Cathepsin Inhibitor

CA-074 methyl ester (Standard) is the analytical standard of CA-074 methyl ester (HY-100350). This product is intended for research and analytical applications. CA-074 methyl ester is a specific inhibitor of Cathepsin B, which has potent bioactivities such as neuroprotective, anti-cancer, and anti-inflamatory effects.

Oxocarbazate is an inhibitor of human cathepsin L with the IC₅₀ values of 6.9 nM (human Cathepsin L,0 h) 0.4 nM ((human Cathepsin L,4 h) and 5.07 μM (human cathepsin B), respectively. Oxocarbazate blockes both SARS-CoV (IC₅₀ = 273 nM) and Ebola virus (IC₅₀ = 193 nM) entry into 293T cells.

NCO-700 sulfate is a dual cathepsin B and calcium-activated neutral protease (CANP) inhibitor with IC₅₀ values of 0.8 and 46 μM, respectively. NCO-700 sulfate reduces the degradation of myocardial fibrin by inhibiting protease activity. NCO-700 sulfate also has inhibitory effects on hormone-independent tumor cells, such as prostate cancer cells, and induces apoptosis. NCO-700 sulfate can be used to study myocardial ischemia and refractory hormone-independent tumors.

Z-LVG-CHN2 (Standard) is the analytical standard of Z-LVG-CHN2 (HY-108137). This product is intended for research and analytical applications. Z-LVG-CHN2 is a cell-permeable and irreversible inhibitor of cysteine proteinase. Z-LVG-CHN2 is a tripeptide derivative and mimics part of the human cysteine proteinase-binding center. Z-LVG-CHN2 displays an inhibition on HSV whereas no significant effect on poliovirus replication. Z-LVG-CHN2 effectively blocks SARS-COV-2 replication (EC₅₀=190 nM) via inhibition of SARS-COV-2 3CL pro protease.

NC 2300 (VEL-0230)is a selective and orally active cysteine cathepsin inhibitor with the IC₅₀ values of 284, 34.5, and 186 nM for cathepsin B, K, and S, respectively.NC 2300 can be used for study of diseases involving bone mineral disorders.

K11002 hydrobromide is a cysteine protease inhibitor. K11002 hydrobromide forms a covalent bond with the active site cysteine residue via Michael addition. K11002 hydrobromide inhibits the growth of Trypanosoma brucei. K11002 hydrobromide can be used in the research of African human trypanosomiasis (sleeping sickness).

Odanacatib (Standard) is the analytical standard of Odanacatib (HY-10042). This product is intended for research and analytical applications. Odanacatib (MK-0822) is a potent and selective inhibitor of cathepsin K, with an IC50 of 0.2 nM for human cathepsin K.

EP-459 is a papain inhibitor (IC₅₀=0.4 μg/mL) with no significant inhibitory activity against serine proteases such as trypsin, plasmin, thrombin, and urokinase. The effects of EP-459 are similar to those of E-64C (HY-100227), but differ from the functions of leupeptin and its analogs. EP-459 can serve as a titration reagent for mouse cathepsin L (precursor form/MEP) activity, covalently binding to the cysteine residue at its active site. EP-459 is also a Ca²⁺-dependent active site-directed inhibitor that can inactivate chicken gizzard smooth muscle calpain II, and can be acetylated to generate Ac-Ep-459, which after radiolabeling can be used to prepare [³H]Ac-Ep-459 for calpain active site labeling.

E-64 (Standard) is the analytical standard of E-64 (HY-15282). This product is intended for research and analytical applications. E-64 (Proteinase inhibitor E 64) is a potent irreversible inhibitor against general cysteine proteases with IC₅₀ of 9 nM for papain.

2-Cyanopyrimidine is a potent and non-selective cysteine protease cathepsin K inhibitor with an IC50 of 170 nM. 2-Cyanopyrimidine is used for osteoporos.

CTSLCTSB-IN-1 (compound 212-148) is a bispecific inhibitor of host viral spike cleaver proteins CTSL/CTSB and TMPRSS2 with IC₅₀s of 2.13/64.07 nM and 1.38 μM, respectively. CTSLCTSB-IN-1 blocks two relevant SARS-CoV-2 viral entry pathways by inhibiting the viral spike cleavage and can be applied to anti-SARS-CoV-2 research.

CA-074 (Standard) is the analytical standard of CA-074 (HY-103350). This product is intended for research and analytical applications. CA-074 is a potent inhibitor of cathepsin B with a K_i of 2 to 5 nM.

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.

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.

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.