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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
uPA Activator
UK-356202 is a potent urokinase-type plasminogen activator (uPA) inhibitor, exhibiting a Ki value of 0.037 μM. This compound plays a significant role in modulating fibrinolysis and cellular processes associated with wound healing. Its primary applications include research focused on the topical treatment of chronic ulcerous wounds, providing insights into therapeutic strategies for enhancing tissue repair and regeneration. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
Thrombin Inactivator
Dermatan sulphate sodium is a glycosaminoglycan that functions as a thrombin inactivator, exhibiting significant antithrombotic activity. It selectively enhances the heparin cofactor II-mediated inactivation of thrombin without affecting antithrombin III. This compound has been shown to promote stem cell differentiation and may alleviate pulmonary fibrosis induced by Bleomycin. Dermatan sulphate sodium is utilized in research focused on cardiovascular diseases, inflammation, and stem cell biology. -
Thrombin Receptor Agonist
TRAP-14 (SFLLRNPNDKYEPF) is a synthetic peptide that acts as an agonist for the thrombin receptor. This compound is utilized in research to study thrombin signaling pathways and their implications in various physiological and pathological processes. Its ability to activate the thrombin receptor makes it valuable for investigating thrombosis, inflammation, and cardiovascular diseases. -
Thrombin Inhibitor
BAY 1217224 is a selective thrombin inhibitor that acts through competitive binding to the active site of thrombin, resulting in the inhibition of fibrinogen conversion and clot formation. This compound demonstrates favorable oral pharmacokinetics, making it suitable for in vivo studies. BAY 1217224 is primarily utilized in research focused on coagulation pathways and the development of anticoagulant therapies. -
Thrombin Inhibitor
(2S,4S)-Argatroban is a potent inhibitor of human thrombin, exhibiting a Ki value of 280 μM. This compound is primarily utilized in research focused on thrombotic diseases and coagulation disorders. Its mechanism of action provides a valuable tool for studying thrombin's role in physiology and pathology, as well as for the development of therapeutic strategies targeting blood coagulation pathways. -
Thrombin Inhibitor
Corthrombin is a highly potent alpha-keto-amide thrombin inhibitor, exhibiting a Ki value of 1 pM. This compound is utilized in the study of cardiovascular diseases, providing valuable insights into thrombin-related mechanisms and potential therapeutic interventions. Its high specificity and efficacy make it an essential tool for research focused on coagulation processes and thrombotic disorders. -
Thrombin Receptor Antagonist
Thrombin receptor peptide ligand is a selective antagonist of the thrombin receptor, inhibiting its activation and downstream signaling. This compound exhibits antithrombotic properties, making it suitable for research focused on thrombotic disorders and cardiovascular diseases. Its ability to modulate thrombin activity positions it as a valuable tool for studying platelet aggregation and related pathways. -
Thrombin Inhibitor
Flovagatran is a potent and reversible thrombin inhibitor, characterized by a Ki value of 9 nM. This compound is primarily utilized in research related to arterial and venous thrombosis, providing valuable insights into thrombotic mechanisms and potential therapeutic interventions. -
Thrombin Inhibitor
Hirullin P18 is a potent thrombin inhibitor that effectively modulates coagulation pathways. This compound exhibits significant anticoagulant activity, making it valuable for research applications focused on thrombus formation and cardiovascular disorders. Hirullin P18 is an essential tool for studying thrombin-related biological processes and developing therapeutic strategies for thrombotic diseases. -
Thrombin Inhibitor
Sofigatran is an orally active thrombin inhibitor that functions as an anticoagulant by selectively targeting factor IIa. This compound exhibits significant biological activity in modulating blood coagulation pathways and is particularly relevant in cardiovascular disease research. Its utility in preclinical studies facilitates the exploration of its therapeutic potential in managing thrombotic disorders. -
Neutral Thrombin Inhibitor
AZD-8165 is a highly selective neutral thrombin inhibitor that demonstrates potent anticoagulant properties. This compound is primarily utilized in research related to cardiovascular diseases, including hypertension and heart failure. Its mechanism of action aids in elucidating thrombotic processes and evaluating therapeutic strategies in related cardiovascular conditions. -
α-Thrombin Substrate
Sar-Pro-Arg-pNA serves as a chromogenic substrate specifically for α-thrombin. It enables the assessment of α-thrombin activity through colorimetric measurements, making it a valuable tool in coagulation studies and thrombin activity assays. This substrate is suitable for research applications that investigate thrombin's role in hemostasis and related disorders. -
Thrombin Inhibitor
L 373890 is a selective thrombin inhibitor characterized by its low Ki value of 0.5 nM, indicating potent activity against thrombin. This compound exhibits high selectivity, showing a significantly reduced Ki of 570 nM for trypsin and minimal inhibition of other serine proteases, such as plasmin and tPA. L 373890 is a valuable tool for researchers investigating thrombosis and related cardiovascular disorders. -
Thrombin Inhibitor
Efegatran is a potent thrombin inhibitor that effectively prevents platelet aggregation. Its anticoagulant and antithrombotic properties make it valuable for research applications focused on cardiovascular health and clotting disorders. This compound serves as an important tool for studying thrombin-related mechanisms and evaluating potential therapeutic strategies in the management of thromboembolic diseases. -
Thrombin Inhibitor
Atecegatran TFA is a selective direct thrombin inhibitor that acts as a potent anticoagulant. It plays a significant role in the management of cardiovascular diseases by effectively inhibiting thrombin, thereby preventing thrombus formation. The active form of this compound, AR-H067637, is critical for its anticoagulation effects and is utilized in various research applications focused on thrombotic disorders and cardiovascular health.

