Proteases

Items 951-1000 of 1361

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  1. DHODH Inhibitor

    DHODH-IN-34 is a selective inhibitor of human dihydroorotate dehydrogenase (DHODH), exhibiting an IC50 value of 13 nM. This compound is particularly valuable for researching RNA viruses, including measles virus and chikungunya virus, due to its ability to disrupt nucleotide synthesis pathways critical for viral replication. Researchers can leverage DHODH-IN-34 to investigate therapeutic strategies against these viral infections.
  2. Aminopeptidase P2 Inhibitor

    ST-115 is a potent inhibitor of aminopeptidase P2, a target involved in the regulation of various physiological processes. Its high specificity makes it an invaluable tool for studying the role of aminopeptidase P2 in ischemic stroke and related conditions. Researchers may utilize ST-115 to explore its potential therapeutic implications in neuroprotection and recovery following cerebral ischemia.
  3. Aminopeptidase A Inhibitor

    Firibastat is a potent inhibitor of aminopeptidase A (APA), exhibiting a Ki value of 200 nM. This first-in-class compound effectively inhibits the conversion of brain angiotensin-II to angiotensin-III, resulting in reduced blood pressure in hypertensive models. Firibastat is particularly valuable in exploring the role of APA in neurophysiological processes and hypertension research.
  4. Aminopeptidase Inhibitor

    L-Leucinol is a competitive inhibitor of aminopeptidase, exhibiting a Ki value of 17 μM. This reagent is primarily utilized in in vitro enzymatic assays to study enzymatic activity and inhibition. Additionally, L-Leucinol serves as a valuable tool in peptide synthesis applications, facilitating the exploration of peptide structure and function in biochemical research.
  5. Aminopeptidase/Epoxide Hydrolase Inhibitor

    ARM1 (4BSA) is a potent inhibitor of aminopeptidase and epoxide hydrolase. It exhibits aminopeptidase inhibitory activity with an IC50 of 7.61 µM and demonstrates epoxide hydrolase inhibitory activity with an IC50 of 12.4 µM. This compound is valuable for research applications targeting metabolic pathways involving peptide and epoxide metabolism.
  6. Anti-inflammatory Agent, Aminopeptidase Inhibitor

    2-(2'-Pyridyl)benzimidazole is an effective anti-inflammatory agent and a potent inhibitor of methionine aminopeptidase in Escherichia coli. This compound exhibits tridentate ligand properties, capable of forming stable complexes with various transition metal ions. Its applications extend to biochemical research focused on inflammatory processes and amino acid metabolism, making it a valuable reagent for studies in these areas.
  7. Leucine Aminopeptidase Inhibitor

    Adamantanine is a potent inhibitor of leucine aminopeptidase, demonstrating an I/S0.5 value of 10.5. It effectively impairs the transport of methionine and leucine in Ehrlich ascites carcinoma cells, with a Ki value of 0.76 mM. Additionally, Adamantanine displays inhibitory effects on the proliferation of P388 lymphocytic leukemia cells, exhibiting an IC50 of greater than 1 mM. This compound serves as a valuable tool for researchers investigating amino acid transport and cancer cell proliferation.
  8. Neutral Endopeptidase Inhibitor, Aminopeptidase N Inhibitor

    RB 101 is a mixed inhibitor of neutral endopeptidase and aminopeptidase N, enzymes that metabolize enkephalins. This compound exhibits long-lasting antinociceptive effects and inhibits in vivo [3H]DPN binding in mice under both basal conditions and after swim stress. RB 101 is particularly useful for studying the in vivo localization of enkephalinergic pathways activated by various stimuli, making it a valuable tool for pain research and neuropharmacology.
  9. D-aminopeptidase Substrate

    H-D-Ala-D-Ala-D-Ala-D-Ala-OH is a substrate for D-aminopeptidase, an enzyme that catalyzes the cleavage of D-amino acids from peptide chains. This compound is primarily utilized in biochemical studies to investigate D-aminopeptidase activity and its role in various physiological processes. It serves as a valuable tool for researchers studying peptide metabolism and the implications of D-amino acids in biological systems.
  10. Aminopeptidase B Inhibitor

