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Ulinastatin (Uristatin) is a trypsin and serine proteaseinhibitor. Ulinastatin is the main protein binding inhibitor of various trypsin, chymotrypsin, and various pancreatic proteases. Ulinastatin shows neuroprotective, anti-inflammatory, anti-apoptotic, anti-oxidant effects .
Benzamidine (Benzenecarboximidamide) hydrochloride hydrate is a reversible competitive trypsin-like serine proteasesinhibitor with Kis of 20, 21, 97, 110, 320 and 750 μM against Tryptase, Trypsin, uPA, Factor Xa, Thrombin and tPA, respectively .
Urinary TrypsinInhibitor Fragment is a fragment derived from urinary trypsininhibitor by proteolysis. Urinary TrypsinInhibitor Fragment can inhibit tumor cell invasion by limited proteolysis .
Benzamidine is a reversible competitive trypsininhibitor with a Ki of 19 μM . Benzamidine shows inhibitory activity against homogeneous boar sperm acrosin with a Ki of 4 μM .
HG1 Toxin is a peptide found in the venom of the scorpion Heterometrus fulvipes, which has the activity of inhibitingpotassium channel Kv1.3. HG1 Toxin also has the activity of inhibitingtrypsin (Ki=107 nM) and can be used in the study of autoimmune diseases .
APC 366 hydrochloride is a selective inhibitor of mast cell trypsin activity. APC 366 hydrochloride is able to inhibittrypsin-induced histamine release in human tonsil and lung cells. APC 366 hydrochloride may have important applications in regulating allergic reactions and inflammation .
Tyropeptin A-4 (TP-101) is a potent proteasome inhibitor with the ability to inhibit mammalian 20S proteasome activity. Tyropeptin A-4 exerts its inhibitory effect by binding to the site responsible for trypsin-like activity. Tyropeptin A-4 derivative TP-104 has a 20-fold increase in inhibitory activity over Tyropeptin A. TP-110 specifically inhibitstrypsin-like activity without affecting PGPH and trypsin-like activity .
YD-3 is a platelet activation inhibitor. YD-3 inhibits Thrombine-induced rabbit platelets aggregation (IC50: 28.3 μM) and phosphoinositol production. In addition, YD-3 also inhibitsTrypsin-induced platelet aggregation in human and rabbit with the IC50 of 38.1 μM and 5.7 μM, respectively, but does not affect the proteolytic activity of trypsin .
Elasnin is a selective granulocyte elastaseinhibitor. Elasnin is almost ineffective for pancreatic elastase, trypsin, chymotrypsin, thermolysin and papain .
N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride (TLCK hydrochloride) is an irreversible inhibitor for serine protease, which inhibitstrypsin and trypsin-like protease by alkylating histidine residues in their active site. N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride inhibits caspase-3, caspase-6 and caspase-7, with IC50s of 12.0, 54.5 and 19.3 μM, respectively. N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride induces apoptosis in cell HL-60, and inhibits the decrease in mitochondrial transmembrane potential during apoptosis .
RWJ-58643 is a β-trypsininhibitor that suppresses allergic inflammation. RWJ-58643 (100 mg) significantly reduced nasal allergy symptoms, eosinophil infiltration, and IL-5 levels at low doses. RWJ-58643 resulted in late eosinophilia and elevated IL-5 levels at high doses (300 mg and 600 mg). RWJ-58643 modulates allergic responses by inhibiting the release of β-trypsin from mast cells .
APC-6860 is a trypsin-like serine proteasesinhibitor with ki values of 0.21 and 0.44 μM for uPA and trypsin, respectively. APC-6860 has a selectivity ratio for tPA versus uPA of 80. APC-6860 has ki values of 0.1 and 0.082 μM for human and murine urokinases, respectively. APC-6860 can be used for the research of cancer .
Camostat is an orally active trypsininhibitor. Camostat can reduce pancreatic fibrosis induced by repeated administration of superoxide dismutase inhibitors in rats, and decrease the proliferation and activation of pancreatic stellate cells (PSCs) .
