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TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is an effective serineproteaseinhibitor and also a blocker of the PDK1/Akt pathway. TPCK can modify the E7 protein in actively keratinocyte cells. TPCK can induce cellular apoptosis, suppress tumor growth, reduce hypoxic-ischemic brain injury in rat pups, and affect vascular permeability in inflamed rats .
Dansyl-Glu-Gly-Arg-Chloromethylketone TFA is a proteaseinhibitor, and inhibitsserine/threonine proteases. Dansyl-Glu-Gly-Arg-Chloromethylketone TFA inhibits activated porcine factor IX .
Leupeptin hemisulfate is a broad-spectrum, membrane-permeable proteaseinhibitor. Leupeptin hemisulfate potently inhibitsserine,cysteine and threonine proteases. Leupeptin hemisulfate inhibitsM pro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity .
3,4-Dichloroisocoumarin is a potent serine-protease and SrLipinhibitor (Ki for SrLip: 26.6 μM). 3,4-Dichloroisocoumarin is opened by serineproteases and then undergoes acylation with the enzyme, thereby inhibitingprotease activity. 3,4-Dichloroisocoumarin can induce DNA fragmentation and Apoptosis. 3,4-Dichloroisocoumarin can be used in the research of multiple fields such as tumors, cardiovascular disease and enzyme catalytic mechanisms .
Dansyl-Glu-Gly-Arg-Chloromethylketone is a proteaseinhibitor, and inhibitsserine/threonine proteases. Dansyl-Glu-Gly-Arg-Chloromethylketone inhibits activated porcine factor IX .
Leupeptin is a broad-spectrum, membrane-permeable proteaseinhibitor. Leupeptin potently inhibitsserine,cysteine and threonine proteases. Leupeptin inhibitsM pro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity .
Ulinastatin (Uristatin) is a trypsin and serineproteaseinhibitor. 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 .
Cyclothiazomycin selectively inhibits renin activity and does not inhibit pepsin, aspartic acid, serine, mercaptan protease and metalloproteinases. Cyclothiazomycin has weak antifungal activity .
Upamostat (WX-671) is a serineproteaseinhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.
Dihydrofuran-3(2H)-one (3-Oxotetrahydrofuran) is a cyclic ketone that can be used to synthesize cyclic ketone inhibitors that inhibit the serineprotease plasmin .
Leupeptin (hemisulfate) (Standard) is the analytical standard of Leupeptin (hemisulfate). This product is intended for research and analytical applications. Leupeptin hemisulfate is a broad-spectrum, membrane-permeable proteaseinhibitor. Leupeptin hemisulfate potently inhibitsserine, cysteine and threonine proteases. Leupeptin hemisulfate inhibits Mpro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity[1][2][3].
Rivulariapeptolides 1155 is a potent serineproteaseinhibitor with IC50s of 41.84, 4.94, 56.54 nM for chymotrypsin, elastase, prpteinase K, respectively .
Activated Protein C (390-404), human is a peptide of the activated protein C (a vitamin K-dependent serineprotease), potently inhibits APC anticoagulant activity .
BI-1230 is potent and digit nanomolar inhibitor of HCV NS3 protease and of viral replication. BI-1230 is also highly selective against other serine/cysteine proteases. BI-1230 shows good Pharmacokinetic(PK) activity .
Rivulariapeptolides 988 is a high potent and selective serineproteaseinhibitor with IC50 values of 95.46 nM, 15.29 nM and 85.50 nM for chymotrypsin, elastase and proteinase K, respectively .
Rivulariapeptolides 1121 is a high potent and selective serineproteaseinhibitor with IC50 values of 35.52 nM, 13.24 nM and 48.05 nM for chymotrypsin, elastase and proteinase K, respectively .
Rivulariapeptolides 1185 is a high potent and selective serineproteaseinhibitor with IC50 values of 13.17 nM, 23.59 nM and 55.26 nM for chymotrypsin, elastase and proteinase K, respectively .
Activated Protein C (390-404), human TFA, a peptide of the activated protein C (a vitamin K-dependent serineprotease), potently inhibits APC anticoagulant activity .
Narlaprevir (SCH 900518) is a selective and orally bioavailable NS3 proteaseinhibitor with a Ki value of 6 nM and an EC90 value of 40 nM . Narlaprevir also inhibits the HCV nonstructural protein 3 serineprotease . Narlaprevir is also a SARS-CoV 3CL proinhibitor with an IC50 of 2.3 μM .
