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.
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-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].
AAF-CMK is a TPPII (tripeptidylpeptidase II) inhibitor, shows anti-tumor activity and induces apoptosis. AAF-CMK can be used in leukemia research[1].
Manusiran is a potent TMPRSS6 (transmembrane protease serine 6) synthesis reducer[1].
Ono 3403 is a synthetic serine protease inhibitor. Ono 3403 inhibits lipopolysaccharide-induced tumor necrosis factor-alpha and nitric oxide production. ONO-3403 also has an antitumor effect on malignant tumors.
Patamostat (E-3123) is a potent protease inhibitor. Patamostat potently inhibits trypsin, plasmin and thrombin with IC50s of 39 nM, 950 nM and 1.9 μM, respectively. E-3123 may possess suppressing effects on pathogenesis and development of acute pancreatitis[1][2].
PCSK9-IN-13(compound 3f) is a potent PCSK9 inhibitor, which can antagonize low-density lipoprotein (LDL) receptor binding by binding to PCSK9, with an IC50 of 537 nM[1].
Z-Val-Gly-Arg-pNA is a chromogenic substrate for urokinase. Z-Val-Gly-Arg-pNA can be used for determination of urokinase activity[1].
UK-371804 is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM.
PF-06815345 (PF 6815345) is a potent prodrug PCSK9 modulator that inhibits PCSK9 secretion in vitro translation assay; PF-06815345is identified after optimization of the prodrug moiety to maximize intestinal stability achieving liver targeting of the active compound after prodrug turnover by carboxylesterase (CES1). Hypercholesterolemia Phase 1 Discontinued
HMB-Val-Ser-Leu-VE is a prototype vinyl ester inhibitor. HMB-Val-Ser-Leu-VE is against trypsin-like (T-L) proteasome activity with an IC50 of 0.033 μM[1].
Upamostat is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.
Flizasertib is a serine/threonine kinase inhibitor[1].
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].
Kallikrein-IN-2 (compound 1) is a Kallikrein inhibitor[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.
BC-11 hydrobromide is a selective TMPRSS2 inhibitor (TMPRSS2 is a key host cellular factor for viral entry and SARS-CoV-2 pathogenesis), and a selective urokinase (uPA) inhibitor (IC50=8.2 μM). BC-11 hydrobromide is cytotoxic to triple-negative MDA-MB231 breast cancer cells. BC-11 hydrobromide is used in research on viral infections and cancer[1][2][3].
PCSK9-IN-16 is a potent PCSK9 inhibitor. PCSK9-IN-16 is extracted from patent WO2020150474, example 87, has the potential for hypercholesterolemia and other cardiovascular diseases research[1].
PPACK II diTFA is an irreversible and specific glandular and plasma kallikreins inhibitor[1].
Recombinant Kex2 protease is a membrane-bound, Ca2+-dependent serine protease. Recombinant Kex2 protease specifically recognize and cleave the carboxyl-terminal peptide bonds of dibasic amino acids[1].
Ralpancizumab is a selective PCSK9 inhibitor with potential application in hemorrhagic stroke[1].
Suc-AAPR-pNA is a substrate of trypsin acyl-enzymes. Suc-AAPR-pNA can be used to test trypsin acyl-enzymes activity[1][2].
Frovocimab (LY 3015014) is a humanized IgG4 monoclonal antibody (mAb) that neutralizes PCSK9. Frovocimab inhibits PCSK9 binding to LDL receptor (LDLR) while permitting the normal proteolytic cleavage of the bound intact PCSK9[1].
PF-06815345 hydrochloride is an orally active and potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) with an IC50 value of 13.4 μM. PF-06815345 hydrochloride significantly decreases the PCSK9 level in vivo in mouse[1][2].
Bococizumab (PF-04950615) is an anti-human PCSK9 inhibitory antibody that reduces LDL cholesterol levels. Bococizumab can be used in the research of hypercholesterolemia[1][2].
ZK824190 is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively[1].
PPACK II is an irreversible and specific glandular and plasma kallikreins inhibitor[1].
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].
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].