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Catalog No.
Product Name
Application
Product Information
Citations
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NEP Inhibitor
SCH-34826 is an orally active neutral metalloendopeptidase (NEP) inhibitor that effectively reduces ANF degradation, thereby enhancing its antihypertensive and diuretic effects. This compound is valuable for research applications in cardiovascular and renal disease studies, allowing for deeper insights into the modulation of fluid balance and blood pressure regulation. -
Neprilysin Inhibitor
NEP-In-1 is a potent inhibitor of neprilysin (NEP), exhibiting an IC50 value of 2 nM for dNEP. This compound effectively modulates the activity of NEP, an enzyme involved in the degradation of bioactive peptides. NEP-In-1 is valuable for research applications investigating neuropeptide signaling pathways and potential therapeutic strategies in neurodegenerative disorders. -
NEP Inhibitor
SCH 42495 is an orally active neutral endopeptidase (NEP) inhibitor that exerts antihypertensive effects. As the ethyl ester proagent of SCH 42354, it is utilized in research applications focused on cardiovascular diseases and the modulation of peptide metabolism. This compound serves as a valuable tool for investigating the role of NEP in various physiological and pathological processes. -
Neprilysin Inhibitor
SQ28603 is a selective inhibitor of neprilysin (NEP), an enzyme involved in the degradation of numerous peptides including atrial natriuretic peptide (ANP). By inhibiting NEP, SQ28603 can enhance the levels of ANP and potentially influence cardiovascular and renal function. This compound is valuable for research into heart failure, hypertension, and other conditions where atrial natriuretic peptide regulation is crucial. -
Neprilysin Inhibitor
NEP-IN-2 is a selective inhibitor of neprilysin, an enzyme involved in the degradation of bioactive peptides. This compound is critical for studying its role in the context of cardiovascular diseases such as atherosclerosis and restenosis. Researchers can utilize NEP-IN-2 to investigate the effects of neprilysin inhibition on cell proliferation and related signaling pathways in these disease models. -
Thrombin Inhibitor, Plasmin Inhibitor
PPACK TFA is a potent and selective irreversible inhibitor of thrombin, demonstrating significant anticoagulant properties. It serves as an alternative to lithium heparin for blood gas and whole blood electrolyte analyses. Additionally, PPACK TFA inhibits plasminogen activator (rt-PA), interfering with its binding to plasma protease inhibitors, and mitigates plasmin-induced alterations in endothelial permeability and morphology in bovine aortic endothelial cell monolayers. This compound is valuable for investigations related to thrombosis and endothelial function. -
uPA Inhibitor
APC8696 is a reversible inhibitor of urokinase-type plasminogen activator (uPA), exhibiting a nanomolar inhibitory constant (Ki) of 8 nM. This compound is valuable for investigating uPA-mediated processes in various biological systems. It is particularly relevant in cancer research and studies addressing tissue remodeling and inflammation. -
uPA Inhibitor
UCD74A hydrochloride is a 5-substituted amiloride analog that functions as a selective inhibitor of urokinase-type plasminogen activator (uPA), exhibiting an IC50 of 110 μM. This compound modulates plasminogen activation cascades associated with extracellular matrix remodeling, making it valuable in the study of tumor metastasis. UCD74A hydrochloride serves as a useful tool for researchers investigating the underlying mechanisms of cancer progression and tissue invasion. -
Thrombin Inhibitor
PPACK dihydrochloride is a potent and selective irreversible inhibitor of thrombin. It serves as an alternative anticoagulant to lithium heparin for blood gas and electrolyte analyses in whole blood. Additionally, PPACK dihydrochloride inhibits plasminogen activator (rt-PA), preventing its binding to plasma protease inhibitors. This compound also reduces plasmin-induced endothelial permeability and morphological changes in bovine aortic endothelial cell monolayers, making it suitable for investigations in thrombosis-related research. -
uPA Inhibitor