VD2173 is a side chain cyclized macrocyclic peptide inhibitor of HGF-activating serineproteases. VD2173 potently inhibitsmatriptase and hepsin. VD2173 can be used for the research of lung cancer .
Kynapcin-13 can non-competitively inhibit the activity of prolyl endopeptidase (PEP) with an IC50 of 76.80 μM. Kynapcin-13 has a little inhibitory effect on other serineproteases .
Kynapcin-28 can non-competitively inhibit the activity of prolyl endopeptidase (PEP) with an IC50 of 76.80 μM. Kynapcin-28 has a little inhibitory effect on other serineproteases .
HTRA1-IN-1 (Compound 17) is a selective inhibitor for serineprotease high temperature requirement A serine peptidase 1 (HTRA1), with IC50 of 13 nM. HTRA1-IN-1 is potential for ameliorating HTRA1-related diseases, such as age-related macular degeneration (AMD), osteoarthritis, and rheumatoid arthritis .
Narlaprevir (Standard) is the analytical standard of Narlaprevir. This product is intended for research and analytical applications. Narlaprevir (SCH 900518) is a selective and orally bioavailable NS3 proteaseinhibitor with a Ki value of 6 nM and an EC90 value of 40 nM . Narlaprevir also inhibits the HCV nonstructural protein 3 serineprotease . Narlaprevir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.3 μM .
Benzamidine (Benzenecarboximidamide) hydrochloride hydrate is a reversible competitive trypsin-like serineproteasesinhibitor with Kis of 20, 21, 97, 110, 320 and 750 μM against Tryptase, Trypsin, uPA, Factor Xa, Thrombin and tPA, respectively .
Camostat mesylate (Camostat mesilate) is an orally active, synthetic serineproteaseinhibitor 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 .
Alpha 1 Antichymotrypsin, Human Plasma is a serineproteaseinhibitor. Alpha 1 Antichymotrypsin, Human Plasma appears in the amyloid lesions of Alzheimer's disease. Alpha 1 Antichymotrypsin, Human Plasma can be used in Alzheimer's disease research .
MM3122 is a selective type II transmembrane serineprotease (TMPRSS2) inhibitor with an IC50 value of 0.34 nM. MM3122 effectively blocks TMPRSS2, thereby inhibiting the entry of SARS-CoV-2 and MERS-CoV into human cells .
ONO-3403 is an orally active serineproteaseinhibitor. ONO-3403 inhibits the production of TNF-α and nitric oxide induced by LPS. ONO-3403 inhibits the cell growth and induces the apoptosis, and has an antitumor effect on malignant tumors .
SP-Chymostatin B (α-MAPI) is a strong inhibitor of many proteases, including chymotrypsin, papain, chymotrypsin-like serine proteinases, chymases, and lysosomal cysteine proteinases such as cathepsins A,B,C, H, and L. SP-Chymostatin B weakly inhibits human leucocyte elastase .
DEC-RVRK-CMK (Decanoyl-Arg-Val-Arg-Lys-chloromethylketone) is a peptide-based CMK (chloromethylketone) inhibitor that targets and inactivates the secreted soluble kexin (Kex2) (Ki=8.45 μM). The yeast enzyme Kex2 (kexin, EC 3.4.21.61) is a calcium-dependent transmembrane protease and belongs to the mammalian protease family of the serineprotease subtilisin family. The binding mechanism of Kex2 with different CMK inhibitors depends on substrate selectivity, particularly the selective differences between lysine and arginine at the P1 position .
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 .
TMPRSS6-IN-1 (TFA) is a potent inhibitor of TMPRSS6 (Matriptase-2), belonging to TTSPs (transmembrane serineprotease). TMPRSS6, is a type II TTSP, the genetic reduction of which will improve symptoms of hemochromatosis and beta thalassemia in mice .
Zifaxaban is an orally active, competitively and selective Factor Xa (FXa)inhibitor with an IC50 of 11.1 nM for human FXa. Zifaxaban shows >10000-fold greater selectivity than other serineproteases. Zifaxaban can be used for the arterial and venous thrombosis research .
VD5123 is a serineproteaseinhibitor. VD5123 inhibits TMPRS2, HGFA, matriptase, hepsin with IC50s of 15, 3980, 140, 37 nM respectively. VD5123 can be used for antiviral research, such as SARS-CoV-2 and broad panel of coronaviruses and influenza viruses .
TMPRSS6-IN-1 (compound 8) is a potent inhibitor of TMPRSS6 (Matriptase-2), belonging to TTSPs (transmembrane serineprotease). TMPRSS6, is a type II TTSP, the genetic reduction of which will improve symptoms of hemochromatosis and beta thalassemia in mice .
