Cathepsin Inhibitor

VK13 (Compound 6) is a potent inhibitor of human cathepsin L (hCatL) with a K_i value of 0.55 nM and SARS-CoV-2 3CL^pro (3CL-PR) with a K_i value of 2.6 nM. VK13 exhibits anti-CoV-2 activity with an EC₅₀ of 1.25 μM.

ONO-5334 (Standard) is the analytical standard of ONO-5334 (HY-108044). This product is intended for research and analytical applications. ONO-5334 is a potent, selective and orally active cathepsin K inhibitor with K_i values of 0.10 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively. ONO 5334 is an effective antiviral compound against SAR-COV-2 virus activity with an EC₅₀ value of 500 nM. ONO-5334 has the potential for the study of osteoporosis and COVID-19 disease.

JPM-OEt (Standard) is the analytical standard of JPM-OEt (HY-102087). This product is intended for research and analytical applications. JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity.

UAWJ9-36-3 is a M^pro and cathepsin L (IC₅₀: 1.81 μM) inhibitor. UAWJ9-36-3 shows potent binding and enzymatic inhibition against the M^pros from SARS-CoV-2, SARS-CoV, MERS-CoV, HCoV-OC43, HCoV-NL63, HCoV-229E, and HCoV-HKU1. UAWJ9-36-3 demonstrates broad-spectrum antiviral activity against not only SARS-CoV-2, but also the common human coronaviruses HCoV-OC43, HCoV-NL63, and HCoV-229E.

Cathepsin K-IN-9 is a selective, potent and orally active Cathepsin K inhibitor with an IC₅₀ of 6.2 nM. Cathepsin K-IN-9 has IC₅₀ > 10000 nM for cathepsin B, L, and S, showing over 1600-fold selectivity. Cathepsin K-IN-9 has excellent safety and metabolic stability.Cathepsin K-IN-9 can be used for the research of osteoporosis.

SARS-CoV-2-IN-77 (compound 11e) is a cathepsin L and cathepsin S inhibitor with K_i values of 111 nM and 103 nM, respectively. SARS-CoV-2-IN-77 inhibits SARS-CoV-2 with an EC₅₀ value of 38.4 nM in Calu-3 cells without showing cytotoxicity.

Cathepsin G Inhibitor I (Standard) is the analytical standard of Cathepsin G Inhibitor I (HY-103351). This product is intended for research and analytical applications. Cathepsin G Inhibitor I (compound 7) is an effective, selective, reversible, competitive, non-peptide cathepsin G inhibitor (IC₅₀=53 nM; Ki=63 nM).

MPI8 (TG0205221) is an inhibitor of the major protease of SARS-CoV-2 (MPro) with high antiviral activity. MPI8 exerts its antiviral effect by dual and selective inhibition of SARS-CoV-2 MPro and host cell cysteine protease L (cathepsin L). MPI8 can be used in clinical studies of COVID-19.

(Rac)-Z-FA-FMK is the racemate of Z-FA-FMK. (Rac)-Z-FA-FMK is an inhibitor of cathepsin B with a K_i of 1.5 μM. (Rac)-Z-FA-FMK inhibits caspase-2, -3, -6, -7, and -9 with IC₅₀s of 6.147, 15.41, 32.45, 9.077, and 110.7 μM. (Rac)-Z-FA-FMK inhibits the main protease of SARS-CoV-2 replication with an IC₅₀ of 11.39 μM. (Rac)-Z-FA-FMK inhibits the increased IL-1β level induced by LPS and NF-κB transactivation in macrophages.

Relacatib (Standard) is the analytical standard of Relacatib (HY-10294). This product is intended for research and analytical applications. Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with K_i values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC₅₀ values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo.

Mpro/Cathepsin L-IN-2 (Compound 1) is a dual irreversible inhibitor of SARS-CoV-2 main protease (M^pro, pIC₅₀=8.61) and human cathepsin L (hCTSL, pIC₅₀=7.64). Mpro/Cathepsin L-IN-2 is promising for research of COVID-19 and other coronavirus infections.

L-006235 (Standard) is the analytical standard of L-006235. This product is intended for research and analytical applications. L-006235 (L-235) is a potent, selective, reversible and orally active inhibitor of cathepsin K, with an IC50 of 5 nM in bone resorption assay. L-006235 shows selectivity for cathepsin K (Ki=0.2 nM) over cathepsin B, cathepsin L, and cathepsin S (Ki=1, 6, and 47 μM, respectively). L-006235 can reduce collagen degradation and prevent bone loss.

BML-244 is a potent cathepsin K inhibitor. BML-244 can be used in the study of rheumatoid arthritis (RA) and periodontitis.

Calpeptin (Standard) is the analytical standard of Calpeptin. This product is intended for research and analytical applications. Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets. Calpeptin is also an inhibitor of cathepsin K.

Aloxistatin (Standard) is the analytical standard of Aloxistatin. This product is intended for research and analytical applications. Aloxistatin (E64d) is a cell-permeable and irreversible broad-spectrum cysteine protease inhibitor. Aloxistatin (E64d) exhibits entry-blocking effect for MERS-CoV.

Petesicatib (Standard) is the analytical standard of Petesicatib (HY-109069). This product is intended for research and analytical applications. Petesicatib (RO5459072; RG-7625) is a cathepsin S inhibitor, used in research of immune diseases.

SARS-CoV-2 3CLpro-IN-34 (Compound 55) is a highly efficient non-covalent inhibitor of the SARS-CoV-2 3CL^pro protease (b. SARS-CoV-2 3CL^pro protease) with an IC₅₀ of 1.9 μM. SARS-CoV-2 3CLpro-IN-34 can inhibit the 3CL^pro protein of SARS-CoV-1, with its IC₅₀ being 3.2 μM, and it shows high selectivity towards host cysteine proteases (such as cathepsins L/K and calpain). SARS-CoV-2 3CLpro-IN-34 exhibits antiviral activity in cells infected with SARS-CoV-2, with its EC₅₀ being 25 μM, and it is not affected by P-gp inhibitors and shows no significant cytotoxicity. SARS-CoV-2 3CLpro-IN-34 can be used for research on SARS-CoV-2 infection.

Cathepsin S-IN-1 (example 1) is a Cathepsin S inhibitor.

MDL 27399 is an inhibitor of human neutrophil cathepsin G (K_i = 7 μM). MDL 27399 can be used for research of inflammatory diseases.