HMB-Val-Ser-Leu-VE is a prototype vinyl esterinhibitor. HMB-Val-Ser-Leu-VE is against trypsin-like (T-L) proteasome activity with an IC50 of 0.033 μM .
Ro 09-1679 is a thrombininhibitor, with an IC50 of 33.6 μM. Ro 09-1679 inhibits the enzyme activities, with IC50 values of 3.3, 0.04 and 0.0346 μM for factor Xa, trypsin and papain, respectively .
Patamostat hydrochloride is a potent proteaseinhibitor. Patamostat hydrochloride potently inhibitstrypsin, plasmin and thrombin with IC50s of 39 nM, 950 nM and 1.9 μM, respectively. Patamostat hydrochloride may possess suppressing effects on pathogenesis and development of acute pancreatitis .
The Bowman-Birk inhibitor, a highly cross-linked protein featuring seven disulfide bridges, possesses spatially distinct domains specifically designed for the inhibition of both trypsin and chymotrypsin, showcasing its significant role as a plant protease inhibitor with anticarcinogenic properties.
Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine proteaseinhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase .
Demethylwedelolactone is a naturally occurring coumestan isolated from Eclipta alba. Demethylwedelolactone is a potent trypsininhibitor with an IC50 of 3.0 μM. Demethylwedelolactone suppresses cell motility and cell invasion of breast cancer cell .
BCX 1470 inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM), 3.4- and 200-fold better, respectively, than that of trypsin.
p-APMSF is an irreversible inhibitor of serinase. p-APMSF
has substrate specificity for positively charged side chains of amino acids,
lysine, or arginine. p-APMSF can be used to study the irreversible inhibition
of trypsin and thrombin .
4-Aminobenzamidine (p-Aminobenzamidine) dihydrochloride is a strong trypsininhibitor, also acting as a relatively weak urokinase type plasminogen activator (uPA) inhibitor (Ki=82 μM). 4-Aminobenzamidine can inhibit growth of a human prostate tumor in SCID mice .
Patamostat (E-3123) is a potent proteaseinhibitor. Patamostat potently inhibitstrypsin, plasmin and thrombin with IC50s of 39 nM, 950 nM and 1.9 μM, respectively. Patamostat may possess suppressing effects on pathogenesis and development of acute pancreatitis .
Patamostat (E-3123) mesylate is a potent proteaseinhibitor. Patamostat mesylate potently inhibitstrypsin, plasmin and thrombin with IC50s of 39 nM, 950 nM and 1.9 μM, respectively. Patamostat mesylate may possess suppressing effects on pathogenesis and development of acute pancreatitis .
BCX 1470 methanesulfonate inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM), 3.4- and 200-fold better, respectively, than that of trypsin.
VR23 is a small molecule that potently inhibits the activities of trypsin-like proteasomes (IC50=1 nM), chymotrypsin-like proteasomes (IC50=50-100 nM), and caspase-like proteasomes (IC50=3 μM).
BMS-199945 is a influenza virus fusioninhibitor with the IC50 values of 0.57 μM and approximately 1 μM aganist influenza A/WSN/33 virus-induced hemolysis of chicken RBC and in the trypsin protection assay, respectively .
Lipstatin is a pancreatic lipase inhibitor (IC50=0.14 μM), whose structure is closely related to the known inhibitor, Esterastin. Lipstatin inhibits the absorption of triglycerides without affecting the absorption of oleic acid. Lipstatin has no inhibitory effects on other pancreatic enzymes, such as phospholipase A2 and trypsin (<200 μM) .
Darexaban (YM150) is a potent, selective and orally active factor Xa (FXa)inhibitor with an IC50 of 54.6 nM. Darexaban shows high selectivity against other related serine proteases, such as trypsin, thrombin, and kallikrein. Darexaban has anticoagulant and antithrombotic effects .