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 serineproteases, such as trypsin, thrombin, and kallikrein. Darexaban has anticoagulant and antithrombotic effects .
DEC-RVRK-CMK (Decanoyl-Arg-Val-Arg-Lys-chloromethylketone) TFA is a peptide-based CMK (chloromethylketone) inhibitor that targets and inactivates the secreted soluble kexin (Kex2) (Ki=8.45 μM). The yeast enzyme Kex2 (kexin, EC 3.4.21.61) is a calcium-dependent transmembrane protease and belongs to the mammalian protease family of the serineprotease subtilisin family. The binding mechanism of Kex2 with different CMK inhibitors depends on substrate selectivity, particularly the selective differences between lysine and arginine at the P1 position .
UKI-1 (WX-UK1) is a potent urokinase-type plasminogen activator (uPA)inhibitor with a Ki of 0.41 μM. UKI-1 is also a low molecular weight serineproteaseinhibitor. UKI-1 is a potent antimetastatic agent and inhibits the invasive capacity of carcinoma cells .
Guanoxyfen (N-(3-Phenoxypropyl)guanidine) nitrate is a compound that exhibits potent inhibitory activity against the serineprotease enzyme TMPRSS2, which plays a crucial role in the infectivity of coronaviruses. Guanoxyfen nitrate is also an effective inhibitor of vasoconstrictor responses to sympathetic nerve stimulation.
Agkistrodon halys batroxobin is a thrombin-like serineprotease. Agkistrodon halys batroxobin reduces the expression of Sirt1 and extracellular signal-regulated kinase activation in brain tissue. Agkistrodon halys batroxobin reduces cleaved caspase-3 expression and inhibits neuronal apoptosis in rat .
Razaxaban hydrochloride (BMS 561389 hydrochloride) is a highly potent, selective and orally active factor Xainhibitor with a Ki of 0.19 nM. Razaxaban hydrochloride exhibits excellent selectivity (>5000-fold) for factor Xa over other related serineproteases. Razaxaban hydrochloride is also a potent thrombininhibitor with a Ki of 540 nM. Razaxaban hydrochloride has strongly antithrombotic activity .
DX-9065a is a selective, nonpeptidic, and orally active factor Xa (FXa)inhibitor with a Ki of 41 nM for human FXa. DX-9065a has low activity against other serineproteases. DX-9065a has strong anticoagulant actions .
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 serineproteaseinhibitor 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 .
Nafamostat, an anticoagulant, is a synthetic serineproteaseinhibitor. Nafamostat has anticancer and antivirus effect. Nafamostat induce apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1). Nafamostat can be used in the development of the pathological thickening of the arterial wall .
Nafamostat hydrochloride, an anticoagulant, is a synthetic serineproteaseinhibitor. Nafamostat hydrochloride has anticancer and antivirus effect. Nafamostat hydrochloride induces apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1). Nafamostat hydrochloride can be used in the development of the pathological thickening of the arterial wall .
Nafamostat formate salt- 13C6 is the 13C labeled Nafamostat. Nafamostat, a synthetic serineproteaseinhibitor, is an anticoagulant. Nafamostat supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat blocks activation of SARS-CoV-2 .
6-(Dimethylamino) purine (6-Dimethylaminopurine) is a serine threonine protein kinaseinhibitor. 6-(Dimethylamino) purine can inhibit prolactin induced expression of lactoprotein genes in rabbit mammary gland cells. 6-(Dimethylamino) purine can affect the maturation of mammalian oocytes. 6-(Dimethylamino) purine can lead to downregulation of genes related to cell proliferation and cell cycle progression, such as proliferating cell nuclear antigen, insulin-like gene 1, and serineproteaseinhibitor 2 genes, and induce apoptosis in lymphoma cells (apoptosis) .
Proteinase, Aspergillus oryzae is a serineprotease that hydrolyzes peptide bonds in protein substrates, preferring alkaline conditions (optimal pH 10.5). It efficiently degrades casein, poly-L-glutamic acid, and poly-L-lysine, with activity irreversibly inhibited by diisopropylfluorophosphate (DFP) and potato inhibitor. This enzyme catalyzes proteolysis via serine residues in its active site, finding applications in food processing (e.g., soy sauce fermentation), detergents, and leather industries due to its high yield in solid-state fermentation and cost-effective production.