    Arphamenine A is a potent inhibitor of aminopeptidase B, derived from Chromobacterium violaceum HMG361-CF4. This compound has demonstrated the ability to inhibit aminopeptidase B activity, contributing to its potential anticancer effects. Research indicates that Arphamenine A may suppress the growth of sarcoma 180 and invasive micropapillary carcinoma (IMC), making it a valuable tool for studying cancer biology and therapeutic strategies targeting aminopeptidase B.
  11. Aminopeptidase N Inhibitor

    Aminopeptidase N Inhibitor 1 is a potent inhibitor targeting aminopeptidase N, demonstrating an IC50 of 25 μM. It plays a significant role in research related to tumor angiogenesis, providing valuable insights into the mechanisms of cancer progression and the development of therapeutic strategies. Its application in studies of angiogenesis makes it a crucial tool for researchers investigating tumor microenvironment interactions.
  12. Aminopeptidase

    Aeromonas proteolytica aminopeptidase is an enzyme that acts as an aminopeptidase, catalyzing the hydrolysis of peptide bonds at the N-terminal of substrates. Additionally, this enzyme exhibits esterase activity, demonstrating the ability to hydrolyze L-leucine ethyl ester (L-Leu-OEt) with a Km value of 700 µM. Its role in protein processing and peptide metabolism makes it a valuable tool for biochemical research and enzymatic studies.
  13. Aminopeptidase N Inhibitor

    Probestin is a potent inhibitor of aminopeptidase N (APN), derived from the bacterium Streptomyces cyanogens MH663-2F6. This compound exhibits significant biological activity by selectively blocking APN activity, leading to the modulation of various physiological processes. Probestin is valuable for research applications focused on studying the role of APN in cancer, inflammation, and immune response pathways.
  14. Aminopeptidase-M Inhibitor

    Leuhistin is an aminopeptidase-M (AP-M) inhibitor, targeting the enzymatic degradation of bioactive peptides within cerebral membranes. By inhibiting AP-M, Leuhistin enhances the availability and activity of these peptides, making it a valuable reagent for studies focused on neurobiology and peptide research. It is derived from Bacillus laterosporus BMI156-14F1, highlighting its natural origins in biochemical applications.
  15. Aminopeptidase/Valine arylamidase Substrate

    H-Val-βNA (L-Valine β-naphthylamide) is a substrate for aminopeptidases and valine arylamidases. It is utilized in biochemical assays to study enzyme activity and substrate specificity. The reaction of H-Val-βNA with these enzymes generates a measurable product, facilitating the investigation of enzymatic processes related to amino acid metabolism and protein turnover.
  16. Dipeptidylaminopeptidase Substrate

    Lysine-2-naphthylamide is a substrate for dipeptidylaminopeptidase (DAP) enzymes. Its primary mechanism involves the cleavage of peptide bonds, facilitating the release of naphthylamide. This compound is useful in biochemical assays for studying DAP activity and can be employed in various research applications, including peptide hydrolysis and enzyme kinetics studies.
  17. Aminopeptidase Inhibitor

    Matlystatin A is a potent inhibitor of aminopeptidases, exhibiting IC50 values of 0.3 μM and 0.56 μM against 92 kDa and 72 kDa type IV collagenases, respectively. This compound is valuable for investigating proteolytic processes in cancer research. Its ability to modulate enzymatic activity provides insights into tumor progression and metastasis mechanisms.
  18. Aminopeptidase Inhibitor

    Ketomethylenebestatin is a selective inhibitor of aminopeptidases, showcasing notable activity against AP-B, AP-M, and Leu-AP with IC50 values of 56 μM, 752 μM, and 0.39 μM, respectively. This compound serves as an analog of the natural aminopeptidase inhibitor Bestatin, and is valuable in research applications focused on the regulation of peptide metabolism and potential therapeutic targets in various diseases. Its specificity towards aminopeptidases makes it a useful tool for investigating enzymatic pathways and the role of these enzymes in physiological processes.
  19. Aminopeptidase Inhibitor

    Lys-psi(CH2NH)-Trp(Nps)-OMe is a pseudodipeptide analog of lysine and tryptophan designed to inhibit aminopeptidase activity. This compound exhibits significant analgesic properties, demonstrated through dose-dependent and naloxone-reversible responses following intracerebroventricular administration in murine models. It not only prolongs analgesic effects compared to its parent compound but also offers protection against the degradation of methionine enkephalin in rat striatal slices. Lys-psi(CH2NH)-Trp(Nps)-OMe's enhanced resistance to proteolysis contributes to its sustained analgesic activity, making it a valuable tool for studying pain mechanisms and the role of aminopeptidases in neuromodulation.
  20. μ-Calpain Inhibitor

