CRA-2059 is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ)[1][2].
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].
Leupeptin is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin potently inhibits serine, cysteine and threonine proteases. Leupeptin inhibits Mpro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity[1][2][3].
Plasma kallikrein-IN-4 (Example 153) is a plasma kallikrein inhibitor with an IC50 of 0.016 μM against human plasma kallikrein[1].
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.
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].
TAO Kinase inhibitor 2 (Example 49) is a TAO Kinase inhibitor (IC50=between 50 and 500 nM). TAO Kinase inhibitor 2 also inhibits KIAA1361 and JIK with IC50s of 50-500 nM[1].
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].
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].
PCSK9-IN-18 (compound 188) is a potent PCSK9 inhibitor with a KD value of <200 nM[1].
APC-6860 is a trypsin-like serine proteases inhibitor 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[1][2].
DCLK1-IN-2 (compound I-5) is a potent DCLK1 inhibitor with an IC50 of 171.3 nM. DCLK1-IN-2 shows remarkable antiproliferative effects on SW1990 cell lines (IC50 of 0.6 μM) and in vivo antitumor potency[1].
Bz-D-Arg-pNA hydrochloride is a competitive trypsin inhibitor[1].
Ralpancizumab is a selective PCSK9 inhibitor with potential application in hemorrhagic stroke[1].
Ebronucimab (AK102) is an IgG1-λ2 antibody targeting PCSK9 and is primarily expressed by CHO DG44 (Chinese Hamster Ovary) cells[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].
NBI-961 is a potent NEK2 inhibitor that inhibits proteasomal degradation. NBI-961 induces G2/mitosis arrest and apoptosis in diffuse large B cell lymphoma (DLBCL) cells[1].
Plasma kallikrein-IN-3 is a plasma kallikrein inhibitor (IC50: 0.15 μM). Plasma kallikrein-IN-3 can be used for hereditary angioedema, diabetic macular edema, and diabetic retinopathy research[1].
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].
Tilpisertib is a serine/threonine kinase inhibitor (WO2017007689)[1].
GGACK (H-Glu-Gly-Arg-CMK) is an irreversible substrate-like serine protease urokinase-type plasminogen activator (uPA) inhibitor[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].
TMPRSS6-IN-1 (compound 8) is a potent inhibitor of TMPRSS6 (Matriptase-2), belonging to TTSPs (transmembrane serine protease). TMPRSS6, is a type II TTSP, the genetic reduction of which will improve symptoms of hemochromatosis and beta thalassemia in mice[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].
Trypsin Inhibitor, soybean is a potent and reversible inhibitor of trypsin[1].