N-alpha-Tosyl-Lys chloromethyl ketone hydrochloride (TLCK hydrochloride) is an irreversible inhibitor for serineprotease, which inhibits trypsin and trypsin-like protease by alkylating histidine residues in their active site. N-alpha-Tosyl-Lys chloromethyl ketone hydrochloride inhibits caspase-3, caspase-6 and caspase-7, with IC50s of 12.0, 54.5 and 19.3 μM, respectively. N-alpha-Tosyl-Lys chloromethyl ketone hydrochloride induces apoptosis in cell HL-60, and inhibits the decrease in mitochondrial transmembrane potential during apoptosis .
Nafamostat mesylate (FUT-175), an anticoagulant, is a synthetic serineproteaseinhibitor. Nafamostat mesylate has anticancer and antivirus effect. Nafamostat mesylate induce apoptosis by up-regulating the expression of tumor necrosis factor receptor-1 (TNFR1). Nafamostat mesylate can be used in the development of the pathological thickening of the arterial wall .
FXIIa-IN-3 (Compound 8) is a potent and selective Factor XIIa (FXIIa) inhibitor, with an IC50 of 0.045 μM. FXIIa-IN-3 also exhibits a substantial margin of selectivity against related serineproteases, including FXIa, FXa, and FIXa. FXIIa-IN-3 can be used for the research of thromboembolic diseases .
VD4162 (Compound 8b) is a macrocyclic inhibitor of serineproteases. VD4162 can significantly improve potency for all four target enzymes TMPRSS2 (IC50 = 3.7 nM), HGFA(IC50 = 3.3 nM), matriptase (IC50 = 2.9 nM), and hepsin (IC50 = 0.54 nM). VD4162 can be used for the research of cancer .
Ucf-101 is a selective and competitive inhibitor of pro-apoptotic protease Omi/HtrA2, with an IC50 of 9.5 μM for His-Omi. Ucf-101 exhibits very little activity against various other serineproteases (IC50>200 μM). Ucf-101 has a natural red fluorescence at 543 nm that is used to monitor its ability to enter mammalian cells. Ucf-101 has a significant cardioprotective effect against MI/R injury and also has certain neuroprotective effect .
PfSUB1-IN-1 (compound 4c) is a plasmodium falciparum subtilisin-like serineprotease 1 (PfSUB1) Inhibitor (IC50: 15 nM). PfSUB1 is an antimalarial target. PfSUB1-IN-1 inhibits the growth of a genetically modified P. falciparum line expressing reduced levels of PfSUB1 13-fold more efficiently compared to a wild-type parasite line .
FD-IN-1 (Compound 12) is an orally bioavailable and selective factor D (FD) inhibitor with an IC50 of 12 nM. Complement FD, a highly specific S1 serineprotease, plays a central role in the alternative complement pathway of the innate immune system. FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC50s of 7.7 and 6.5 µM, respectively .
APC-6860 is a trypsin-like serineproteasesinhibitor 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 .
MASP-2-IN-1 (Compound 77) is the inhibitor for mannan-binding lectin-associated serineprotease (MASP), that inhibitsMASP2 and MASP3 with IC50 of 11.4 nM and 13.2 µM. MASP-2-IN-1 exhibits a weak inhibitory activity against hERG with an IC50 of 175 µM. MASP-2-IN-1 reveals a poor stability in mouse plasma with a half-life of 4.4 hours .
RH12 is a dual inhibitor for SARS-CoV-2 related RNA-dependent RNA polymerase (RdRp, IC50 is 4.42 nM) and human transmembrane serineprotease 2 (TMPRSS2, IC50 is 4.2 nM). RH12 exhibits antiviral efficacy. RH12 inhibits viral replication and absorption, and exhibits a 90.5% virucidal effects on Vero-E6 cells. RH12 inhibits cell viability of Calu-3 with an IC50 of 17.5 nM .
C1s Enzyme is a subunit of the complement C1 complex, which activates the complement as a serineprotease. C1s Enzyme cleaves LRP5 and LRP6, and thus activates the Wnt/β-Catenin signaling pathway. C1s Enzyme promotes the macrophage M2 polarization and inhibits M1 polarization. C1s Enzyme enhances efferocytosis, exhibits anti-inflammatory activity .
Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally active Cathepsin Cinhibitor with IC50s of 59.9 nM, 4.26 µM, >5 µM, >5 µM, >5 µM for Cat C, Cat L, Cat S, Cat B, Cat K, respectively. Cathepsin C-IN-5 inhibits the Cat C activity in bone marrow and blood. Cathepsin C-IN-5 decreases the activation of NSPs (neutrophil serineproteases). Cathepsin C-IN-5 shows anti-inflammatory activity .