    Calpain Inhibitor-2 is a peptide inhibitor targeting μ-calpain, with a Ki value of 9 nM. This compound demonstrates significant antiproliferative activity against melanoma cell lines, specifically A-375 and B-16F1, as well as PC-3 prostate cancer cells in vitro. It is a valuable tool for research applications focused on exploring calpain-mediated pathways in cancer biology.
  21. Glutamine Synthetase Inhibitor; Convulsant

    L-Methionine-DL-sulfoximine is a highly specific and irreversible inhibitor of glutamine synthetase, which significantly affects astroglial metabolism and morphology. This compound also demonstrates potent convulsant properties. L-Methionine-DL-sulfoximine has been utilized in research to inhibit glutamine-dependent neuronal toxicity in vitro and to study the mechanisms underlying convulsive seizures. Additionally, it enhances the rate of fixed nitrogen release in cyanobacteria, making it a valuable tool for applications in biofertilizer research.
  22. Glutamine Antagonist

    Duazomycin is a glutamine antagonist that plays a critical role in modulating metabolic pathways. This compound significantly enhances the efficacy of 6-Mercaptopurine in experimental allergic encephalomyelitis models, demonstrating improved therapeutic outcomes without elevating toxicity. Duazomycin is valuable for research applications focusing on metabolic interactions and therapeutic strategies in autoimmune diseases.
  23. Glutamine Antagonist

    Duazomycin sodium is a potent glutamine antagonist that enhances the efficacy of 6-Mercaptopurine in models of experimental allergic encephalomyelitis (EAE). By targeting glutamine metabolism, it demonstrates potential to improve therapeutic outcomes while maintaining a favorable toxicity profile. This compound is valuable for research applications focused on neuroinflammatory disorders and the modulation of immune responses.
  24. Tyrosinase Inhibitor

    Cepharadione B is a natural tyrosinase inhibitor derived from the leaves of Piper sanctum, exhibiting an IC50 value of 170 μM. This compound demonstrates significant inhibitory effects on cell growth in various cancer cell lines, including A-549, SK-OV-3, SK-MEL-2, XF-498, and HCT-15. Cepharadione B is valuable for research exploring pigmentation processes, melanoma, and potential therapeutic interventions against cancer.
  25. Thrombin/ Factor Xa Inhibitor

    Ciraparantag is a potent inhibitor of thrombin and factor Xa, serving as a broad-spectrum reversal agent for various anticoagulants. This compound effectively neutralizes the effects of low-molecular-weight heparin, unfractionated heparin, and certain direct oral anticoagulants, while sparing vitamin K antagonists and argatroban. Its unique mechanism makes Ciraparantag a valuable tool for research focused on anticoagulation reversal and hemostasis.
  26. Thrombin/Factor Xa Inhibitor

    Ciraparantag acetate is a potent inhibitor of thrombin and factor Xa, serving as a broad-spectrum reversal agent for various anticoagulants, including low molecular weight heparins, unfractionated heparins, and certain direct oral anticoagulants, excluding vitamin K antagonists (VKAs). Its primary mechanism targets the coagulation pathway, facilitating the restoration of normal hemostasis in clinical situations where anticoagulation reversal is necessary. Ciraparantag acetate is valuable in research applications focused on anticoagulation management and hemostatic balance in cardiovascular studies.
  27. Thrombin Inhibitor

    Edoxaban impurity 4 is a structural impurity related to Edoxaban, a selective and potent thrombin inhibitor. It demonstrates significant biological activity and is primarily utilized in research applications focusing on anticoagulation strategies. Edoxaban itself serves as an effective anticoagulant, with its mechanistic role in inhibiting factor Xa contributing to therapeutic approaches for stroke prevention and other thromboembolic disorders.
  28. Thrombin/Factor Xa Inhibitor

    Ciraparantag TFA is a potent thrombin and factor Xa inhibitor utilized as a broad-spectrum reversal agent for anticoagulants. It effectively antagonizes the effects of various anticoagulants, including low-molecular-weight heparin, unfractionated heparin, and specific direct oral anticoagulants, while sparing vitamin K antagonists and argatroban. This compound is significant for research applications focused on enhancing hemostatic management in patients receiving anticoagulant therapy.
  29. Thrombin/Factor Xa/Trypsin/Papain Inhibitor

