ONO-3307 is a protease inhibitor 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[1][2].
Ac-Phe-Gly-pNA is the chymotrypsin specific substrate[1].
SPC4061 an antisense nucleotide, is a potent PCSK9 inhibitor. SPC4061 targets the lock-in nucleic acid (LNA) of PCSK9 for the study of hypercholesterolemia and related diseases[1][2].
Aprotinin is a bovine pancreatic trypsin inhibitor (BPTI) inhibitor which inhibits trypsin and chymotrypsin with Kis of 0.06 pM and 9 nM, respectively.
AAA-pNA is a chromogenic substrate of Tripeptidyl-peptidase II. AAA-pNA can be used to test Tripeptidyl-peptidase II activity[1].
WNK1-IN-1 is a selective inhibitor of WNK1 with an IC50 value of 1.6 μM. WNK1-IN-1 inhibits OSR1 phosphorylation with an IC50 value of 4.3 μM. WNK1-IN-1 can be used for the research of blood pressure regulation and cancer[1].
Benzenecarboximidamide, hydrochloride, hydrate (1:1:x) (Benzamidine hydrochloride hydrate) is a reversible competitive trypsin-like serine proteases inhibitor with Kis of 20, 21, 97, 110, 320 and 750 μM against Tryptase, Trypsin, uPA, Factor Xa, Thrombin and tPA, respectively[1][2].
Rennin, also known as Chymosin, is a pepsin-related proteolytic enzyme synthesized by cells in the stomach of certain animals that efficiently converts liquid milk into a semi-solid, allowing it to remain in the stomach for longer. The natural substrate of Rennin is K-casein, which is specifically cleaved at the peptide bond between amino acid residues 105 and 106, phenylalanine and methionine, and is widely used in cheese production[1].
Ecallantide (DX-88) is a specific recombinant plasma kallikrein inhibitor. Ecallantide inhibits the production of bradykinin. Ecallantide can be used to prevent acute attacks of angioedema[1].
Bezeparsen is a PCSK9 synthesis inhibitor[1].
Tilpisertib fosmecarbil is a potent serine/threonine kinase inhibitor. Tilpisertib fosmecarbil has anti-inflammatory activity[1].
PKR-IN-C51(compound 51) is an ATP-competitive double-stranded RNA-activated protein kinase (PKR) inhibitor with an IC50 of 9 μM. PKR-IN-C51 inhibits intracellular PKR activation in a dose-dependent manner in primary mouse macrophages[1].
TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is a potent serine protease inhibitor that reacts with the retinoblastoma protein (RB)-binding core of HPV-18 E7 protein and abolish its RB-binding capability. TPCK is able to modify E7 protein in live keratinocytes following its addition to the culture medium[1].
Irucalantide is kallikrein inhibitor[1].
Urokinase peptidolytic (Urokinase-type plasminogen activator) is a serine protease, an inactive form (zymogen) of the serine protease plasminogen. Activation of plasmin triggers a proteolytic cascade reaction, which in turn participates in thrombolysis or extracellular matrix degradation, implicated in vascular disease and cancer-related research[1].
Ala-Phe-Pro-pNA is a chromogenic substrate of tripeptidyl peptidase. Ala-Phe-Pro-pNA can be used to test tripeptidyl peptidase activity[1].
PCSK9-IN-17 is a PCSK9 inhibitor. PCSK9-IN-17 can be used for the research of cholesterol metabolism (WO2020150474A1, compound 105)[1].
Dansyl-Glu-Gly-Arg-Chloromethylketone is a protease inhibitor, and inhibits serine/threonine proteases. Dansyl-Glu-Gly-Arg-Chloromethylketone inhibits activated porcine factor IX[1].
Antipain dihydrochloride is a protease inhibitor isolated from Actinomycetes. Antipain dihydrochloride inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations. Antipain dihydrochloride restricts uterine DNA synthesis and function in mice[1][2][3][4].
BMS-262084 is a potent, selective and irreversible inhibitor of factor XIa, with an IC50 of 2.8 nM against human factor XIa. BMS-262084 also inhibits human tryptase (IC50=5 nM). BMS-262084 exhibits antithrombotic effects[1][2].
Tos-Gly-Pro-Lys-AMC is a fluorogenic peptide substrate of tryptase[1].
Nafamostat mesylate, a synthetic serine protease inhibitor, is an anticoagulant.Target: Serine ProteaseTranilast (FUT-175) is an antiallergic drug for bronchial asthma. It has been used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis. It has also been investigated for use as an antiproliferative drug on drug-eluting stents.A 20-40 mg/h dose of FUT-175 prolonged coagulation time sufficiently in the instrumental blood of the extracorporeal circuit but not in the systemic blood. Its anticoagulant activity decreased immediately after hemodialysis. Therefore, we could manage all patients without any bleeding trouble during hemodialysis with FUT-175 as an anticoagulant. Although there were side effects of FUT-175, such as nausea, vomiting, itching and eruption, they were not serious, and FUT-175 could be administered without interruption. FUT-175 seems to be useful as an anticoagulant during hemodialysis for patients susceptible to bleeding.
DPP-IV-IN-1 is a potent inhibitor of dipeptidyl peptidase IV (DPP-IV), a highly specific serine protease, with an IC50 of 4.6 nM.
CRA-2059 is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ)[1][2].
Boc-Gln-Ala-Arg-AMC hydrochloride is a fluorogenic substrate for trypsin. Boc-Gln-Ala-Arg-AMC hydrochloride can also be used for measuring the proteolytic activity of TMPRSS2[1][2].
PCSK9-IN-1 is a novel and highly potent cyclic peptide PCSK9 inhibitor with a Ki value of 1.46 nM.
4-Aminobenzamidine (p-Aminobenzamidine) dihydrochloride is a strong trypsin inhibitor, 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[1][2].
Kallikrein-IN-1 (Formula A) is a Kallikrein inhibitor[1].
PCSK9-IN-18 (compound 188) is a potent PCSK9 inhibitor with a KD value of <200 nM[1].
Ongericimab (JS002) is a humanized anti-PCSK9 monoclonal antibody. Ongericimab has lipid-lowering efficacy. Ongericimab can be used in research of hypercholesteremia and hyperlipidemia[1].