CE-2072 is an inhibitor of serineproteases neutrophil elastase and proteinase-3. CE-2072 inhibitsHIV-1 production and p24 production in response to IL-18 or NaCl in infected U1 monocytic cells, reduces virus replication in infected peripheral blood mononuclear cells and blocks infection of permissive HeLa cells. CE-2072 suppresses activation of the HIV-1-inducing transcription factor NF-kB in U1 cells. CE-2072 is promising for research of HIV-1-related disease .
Cholesteryl sulfate sodium is an orally available, NPC2-targeted cholesterol biosynthesis agonist. Cholesteryl sulfate sodium activates SREBP2 by competitively binding to NPC2, promoting cholesterol synthesis (EC50=50 μM). Cholesteryl sulfate sodium enhances the self-assembly ability of Mitoxantrone hydrochloride (HY-13502A), while repairing the intestinal mucosal barrier and inhibiting inflammation by regulating serineprotease activity and PKCη signaling pathway. Cholesteryl sulfate sodium is a component of the platelet cell membrane and supports platelet adhesion. Cholesteryl sulfate sodium also regulates the activity of selective protein kinase C isoforms and modulates the specificity of PI3K, playing a role in keratinocyte differentiation .
Benzamidine (Benzenecarboximidamide) hydrochloride hydrate is a reversible competitive trypsin-like serineproteasesinhibitor with Kis of 20, 21, 97, 110, 320 and 750 μM against Tryptase, Trypsin, uPA, Factor Xa, Thrombin and tPA, respectively .
Agkistrodon halys batroxobin is a thrombin-like serineprotease. Agkistrodon halys batroxobin reduces the expression of Sirt1 and extracellular signal-regulated kinase activation in brain tissue. Agkistrodon halys batroxobin reduces cleaved caspase-3 expression and inhibits neuronal apoptosis in rat .
Proteinase, Aspergillus oryzae is a serineprotease that hydrolyzes peptide bonds in protein substrates, preferring alkaline conditions (optimal pH 10.5). It efficiently degrades casein, poly-L-glutamic acid, and poly-L-lysine, with activity irreversibly inhibited by diisopropylfluorophosphate (DFP) and potato inhibitor. This enzyme catalyzes proteolysis via serine residues in its active site, finding applications in food processing (e.g., soy sauce fermentation), detergents, and leather industries due to its high yield in solid-state fermentation and cost-effective production.
Dansyl-Glu-Gly-Arg-Chloromethylketone TFA is a proteaseinhibitor, and inhibitsserine/threonine proteases. Dansyl-Glu-Gly-Arg-Chloromethylketone TFA inhibits activated porcine factor IX .
Activated Protein C (390-404), human is a peptide of the activated protein C (a vitamin K-dependent serineprotease), potently inhibits APC anticoagulant activity .
DEC-RVRK-CMK (Decanoyl-Arg-Val-Arg-Lys-chloromethylketone) TFA is a peptide-based CMK (chloromethylketone) inhibitor that targets and inactivates the secreted soluble kexin (Kex2) (Ki=8.45 μM). The yeast enzyme Kex2 (kexin, EC 3.4.21.61) is a calcium-dependent transmembrane protease and belongs to the mammalian protease family of the serineprotease subtilisin family. The binding mechanism of Kex2 with different CMK inhibitors depends on substrate selectivity, particularly the selective differences between lysine and arginine at the P1 position .
Dansyl-Glu-Gly-Arg-Chloromethylketone is a proteaseinhibitor, and inhibitsserine/threonine proteases. Dansyl-Glu-Gly-Arg-Chloromethylketone inhibits activated porcine factor IX .
Leupeptin is a broad-spectrum, membrane-permeable proteaseinhibitor. Leupeptin potently inhibitsserine,cysteine and threonine proteases. Leupeptin inhibitsM pro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity .
Activated Protein C (390-404), human TFA, a peptide of the activated protein C (a vitamin K-dependent serineprotease), potently inhibits APC anticoagulant activity .
DEC-RVRK-CMK (Decanoyl-Arg-Val-Arg-Lys-chloromethylketone) is a peptide-based CMK (chloromethylketone) inhibitor that targets and inactivates the secreted soluble kexin (Kex2) (Ki=8.45 μM). The yeast enzyme Kex2 (kexin, EC 3.4.21.61) is a calcium-dependent transmembrane protease and belongs to the mammalian protease family of the serineprotease subtilisin family. The binding mechanism of Kex2 with different CMK inhibitors depends on substrate selectivity, particularly the selective differences between lysine and arginine at the P1 position .
