide therapeutic development.
  12. 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.
  13. Chymotrypsin Substrate

    Ac-Phe-Gly-pNA is a substrate specific for chymotrypsin, a serine protease. This compound undergoes enzymatic cleavage by chymotrypsin, resulting in the release of para-nitroaniline (pNA), which can be quantitatively measured, allowing for the assessment of enzyme activity. Ac-Phe-Gly-pNA is widely utilized in biochemical assays for studying chymotrypsin function and its kinetics in various biological research applications.
  14. Fluorogenic Substrate

    Boc-Ala-Gly-Pro-Arg-AMC is a fluorogenic substrate designed for monitoring protease activity, particularly within serine proteases. This substrate is ideal for assessing enzymatic function in research applications involving protease activity, such as studying the oligopeptide enzyme B of Trypanosoma brucei. Its fluorescence allows for sensitive detection of enzymatic events, making it a valuable tool in biochemical and molecular biology studies.
  15. Enzyme Substrate

    Ala-Phe-Pro-βNA is a substrate for prolyl tripeptidyl aminopeptidase derived from Porphyromonas gingivalis. This compound exhibits potent binding affinity toward H-Ala-Ile-pyrrolidin-2-yl boronic acid, demonstrating Ki values of 88.1 nM for PTP39 and 48.8 nM for the E636A mutant. It is valuable for research applications involving enzyme activity assays and studies of proteolytic processes.
  16. TNIK Inhbitor

    TNIK-IN-2 is a selective inhibitor of Traf2- and Nck-interacting protein kinase (TNIK) with an IC50 of 1.3337 μM. This compound is primarily utilized in research to investigate its potential role in colorectal cancer (CRC) progression and therapeutic targeting. Its inhibition of TNIK may provide insights into the molecular mechanisms underlying CRC and support the development of novel treatment strategies.
  17. Fluorogenic Substrate

    Boc-Glu(OBzl)-Ala-Arg-AMC serves as a fluorogenic substrate specifically for coagulation factor XIa and trypsin. The enzymatic cleavage of the amide bond located between arginine and the methylcoumarin amide moiety leads to the release of the fluorescent compound 7-Amino-4-methylcoumarin. This reagent is valuable for research applications focused on protease activity detection and the study of coagulation pathways.
  18. 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.
  19. E-isomer of Upamostat

    (E)-Upamostat is an E-isomer of Upamostat, functioning primarily as an orally active serine protease inhibitor. This compound has demonstrated significant biological activity in modulating protease activity, making it valuable in research focused on cancer biology and therapeutic development. Its mechanisms of action and potential in various studies highlight its importance in the exploration of proteolytic processes and associated disorders.
  20. Rhodamine Derivative

    (Z-AR)2Rh110 is a Rhodamine derivative that serves as a fluorescent probe. Its primary mechanism involves hydrolysis by trypsin, which enables the study of proteolytic activity. This compound is utilized in various applications, including fluorescent imaging and tracking cellular processes in biochemical assays.
  21. 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.
  22. KIAA1363 Substrate

    2-thioacetyl MAGE is a colorimetric substrate specifically designed for the serine hydrolase enzyme KIAA1363. This compound facilitates the assessment of KIAA1363 enzymatic activity, enabling researchers to study its biological functions and implications in various cellular processes. Its application in biochemical assays contributes to the understanding of KIAA1363's role in health and disease.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. TMPRSS6 Synthesis Reducer

    Manusiran (SLN124) is a GalNAc-conjugated 19-mer siRNA targeting TMPRSS6 (transmembrane protease serine 6). It effectively reduces plasma iron levels while increasing hepcidin expression in healthy individuals. This compound is primarily used in research applications focused on iron metabolism and disorders related to iron homeostasis.
  30. 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.
  31. 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.
  32. 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.
  33. Human Kallikrein 6 Substrate

    Abz-AFRFSQ-EDDnp is a substrate specifically designed for human kallikrein 6, exhibiting a catalytic efficiency of Kcat/Km = 38667 s-1 mM-1. This compound facilitates the study of kallikrein 6 activity and is instrumental in various biological assays aimed at exploring protease functionalities and related pathways. Its application is essential in research focused on cancer, neurodegenerative diseases, and other physiological processes where kallikrein 6 plays a pivotal role.
  34. 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.
  35. 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.
  36. Plant Growth Signaling Molecule

    6-O-Bis[1-(2-nitrophenyl)-ethoxyphosphoryl]-D-trehalose is a signaling molecule that modulates carbon utilization and growth in plants. This compound activates the release of trehalose-6-phosphate (T6P) upon light exposure, facilitating starch synthesis and promoting growth by inhibiting SnRK1, a kinase that plays a crucial role in cellular energy conservation. 6-O-Bis[1-(2-nitrophenyl)-ethoxyphosphoryl]-D-trehalose is valuable for investigating mechanisms of plant growth and metabolism.
  37. Recombinant Human Factor IX

    Nonacog alfa is a recombinant human Factor IX, primarily utilized in the study of haemophilia B. This biologically active protein plays a critical role in the coagulation cascade, facilitating blood clotting in individuals deficient in Factor IX. Research applications include elucidating the mechanisms of haemostasis and developing therapeutic strategies for managing bleeding disorders.
  38. Probe

    4-Iodobenzylamine hydrochloride is a chemical probe that selectively interacts with serine proteases, including trypsin and urokinase-type plasminogen activator (uPA). This reagent facilitates the study of enzyme binding patterns and can aid in understanding enzymatic roles in various biological processes. Its applications extend to research in protease activity and modulation in disease models.
  39. 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.
  40. Plasminogen Activator

    Staphylokinase is a plasminogen activator derived from Staphylococcus aureus. This potent enzyme exhibits fibrin-specific thrombolytic activity, facilitating the conversion of plasminogen to plasmin. Staphylokinase is utilized in research focused on fibrinolysis and related cardiovascular studies, offering valuable insights into thrombus resolution mechanisms.
  41. 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.
  42. 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.
  43. 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.
  44. Urokinase Substrate

    Ac-Gly-Lys-OMe is a substrate for urokinase, primarily utilized to evaluate the enzymatic activity of this serine protease. This reagent is essential for investigating the effects of small molecule inhibitors on urokinase function in various biochemical assays and research applications focused on fibrinolysis and related pathways.
  45. 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.
  46. TNIK Modulator

    TNIK modulator-1 is a selective modulator of TNIK, a protein kinase involved in Wnt signaling pathways and neuronal development. This compound has been shown to enhance neuronal differentiation and may play a role in neurodevelopmental disorders. Its ability to regulate TNIK activity makes it a valuable tool for research in neurobiology, cancer, and regenerative medicine.
  47. 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.
  48. 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.
  49. 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.

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