ZK824190 hydrochloride is a selective inhibitor of the urokinase plasminogen activator (uPA), demonstrating promising potential for the treatment of multiple sclerosis. With IC50 values of 237 nM for uPA, and higher IC50s of 1600 nM and 1850 nM for tissue plasminogen activator (tPA) and Plasmin, respectively, this compound can effectively modulate pathways associated with neuroinflammation. Its oral bioavailability also supports its applicability in in vivo studies aimed at elucidating the role of uPA in various disease models. -
uPA Inhibitor
Bicyclic UK18 is a competitive inhibitor of human urokinase-type plasminogen activator (uPA), demonstrating a Ki value of 53 nM. This compound plays a significant role in modulating fibrinolytic activity, making it useful in research related to thrombolysis and cancer metastasis. Its selective inhibition of uPA allows for detailed investigations into tissue remodeling and inflammatory processes. -
uPA inhibitor
CJ-463 is a potent and selective inhibitor of urokinase plasminogen activator (uPA). It exhibits significant antitumor activity, making it a valuable tool for cancer research. This compound is primarily utilized to investigate the role of uPA in tumor progression and metastasis, and may facilitate the development of novel therapeutic strategies targeting uPA-related pathways. -
Prolyl Endopeptidase Inhibitor
SUAM 1221 is a potent inhibitor of prolyl endopeptidase, an enzyme involved in the metabolism of neuroactive peptides. This compound exhibits significant biological activity by modulating peptide levels, making it a valuable tool in Alzheimer’s disease research. Its application facilitates the exploration of therapeutic strategies aimed at neurodegeneration and cognitive decline. -
PREP Inhibitor
PREP inhibitor-1 is a potent prolyl oligopeptidase (PREP) inhibitor with an IC50 value of less than 1 nM. This compound selectively targets PREP, an enzyme involved in the modulation of neuropeptides and signaling pathways. Its high inhibitory activity makes it a valuable tool for research on neurodegenerative disorders and related neurological studies. -
Prolyl endopeptidase Inhibitor
Prolyl Endopeptidase Inhibitor 1 is a potent inhibitor of prolyl endopeptidase (PEP), with a Ki value of 15 nM. Its inhibitory action on PEP suggests potential applications in neurobiology, particularly for the investigation of cognitive processes. Additionally, Prolyl Endopeptidase Inhibitor 1 has demonstrated anti-amnesic effects, indicating its relevance in research on memory and cognitive disorders. -
Prolyl endopeptidase Inhibitor
Prolyl Endopeptidase Inhibitor 2 is a selective inhibitor of prolyl endopeptidase (PEP) with an IC50 value of 31.11 μM. This compound plays a crucial role in the modulation of proline-rich peptides and is relevant to research on neurodegenerative diseases. Its ability to inhibit PEP makes it a valuable tool for exploring therapeutic strategies in conditions where peptide degradation is implicated. -
PREP Inhibitor
Pramiracetam sulfate is a selective inhibitor of prolyl endopeptidase (PREP). It has been shown to enhance cognitive function, particularly following traumatic brain injury, making it a valuable tool in studying neurodegenerative diseases. This compound is suitable for research focused on the mechanisms of cognitive enhancement and potential therapeutic interventions for brain injuries and related disorders. -
POP Inhibitor
POP-IN-2 is a potent, covalent inhibitor of prolyl oligopeptidase (POP) with a Ki value of 6 nM. This reagent serves as a valuable tool for investigating the physiological roles of POP in neurodegenerative diseases and cancer, facilitating research into therapeutic strategies targeting these conditions. Its high specificity makes it suitable for detailed mechanistic studies in various biological contexts. -
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. -
uPA Inhibitor
UK122 TFA is a potent and selective inhibitor of urokinase-type plasminogen activator (uPA), exhibiting an IC50 of 0.2 μM. This compound demonstrates negligible inhibition of tissue-type plasminogen activator (tPA), plasmin, thrombin, and trypsin, with IC50 values exceeding 100 μM. As a 4-oxazolidinone analogue, UK122 TFA acts as an anticancer agent, effectively inhibiting cancer cell migration and invasion, making it a valuable tool in cancer research. -
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. -
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.
