Chymotrypsin (Chymotrypsin A) is a serine protease produced by the pancreas. Chymotrypsin cleaves protein chains at the carboxyl side of aromatic amino acids[1][2].
Flizasertib is a serine/threonine kinase inhibitor[1].
5-O-Methylembelin is a natural isocoumarin that inhibits PCSK9, low-density lipoprotein receptor (IDOL), and sterol regulatory element binding protein 2 (SREBP2) mRNA expression[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].
PF-06446846 (PF-6446846) is a potent, highly selective inhibitor of PCSK9 translation with IC50 of 0.3 uM for inhibition the secretion of PCSK9 by Huh7 cells; shows no general effect on the secreted and intracellular proteome; induces the ribosome to stall around codon 34, mediated by the sequence of the nascent chain within the exit tunnel; reduces plasma PCSK9 and total cholesterol levels in rats following oral dosing.
Boc-QAR-pNA is a chromogenic substrate of trypsin. Boc-QAR-pNA can be used to test trypsin activity[1][2].
Lanadelumab (SHP643) is a humanized IgG1 monoclonal antibody against plasma kallikrein (pKal) with an Ki value of 0.12 nM. Lanadelumab inhibits both free and HMWK (high molecular weight kininogen)-bound pKal. Lanadelumab has the potential for the research of hereditary angioedema[1][2].
Nafamostat hydrochloride, 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.
Nafamostat is a broad spectrum serine protease inhibitor, kallikrein inhibitor, and inhibits blood coagulation; is also a possible complement inhibitor.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.
WNK-IN-11 D3 is an orally active, selective and potent With-No-Lysine (WNK) kinase inhibitor. WNK-IN-11 D3 is effective at regulating cardiovascular homeostasis[1].
Chymotrypsinogen is an inactive precursor of Chymotrypsin (HY-108910). Chymotrypsin is a serine protease produced by the pancreas[1][2].
Urinary Trypsin Inhibitor Fragment is a fragment derived from urinary trypsin inhibitor by proteolysis. Urinary Trypsin Inhibitor Fragment can inhibit tumor cell invasion by limited proteolysis[1].
UAMC-00050 is a potent trypsin-like serine protease inhibitor. UAMC-00050 can be used in research of dry eye syndrome and ocular inflammation[1].
Enlicitide chloride is a potent PCSK9 antagonist. Enlicitide chloride can be used for research of cardiovascular disease, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions[1][2].
Pinostrobin is a flavonoid can be found in many plants, and has anti-oxidant, anti-inflammatory, anti-cancer and neuroprotective properties. Pinostrobin is a potent PCSK9 inhibitor and inhibits the catalytic activity of PCSK9. Pinostrobin is a promising agent for cholesterol regulation and lipid management[1].
PCSK9-IN-12 is a heteroaryl compound. PCSK9-IN-12 has bind affinity for PCSK9 with a Kd value of ＜200 nM. PCSK9-IN-12 can be used for the research of cholesterol metabolism[1].
PKSI-527 is a new, highly selective plasma kallikrein inhibitor. PKSI-527 can suppress collagen-induced arthritis (CIA) by modifying the kallikrein-kinin system[1].
PCSK9-IN-2 is a novel small molecule inhibitor of PCSK9-LDLR protein–protein interaction (PPI) with an IC50 value of 7.57 μM.
PCSK9-IN-17 is a PCSK9 inhibitor. PCSK9-IN-17 can be used for the research of cholesterol metabolism (WO2020150474A1, compound 105)[1].
AP-C2 is a potent guanosine 3',5'-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) inhibitor with a pIC50 of 5.2[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].
A potent, selectiive inhibitor of WNK1 kinase with IC50 of 95 nM, shows IC50 of 1.39 uM in the cellular OSR1 phosphorylation assay with reasonable aqueous solubility.
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].
Kallikrein-IN-2 (compound 1) is a Kallikrein inhibitor[1].
Tos-Gly-Pro-Lys-AMC is a fluorogenic peptide substrate of tryptase[1].
GCN2-IN-1 is a potent general control nonderepressible 2 kinase (GCN2) inhibitor with IC50s of <0.3 μM in the enzyme and cell assay.
Tafolecimab (IBI-306) is a human lgG2 monoclonal antibody that specifically binds PCSK-9 and reduces LDL-C levels by inhibiting PCSK-9-mediated endocytosis of the LDL receptor, which in turn enhances clearance of LDL-C and leads to a reduction in LDL-C levels. Tafolecimab may be used in studies of hypercholesterolaemia[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.