Camostat (mesylate) (Standard) is the analytical standard of Camostat (mesylate). This product is intended for research and analytical applications. Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine proteaseinhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase .
HA-IN-1 (compound 5g) is a Hemagglutinin (HA) ligand with high affinity, targeting to the trypsin cleavage site of HA. HA-IN-1 inhibits HA-mediated membrane fusion and reduces the pulmonary virus titer in vivo. HA-IN-1 is a potential influenza A virus (IAV) inhibitor, and an anti-influenza agent .
ONO-3307 is a proteaseinhibitor that competitively inhibits a variety of proteases including trypsin, thrombin, plasma kallikrein, plasmin, pancreatic kallikrein, and chymotrypsin. ONO-3307 alleviates endotoxin-induced experimental disseminated intravascular coagulation (DIC) in rats. ONO-3307 can be used in the study of thrombosis and protease-mediated diseases .
Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasomeinhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC50=3.5, 28, and 430 nM, respectively) .
UK122 is a potent and selective urokinase-type plasminogen activator (uPA)inhibitor with an IC50 of 0.2 μM. UK122 shows no or little inhibition of tissue-type PA (tPA), plasmin, thrombin, and trypsin (all IC50>100 μM). UK122, 4-oxazolidinone analogue, is an anticancer agent and inhibits cancer cell migration and invasion .
23-O-β-D-Glucopyranosyl-20-isoveratramine is a potential anti-allergic agent extracted from nettles. A variety of COX-1, COX-2, 5-lipoxygenase and trypsin-like inhibitors and H1 antagonists are found in nettle extract, which can inhibit seasonal allergies, allergic rhinitis and other inflammatory diseases. and preventive effects .
Freselestat (ONO-6818) is a potent and orally active neutrophil elastaseinhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity .
Calmodulin antagonist-1 (A-5) is a calmodulin (CaM) antagonist. Calmodulin antagonist-1 inhibits calmodulin-activated Ca 2+-phosphodiesterase (PDE) (IC50=66 μM). Calmodulin antagonist-1 also inhibitstrypsin-treated Ca 2+-PDE (IC50=560 μM) in a competitive fashion with respect to cyclic GMP .
Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease .
Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastaseinhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity .
FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibitsmouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect .
SPSB2-iNOS inhibitory cyclic peptide-1 is an inhibitor for the interaction of SPRY domain and SOCS-box protein 2 (SPSB2) and iNOS, through binding SPSB2 on iNOS site with KD of 4.4 nM. SPSB2-iNOS inhibitory cyclic peptide-1 is resistant to the proteases pepsin, trypsin and α-chymotrypsin. SPSB2-iNOS inhibitory cyclic peptide-1 is stable in human plasma and in oxidative environment .
Milvexian TFA (BMS-986177 TFA) is a factor XIa inhibitor with biological activity to prevent venous thromboembolism. Milvexian TFA was effective in reducing the occurrence of venous thromboembolism in patients undergoing knee replacement surgery. Milvexian TFA has good selectivity and shows significant inhibitory effects on plasma kallikrein and trypsin. Milvexian TFA has a bioavailability of 32%, which means it has a high absorption rate in the body. Milvexian TFA showed a relatively low risk of bleeding in clinical trials .
Gabexate mesylate (FOY) is is a competitive and non-antigenic synthetic inhibitor of trypsin-like serine proteinases. Gabexate mesylate inhibits human thrombin, urokinase, plasmin, and Factor Xa with Kis of 0.97, 1.3, 1.6, and 8.5 μM, respectively. Gabexate mesylate binds to human and bovine tryptase with Kis of 3.4 nM and 18 μM, respectively. Gabexate mesylate exerts an anticoagulant effect on the clotting activity of thrombin and has anti-inflammatory effect by viainhibition of NF-κB, proinflammatory cytokines, and nitric oxide. Gabexate mesylate is used for pancreatitis and disseminated intravascular coagulation .
