PPACK II is an irreversible and specific glandular and plasma kallikreins inhibitor[1].
TP-030-2 is a RIPK1 inhibitor (human Ki=0.43 nM; mouse IC50=100 nM)[1][2].
Recaticimab (SHR-1209) is a humanized monoclonal antibody that inhibits PCSK9. Receticimab mediates the degradation of PCSK9 by binding to PCSK9, increasing the level of low-density lipoprotein (LDL) receptors on the surface of hepatocytes, reducing the level of LDL in plasma, and achieving the goal of lowering blood lipids. Recaticimab has potential application in hypercholesterolemia[1][2].
Suc-AAPA-pNA is a substrate of chymotrypsin Aα. Suc-AAPA-pNA can be used to test chymotrypsin Aα activity[1].
Ulinastatin (Uristatin) is a trypsin and serine protease inhibitor. 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[1][2].
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].
Dim16 is a dual PCSK9/HMG-CoAR inhibitor, with an IC50 value of 19 nM for PCSK9. Dim16 inhibits PCSK9-LDLR binding with an IC50 value of 0.8 nM. Dim16 increases LDL uptake in HepG2 cells[1].
Ac-Phe-Gly-pNA is the chymotrypsin specific substrate[1].
Ac-Gly-Lys-OMe is a substrate for urokinase. Ac-Gly-Lys-OMe can be used to measure the effects of small molecule inhibitors on urokinase activity[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].
PCSK9 degrader 1 is a selective proprotein convertase substilisin-like/kexin type 9 (PCSK9) degrader. PCSK9 degrader 1 does not affect PCSK9 function[1].
Aprotinin is a bovine pancreatic trypsin inhibitor (BPTI) inhibitor which inhibits trypsin and chymotrypsin with Kis of 0.06 pM and 9 nM, respectively.
Glutamic acid protease only can be found in fungi. Glutamic protease is a proteolytic enzyme containing a glutamic acid residue[1].
PCSK9-IN-10 is a potent and orally active PCSK9 inhibitor with an IC50 value of 6.4 µM. PCSK9-IN-10 increases the expression of LDLR protein and decreases the expression of PCSK9. PCSK9-IN-10 reduces atherosclerosis progression. PCSK9-IN-10 has the potential for the research of hyperlipidemia[1].
Cetraxate hydrochloride (DV-1006), an orally active anti-ulcer agent with mucosal protective effects, can be used for gastric ulcers research[1]. Cetraxate hydrochloride is a potent acrosomal proteinase acrosin inhibitor with a Ki and an IC50 of 0.94 μM and 3.3 μM, respectively[2].
Trypsin is an enzyme that hydrolyzes proteins at the carboxyl side of the Lysine or Arginine. Trypsin activates PAR2 and PAR4. Trypsin induces cell-to-cell membrane fusion in PDCoV infection by the interaction of S glycoprotein of PDCoV and pAPN. Trypsin also promotes cell proliferation and differentiation. Trypsin can be used in the research of wound healing and neurogenic inflammation[1][2][3][4][6].
NSC45586 free base (NCS 45586, NCI45586) is a potent, specific PHLPP2 inhibitor with IC50 of 4 uM, targets the PHLPP2 PP2C domain, suppresses MYC and triggers cell death.
AAA-pNA is a chromogenic substrate of Tripeptidyl-peptidase II. AAA-pNA can be used to test Tripeptidyl-peptidase II activity[1].
VD2173 is a side chain cyclized macrocyclic peptide inhibitor of HGF-activating serine proteases. VD2173 potently inhibits matriptase and hepsin. VD2173 can be used for the research of lung cancer[1].
PCSK9-IN-14 (compound Ia-8) is a potent PCSK9 inhibitor[1].
Phe-Pro-Ala-pNA is a chromogenic substrate of tripeptidyl peptidase. Phe-Pro-Ala-pNA can be used to test tripeptidyl peptidase activity[1].
PCSK9-IN-20 (Compound 3i) is a PCSK9 inhibitor with an IC50 of 3.96 µM. PCSK9-IN-20 decreases PCSK9 and increases LDLR protein expression in vitro[1].
Enteropeptidase (TMPRSS15), a type II transmembrane serine protease and a physiological activator of trypsinogen. Enteropeptidase is associated with the brush border membrane (BBM) of the enterocytes in the upper small intestine. Trypsinogen is the primary substrate for Enteropeptidase. Enteropeptidase is involved in digestion in humans and animals[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].
SBC-115337, as a potent benzofuran compound, is a PCSK9 inhibitor with an IC50 value of 0.5 μM[1][2].
PCSK9-IN-22 (compound 29) is an orally active inhibitor of PCSK9. PCSK9-IN-22 inhibits the interaction of the protein with LDLR in vivo[1].
Lerodalcibep (LIB003) is a recombinant fusion protein of a PCSK9-binding domain (adnectin) and human serum albumin. Lerodalcibep is a Lipid-lowering agent. Lerodalcibep can be used for the research of hypercholesterolemia and cardiovascular diseases[1].
AAF-CMK is a TPPII (tripeptidylpeptidase II) inhibitor, shows anti-tumor activity and induces apoptosis. AAF-CMK can be used in leukemia research[1].
N-Benzoyl-L-tyrosine p-nitroanilide is a chymotrypsin substrate[1].
Manusiran is a potent TMPRSS6 (transmembrane protease serine 6) synthesis reducer[1].