Leupeptin hemisulfate is a broad-spectrum, membrane-permeable proteaseinhibitor. Leupeptin hemisulfate potently inhibitsserine,cysteine and threonine proteases. Leupeptin hemisulfate inhibitsM pro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity .
3,4-Dichloroisocoumarin is a potent serine-protease and SrLipinhibitor (Ki for SrLip: 26.6 μM). 3,4-Dichloroisocoumarin is opened by serineproteases and then undergoes acylation with the enzyme, thereby inhibitingprotease activity. 3,4-Dichloroisocoumarin can induce DNA fragmentation and Apoptosis. 3,4-Dichloroisocoumarin can be used in the research of multiple fields such as tumors, cardiovascular disease and enzyme catalytic mechanisms .
Cyclothiazomycin selectively inhibits renin activity and does not inhibit pepsin, aspartic acid, serine, mercaptan protease and metalloproteinases. Cyclothiazomycin has weak antifungal activity .
Leupeptin (hemisulfate) (Standard) is the analytical standard of Leupeptin (hemisulfate). This product is intended for research and analytical applications. Leupeptin hemisulfate is a broad-spectrum, membrane-permeable proteaseinhibitor. Leupeptin hemisulfate potently inhibitsserine, cysteine and threonine proteases. Leupeptin hemisulfate inhibits Mpro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity[1][2][3].
Rivulariapeptolides 1155 is a potent serineproteaseinhibitor with IC50s of 41.84, 4.94, 56.54 nM for chymotrypsin, elastase, prpteinase K, respectively .
Rivulariapeptolides 988 is a high potent and selective serineproteaseinhibitor with IC50 values of 95.46 nM, 15.29 nM and 85.50 nM for chymotrypsin, elastase and proteinase K, respectively .
Rivulariapeptolides 1121 is a high potent and selective serineproteaseinhibitor with IC50 values of 35.52 nM, 13.24 nM and 48.05 nM for chymotrypsin, elastase and proteinase K, respectively .
Rivulariapeptolides 1185 is a high potent and selective serineproteaseinhibitor with IC50 values of 13.17 nM, 23.59 nM and 55.26 nM for chymotrypsin, elastase and proteinase K, respectively .
Kynapcin-13 can non-competitively inhibit the activity of prolyl endopeptidase (PEP) with an IC50 of 76.80 μM. Kynapcin-13 has a little inhibitory effect on other serineproteases .
Kynapcin-28 can non-competitively inhibit the activity of prolyl endopeptidase (PEP) with an IC50 of 76.80 μM. Kynapcin-28 has a little inhibitory effect on other serineproteases .
Camostat mesylate (Camostat mesilate) is an orally active, synthetic serineproteaseinhibitor 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 .
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 serineproteaseinhibitor 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 .
6-(Dimethylamino) purine (6-Dimethylaminopurine) is a serine threonine protein kinaseinhibitor. 6-(Dimethylamino) purine can inhibit prolactin induced expression of lactoprotein genes in rabbit mammary gland cells. 6-(Dimethylamino) purine can affect the maturation of mammalian oocytes. 6-(Dimethylamino) purine can lead to downregulation of genes related to cell proliferation and cell cycle progression, such as proliferating cell nuclear antigen, insulin-like gene 1, and serineproteaseinhibitor 2 genes, and induce apoptosis in lymphoma cells (apoptosis) .
Cholesteryl sulfate sodium is an orally available, NPC2-targeted cholesterol biosynthesis agonist. Cholesteryl sulfate sodium activates SREBP2 by competitively binding to NPC2, promoting cholesterol synthesis (EC50=50 μM). Cholesteryl sulfate sodium enhances the self-assembly ability of Mitoxantrone hydrochloride (HY-13502A), while repairing the intestinal mucosal barrier and inhibiting inflammation by regulating serineprotease activity and PKCη signaling pathway. Cholesteryl sulfate sodium is a component of the platelet cell membrane and supports platelet adhesion. Cholesteryl sulfate sodium also regulates the activity of selective protein kinase C isoforms and modulates the specificity of PI3K, playing a role in keratinocyte differentiation .
Plasma serine protease inhibitor (SERPINA5) is a glycoproteins that inhibit serine proteases. SERPINA5 is involved in the regulation of intravascular and extravascular proteolytic activities, controls the sperm motility and fertilization and protect components of the genital tract. SERPINA5 also inhibits urinary-type plasminogen activator-dependent tumor cell invasion and metastasis. Serpin A5 Protein, Human (HEK293, His) is the recombinant human-derived Serpin A5 protein, expressed by HEK293 , with C-6*His labeled tag.