Gabexate (mesylate) (Standard) is the analytical standard of Gabexate (mesylate). This product is intended for research and analytical applications. Gabexate mesylate (FOY) is is a competitive and non-antigenic synthetic inhibitor of trypsin-like serine proteinases. Gabexate mesylate inhibits human thrombin, urokinase, plasmin, and Factor Xa with Kis of 0.97, 1.3, 1.6, and 8.5 μM, respectively. Gabexate mesylate binds to human and bovine tryptase with Kis of 3.4 nM and 18 μM, respectively. Gabexate mesylate exerts an anticoagulant effect on the clotting activity of thrombin and has anti-inflammatory effect by viainhibition of NF-κB, proinflammatory cytokines, and nitric oxide. Gabexate mesylate is used for pancreatitis and disseminated intravascular coagulation .
Benzamidine (Benzenecarboximidamide) hydrochloride hydrate is a reversible competitive trypsin-like serine proteasesinhibitor with Kis of 20, 21, 97, 110, 320 and 750 μM against Tryptase, Trypsin, uPA, Factor Xa, Thrombin and tPA, respectively .
Pyr-Arg-Thr-Lys-Arg-AMC TFA is a AMC peptide. AMC is a decapeptide that is specifically hydrolyzed by proteases such as trypsin and thrombin. The AMC peptide can be used to determine the activity of protease and the potency of enzyme inhibitors .
Urinary TrypsinInhibitor Fragment is a fragment derived from urinary trypsininhibitor by proteolysis. Urinary TrypsinInhibitor Fragment can inhibit tumor cell invasion by limited proteolysis .
HG1 Toxin is a peptide found in the venom of the scorpion Heterometrus fulvipes, which has the activity of inhibitingpotassium channel Kv1.3. HG1 Toxin also has the activity of inhibitingtrypsin (Ki=107 nM) and can be used in the study of autoimmune diseases .
HMB-Val-Ser-Leu-VE is a prototype vinyl esterinhibitor. HMB-Val-Ser-Leu-VE is against trypsin-like (T-L) proteasome activity with an IC50 of 0.033 μM .
Pyr-Arg-Thr-Lys-Arg-AMC is a AMC peptide. AMC is a decapeptide that is specifically hydrolyzed by proteases such as trypsin and thrombin. The AMC peptide can be used to determine the activity of protease and the potency of enzyme inhibitors .
SPSB2-iNOS inhibitory cyclic peptide-1 is an inhibitor for the interaction of SPRY domain and SOCS-box protein 2 (SPSB2) and iNOS, through binding SPSB2 on iNOS site with KD of 4.4 nM. SPSB2-iNOS inhibitory cyclic peptide-1 is resistant to the proteases pepsin, trypsin and α-chymotrypsin. SPSB2-iNOS inhibitory cyclic peptide-1 is stable in human plasma and in oxidative environment .
SPSB2-iNOS inhibitory cyclic peptide-1 TFA is the TFA salt form of SPSB2-iNOS inhibitory cyclic peptide-1(HY-P10383). SPSB2-iNOS inhibitory cyclic peptide-1 is an inhibitor for the interaction of SPRY domain and SOCS-box protein 2 (SPSB2) and iNOS, through binding SPSB2 on iNOS site with KD of 4.4 nM. SPSB2-iNOS inhibitory cyclic peptide-1 is resistant to the proteases pepsin, trypsin and α-chymotrypsin. SPSB2-iNOS inhibitory cyclic peptide-1 is stable in human plasma and in oxidative environment .
Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine proteaseinhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase .
Demethylwedelolactone is a naturally occurring coumestan isolated from Eclipta alba. Demethylwedelolactone is a potent trypsininhibitor with an IC50 of 3.0 μM. Demethylwedelolactone suppresses cell motility and cell invasion of breast cancer cell .