    Bacithrocin D is a potent inhibitor of key proteases, specifically targeting thrombin, factor Xa, trypsin, and papain. It effectively prolongs clotting time, making it valuable in studies related to coagulation and hemostasis. Bacithrocin D demonstrates IC50 values of 124 μM for thrombin, 9 μM for factor Xa, 0.85 μM for trypsin, and a remarkable 0.01 μM for papain, showcasing its high potency against these proteases. This reagent is useful for investigating protease-related pathways and developing therapeutic strategies in anticoagulation research.
  30. Thrombin Inhibitor

    Bacithrocin A is a potent thrombin inhibitor that also targets factor Xa, trypsin, and papain, demonstrating IC50 values of 48 μM, 13 μM, 0.65 μM, and 0.02 μM, respectively. This compound is of particular interest in the study of coagulation processes and the development of anticoagulant therapies. Its broad-spectrum inhibitory activity makes it a valuable reagent for biological research focused on protease activity modulation and hemostasis.
  31. Thrombin Inhibitor

    Bacithrocin C is a potent thrombin inhibitor that effectively targets thrombin, factor Xa, trypsin, and papain, exhibiting IC50 values of 80 μM, 15 μM, 1.3 μM, and 0.02 μM, respectively. This compound demonstrates significant inhibitory activity, making it a valuable tool for research in coagulation pathways and protease-related studies. It is suitable for applications focused on understanding thrombotic processes and developing antithrombotic strategies.
  32. Thrombin Inhibitor

    Bacithrocin B is a potent thrombin inhibitor that also targets factor Xa, trypsin, and papain. It exhibits inhibitory activity with IC50 values of 84 μM for thrombin, 17 μM for factor Xa, 1.7 μM for trypsin, and 0.02 μM for papain. This compound is valuable for research applications aiming to study coagulation processes and enzyme dynamics in various biological systems.
  33. Microsomal Aminopeptidase

    Microsomal Aminopeptidase, Microorganism is an enzyme known to target the microsomal aminopeptidase activity. This enzyme plays a crucial role in protein degradation and peptide processing, making it valuable for research in immunology and vaccine development. Its application in the study of parasitic nematodes facilitates advances in molecular vaccines, aiding in the fight against these pathogens.
  34. Gamma-Secretase Modulator

    γ-Secretase modulator 13 is a gamma-secretase modulator that inhibits the production of the aggregated amyloid β-peptide Aβ42, exhibiting an IC50 value of 163 nM. This compound is valuable for research in Alzheimer's disease, facilitating investigations into amyloidogenic processes and potential therapeutic interventions. Its specific modulation of γ-secretase activity positions it as a significant tool for studying the mechanisms underlying neurodegenerative disorders.
  35. Serine Protease

    Proteinase K is a nonspecific serine protease that effectively digests a wide variety of proteins. It exhibits robust activity in the presence of SDS or urea and functions across a broad pH range (4-12), temperature, and ionic conditions. This enzyme is commonly utilized in the extraction and detection of viral nucleic acids, making it a valuable tool in molecular biology and diagnostic applications.
  36. 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.
  37. Plasminogen Activator

    Alteplase is a recombinant tissue plasminogen activator that acts primarily as a thrombolytic agent by converting plasminogen to plasmin, which leads to fibrinolysis. This compound is crucial in the management of acute ischemic stroke, pulmonary embolism, and acute myocardial infarction. Alteplase is also utilized for the treatment of occluded catheters, facilitating the restoration of vascular patency in clinical settings.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. Serine Protease

    Recombinant enterokinase (rEK) is a serine protease that functions as the physiological activator of trypsinogen, converting it into its active form, trypsin. This enzyme is essential for various biochemical assays and applications involving protein digestion and processing. Recombinant enterokinase is widely used in research focused on proteolytic processes, enzyme activation, and protein purification techniques.
  43. ASS1 Enzyme ctivators

    LM2I is an argininosuccinate synthase (ASS1) enzyme activator derived from Spinosyn A. This compound demonstrates significant antiproliferative activity against various colorectal cancer cell lines and xenograft tumors. LM2I effectively inhibits colorectal cancer cell growth through the EGFR signaling pathway, making it a valuable tool for research in cancer biology and therapeutic development targeting ASS1.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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