Serpin E2, a serine protease inhibitor, inhibits thrombin, trypsin, and urokinase, with a notable role in promoting neurite extension by specifically inhibiting thrombin.Its ability to bind heparin underscores interactions with glycosaminoglycans.The multifaceted inhibitory functions of Serpin E2 highlight its significance in regulating serine protease activities and potential impact on cellular processes, particularly in neurodevelopment.Serpin E2 Protein, Mouse (HEK293, His) is the recombinant mouse-derived Serpin E2 protein, expressed by HEK293 , with C-10*His labeled tag.
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.
Serpin B12 Protein inhibits trypsin and plasmin, excluding thrombin, coagulation factor Xa, or urokinase-type plasminogen activator. It may have a role in cell differentiation, interacting with SLFN12 in a pathway regulating differentiation, and potentially interacting with USP14. Serpin B12 Protein, Human (HEK293, His) is the recombinant human-derived Serpin B12 protein, expressed by HEK293 , with C-6*His labeled tag.
Serpin B12 inhibits trypsin and plasmin but not thrombin, coagulation factor Xa, and urokinase-type plasminogen activator. Additionally, it interacts with SLFN12, contributing to cellular differentiation pathways, showcasing its multifunctional nature beyond classical protease inhibition. Serpin B12 Protein, Mouse (sf9, His) is the recombinant mouse-derived Serpin B12 protein, expressed by Sf9 insect cells , with C-His labeled tag.
Serpin A3C Protein, with its reactive center loop (RCL), guides interactions with target proteases.Binding leads to protease cleavage at the RCL, forming a stable serpin-protease complex, inactivating the protease.Variability in Serpin A3C's RCL sequences among Serpina3 paralogs may influence the specificity of target protease interactions, showcasing the protein's adaptability.Serpin A3C Protein, Mouse (HEK293, His) is the recombinant mouse-derived Serpin A3C protein, expressed by HEK293 , with C-His labeled tag.
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.
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 Serpin A1c protein is a skilled guardian of cellular regulation, specifically acting as an inhibitor of serine proteases, specifically trypsin and chymotrypsin. Its efficacy in blocking enzymatic activity contrasts with its relative ineffectiveness against elastase. Serpin A1c Protein, Mouse (HEK293, His) is the recombinant mouse-derived Serpin A1c protein, expressed by HEK293 , with C-6*His labeled tag.
Serpin A5 protein is a heparin-dependent serine protease inhibitor that controls proteolytic activity in body fluids. It binds irreversibly to the serine activation site, inactivating serine proteases and regulating intravascular and extravascular proteolysis. Serpin A5 Protein, Mouse (Sf9, His) is the recombinant mouse-derived Serpin A5 protein, expressed by Sf9 insect cells , with N-10*His labeled tag.
The SPINK4 protein is specifically expressed in the intestine, suggesting a potential role in gastrointestinal physiology.Its local expression implies involvement in digestive system processes, regulation of protease activity, or other functions critical to intestinal homeostasis.SPINK4 Protein, Mouse (HEK293, Fc) is the recombinant mouse-derived SPINK4 protein, expressed by HEK293 , with C-hFc labeled tag.
The SPINK4 protein acts as a serine-type endopeptidase inhibitor, regulating peptidase activity.It is located in the extracellular region, suggesting that it has inhibitory functions outside the cell.SPINK4 Protein, Mouse (HEK293, His) is the recombinant mouse-derived SPINK4 protein, expressed by HEK293 , with C-His, C-6*His labeled tag.
Vaspin is an adipokine that regulates adipogenesis, metabolism, and inflammation by binding to the chemokine receptors CMKLR1 and CMKLR2. It mainly regulates adipocyte differentiation and affects lipid and glucose metabolism genes. Vaspin Protein, Human (GST) is the recombinant human-derived Vaspin protein, expressed by E. coli , with N-GST labeled tag.
The serpin A3N protein is ubiquitously found in a variety of tissues, showing elevated expression in the brain, heart, liver, lung, spleen, testis, and thymus, implying a variety of physiological functions.In contrast, it shows lower expression in bone marrow, kidney, and skeletal muscle, suggesting a tissue-specific pattern of regulation.Serpin A3N Protein, Mouse (HEK293, His) is the recombinant mouse-derived Serpin A3N protein, expressed by HEK293 , with C-6*His labeled tag.