Lipstatin is a pancreatic lipase inhibitor (IC50=0.14 μM), whose structure is closely related to the known inhibitor, Esterastin. Lipstatin inhibits the absorption of triglycerides without affecting the absorption of oleic acid. Lipstatin has no inhibitory effects on other pancreatic enzymes, such as phospholipase A2 and trypsin (<200 μM) .
Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasomeinhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC50=3.5, 28, and 430 nM, respectively) .
Camostat (mesylate) (Standard) is the analytical standard of Camostat (mesylate). This product is intended for research and analytical applications. Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine proteaseinhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase .
23-O-β-D-Glucopyranosyl-20-isoveratramine is a potential anti-allergic agent extracted from nettles. A variety of COX-1, COX-2, 5-lipoxygenase and trypsin-like inhibitors and H1 antagonists are found in nettle extract, which can inhibit seasonal allergies, allergic rhinitis and other inflammatory diseases. and preventive effects .
The SPINK1 protein is a serine protease inhibitor that significantly inhibits trypsin, especially in the pancreas, preventing premature activation of the zymogen. This critical role maintains the integrity of pancreatic cellular processes. SPINK1 Protein, Human (HEK293, His) is the recombinant human-derived SPINK1 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of SPINK1 Protein, Human (HEK293, His) is 56 a.a., with molecular weight of 12-16 kDa.
SPINK1 is a serine protease inhibitor that significantly inhibits trypsin, especially in the pancreas, preventing premature activation of the zymogen. In the male reproductive tract, SPINK1 binds to sperm heads and regulates sperm volume by inhibiting calcium absorption and nitrogen oxide (NO) production. SPINK1 Protein, Mouse (P.pastoris, His) is the recombinant mouse-derived SPINK1 protein, expressed by P. pastoris , with N-6*His labeled tag. The total length of SPINK1 Protein, Mouse (P.pastoris, His) is 57 a.a., with molecular weight of 10 kDa.
SPINK2, a robust acrosin inhibitor, is vital for normal spermiogenesis, preventing premature activation of proacrosin and other proteases to avoid spermiogenesis defects. It likely regulates germ cell apoptosis mediated by serine proteases and displays inhibitory activity against trypsin, indicating involvement in diverse serine protease-dependent processes. SPINK2 Protein, Human (HEK293, Fc) is the recombinant human-derived SPINK2 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of SPINK2 Protein, Human (HEK293, Fc) is 61 a.a., with molecular weight of ~33.6-38 kDa.
The ITIH3 protein has a dual role: as a carrier of hyaluronic acid in serum and as a binding protein that facilitates interactions with various matrix proteins. These interactions regulate the localization, synthesis, and degradation of hyaluronic acid, which is critical for multiple cellular activities. ITIH3 Protein, Human (HEK293, His) is the recombinant human-derived ITIH3 protein, expressed by HEK293 , with C-6*His labeled tag.
The ITIH5 protein was identified as a potential tumor suppressor, indicating its critical role in controlling tumorigenesis. As a tumor suppressor, ITIH5 is expected to counteract uncontrolled cell growth and inhibit or regulate key pathways in tumor development. ITIH5 Protein, Human (His-SUMO) is the recombinant human-derived ITIH5 protein, expressed by E. coli , with N-SUMO, N-6*His labeled tag.
DBI, a versatile protein, binds medium- and long-chain acyl-CoA esters, indicating a potential intracellular carrier role. It also displaces diazepam from the benzodiazepine recognition site on the GABA type A receptor. This dual functionality suggests DBI may act as a neuropeptide, modulating GABA receptor activity. Remarkably, DBI functions as a monomer in these interactions. DBI Protein, Human (103a.a, His) is the recombinant human-derived DBI protein, expressed by E. coli , with N-6*His labeled tag. The total length of DBI Protein, Human (103a.a, His) is 103 a.a., with molecular weight of ~14 kDa.
Trypsin inhibitor DE-3 Protein, Erythrina caffra (P. pastoris, His) is the recombinant Trypsin inhibitor DE-3, expressed by P. pastoris , with N-6*His labeled tag. ,
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