matriptase

SRI 31215 TFA, a small molecule that acts as a triplex inhibitor of matriptase, hepsin and HGFA and mimics the activity of HAI-1/2, endogenous inhibitors of HGF activation with IC50s of 0.69 μM, 0.65 μM, 0.3 μM,

Anti-Matriptase Antibody is a human-derived antibody expressed in CHO cells, targeting Matriptase.

Matriptase-IN-2 free base, a matriptase inhibitor with a K i of 5 nM, has potential applications in musculoskeletal system disorder research (WO2011023958A1; compound 432) [1].

TMPRSS6-IN-1 (TFA) is a potent inhibitor of TMPRSS6 (Matriptase-2), a member of the TTSP family (a type of transmembrane serine protease). TMPRSS6 is a type II TTSP, and genetically reduced levels of TMPRSS6 have been shown to improve symptoms of hemochromatosis and β-thalassemia in mice.

VD5123 is a serine protease inhibitor that targets TMPRSS2, HGFA, matriptase, and hepsin with IC50 values of 15, 3980, 140, and 37 nM, respectively. It is useful in antiviral research, particularly concerning SARS-CoV-2, as well as a wide range of coronaviruses and influenza viruses.

WGU55 is a selective and potent reversible type II transmembrane serine protease TMPRSS6 inhibitor with a Ki value of 12.15 nM. In KEK293 cells, WGU55 inhibits TMPRSS6 activity with an IC50 value of 138 nM. It displays a Ki value of 3510 nM for the homologous protease matriptase (SI=289) and a Ki value of 5.2 μM for the key coagulation protease factor Xa. WGU55 is applicable in the study of iron overload-related diseases, such as hereditary hemochromatosis.

Cbz-QFR-kbt is a ketobenzothiazolone-based TMPRSS2 inhibitor with an IC50 of 0.42 nM. It also exhibits inhibitory activity against Matriptase, Hepsin, HGFA, and Factor Xa, with IC50 values of 1, 1.3, 85, and 85 nM, respectively. Furthermore, Cbz-QFR-kbt demonstrates significant inhibitory effects on SARS-CoV-2 and H1N1 (IC50= 60 nM) and is applicable for antiviral research.

VD2173, a macrocyclic peptide inhibitor with a side chain cyclization, effectively inhibits HGF-activating serine proteases including matriptase and hepsin, and is utilized in lung cancer research [1].

VD4162 (Compound 8b), a macrocyclic inhibitor of serine proteases, exhibits enhanced potency against four key target enzymes: TMPRSS2 (IC 50 = 3.7 nM), HGFA (IC 50 = 3.3 nM), matriptase (IC 50 = 2.9 nM), and hepsin (IC 50 = 0.54 nM). This compound is utilized in cancer research [1].

MI-1904 is an inhibitor of matriptase/TMPRSS2, exhibiting antiviral activity against influenza virus (influenza virus) strains H1N1 and H9N2. This compound prevents the cleavage of viral surface glycoproteins, thereby inhibiting the binding of the virus to host cell receptors, which effectively blocks viral entry and replication.

Stromemycin is a matriptase inhibitor. On its own, Stromemycin exhibits weak antibacterial activity against Staphylococcus aureus, vancomycin-resistant Enterococcus faecium, and Bacillus subtilis. However, its antibacterial effectiveness significantly increases when used in combination with Compound 5. Additionally, Stromemycin does not show significant cytotoxicity against HCT-116 cells.