The serpin A3N protein is ubiquitously found in a variety of tissues, showing elevated expression in the brain, heart, liver, lung, spleen, testis, and thymus, implying a variety of physiological functions.In contrast, it shows lower expression in bone marrow, kidney, and skeletal muscle, suggesting a tissue-specific pattern of regulation.Serpin A3N Protein, Mouse (P.pastoris, His) is the recombinant mouse-derived Serpin A3N protein, expressed by P.pastoris , with N-6*His labeled tag.
The Serpin A3N Protein, belonging to the serpin family, is predominantly expressed in the liver, where it regulates protease activity.As a serine protease inhibitor, Serpin A3N plays a crucial role in modulating enzymatic processes within the liver, highlighting its significance in hepatic functions and maintaining the balance of proteolytic activities in this vital organ.Serpin A3N Protein, Rat (HEK293, His) is the recombinant rat-derived Serpin A3N protein, expressed by HEK293 , with C-His labeled tag.
SPINK4 Protein is a member of the serine protease inhibitors family named Kazal type (SPINK) in humans. SPINK4 is known as a gastrointestinal peptide in the gastrointestinal tract and is abundantly expressed in human goblet cells. SPINK4 can serve as a prognostic marker for colorectal cancer (CRC), bladder cancer (BCa) and Barrett's esophagus. The reduced expression of SPINK4 relates to poor survival in colorectal cancer (CRC). SPINK4 Protein, Human (60a.a, HEK293, His) is the recombinant human-derived SPINK4 protein, expressed by HEK293 , with C-6*His labeled tag.
Vaspin is an adipokine that regulates adipogenesis, metabolism, and inflammation by binding to the chemokine receptors CMKLR1 and CMKLR2. It mainly regulates adipocyte differentiation and affects lipid and glucose metabolism genes. Vaspin Protein, Human (HEK293, His) is the recombinant human-derived Vaspin protein, expressed by HEK293 , with C-10*His labeled tag.
Serpin I2 Protein, is a member of the serpin (serine protease inhibitor) superfamily. Serpin I2 (pancpin) is an inhibitory serpin targeting pancreatic elastase and chymotrypsin. Serpin I2 is downregulated in pancreatic and breast cancer, and associated with acinar cell apoptosis and pancreatic insufficiency when absent in mice. Serpin I2 is associated with refractive error and has the potential for further investigations of the genetic susceptibility to myopia research. Serpin I2 Protein, Human (HEK293, His) is the recombinant human-derived Serpin I2 protein, expressed by HEK293 , with C-6*His labeled tag.
The Serpina1d protein is a vigilant sentinel in cellular regulation, acting specifically as an inhibitor of serine proteases, particularly trypsin and chymotrypsin. It effectively blocks their enzymatic activity but appears relatively ineffective against elastase. Serpina1d Protein, Mouse (HEK293) is the recombinant mouse-derived Serpina1d protein, expressed by HEK293 , with tag free.
The Serpina1d protein is a vigilant sentinel in cellular regulation, acting specifically as an inhibitor of serine proteases, particularly trypsin and chymotrypsin. It effectively blocks their enzymatic activity but appears relatively ineffective against elastase. Serpina1d Protein, Mouse (HEK293, Fc) is the recombinant mouse-derived Serpina1d protein, expressed by HEK293 , with C-hFc labeled tag.
The Serpina1d protein is a vigilant sentinel in cellular regulation, acting specifically as an inhibitor of serine proteases, particularly trypsin and chymotrypsin. It effectively blocks their enzymatic activity but appears relatively ineffective against elastase. Serpina1d Protein, Mouse (HEK293, His) is the recombinant mouse-derived Serpina1d protein, expressed by HEK293 , with C-His labeled tag.
SPINK7 Protein, a probable serine protease inhibitor, suggests a role in modulating serine protease activity, crucial in diverse biological processes. Its participation likely regulates proteolytic activities, influencing cellular homeostasis and signaling pathways. Further exploration of specific targeted serine proteases and biological contexts will offer insights into SPINK7's role in cellular processes and potential therapeutic applications. SPINK7 Protein, Human (HEK293, His) is the recombinant human-derived SPINK7 protein, expressed by HEK293 , with C-6*His labeled tag.
Nafamostat formate salt- 13C6 is the 13C labeled Nafamostat. Nafamostat, a synthetic serineproteaseinhibitor, is an anticoagulant. Nafamostat supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat blocks activation of SARS-CoV-2 .
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