Cathepsin S Inhibitor

LY 3000328 (Z-FL-COCHO) is a potent and selective Cathepsin S (Cat S) inhibitor with IC₅₀s of 7.7 and 1.67 nM for hCat S and mCat S, respectively.

Balicatib (AAE581) is a potent, orally active and selective cathepsin K inhibitor with IC₅₀ values of 22, 61, 48, 2900 nM for cathepsin K, cathepsin B, cathepsin L, cathepsin S, respectively. Balicatib inhibits bone turnover, decreases bone formation rates. Balicatib has the potential for the research of osteoporosis.

LHVS is a potent, non-selective, irreversible, cell-permeable cysteine protease and cathepsin inhibitor. LHVS decreases actin ring formation. LHVS inhibits T. gondii invasion with an IC₅₀ of 10 μM.

Petesicatib (RO5459072; RG-7625) is a cathepsin S inhibitor, used in research of immune diseases.

Cathepsin-IN-5 is a cathepsin inhibitor with IC₅₀ values of 6.2 μM and 81 nM for cathepsin L and cathepsin S. Cathepsin-IN-5 inhibits cancer cells proliferation, induces apoptosis, reduces growth of hepatocellular tumors in mouse models, and modulates expression of genes linked to cell death, cell proliferation, and cellular processes. Cathepsin-IN-5 can be used for the research of hepatocellular carcinoma.

Cathepsin L-IN-7 is an inhibitor of cathepsin L, cathepsin B and cathepsin S. Cathepsin L-IN-7 has an IC₅₀ of 0.011 μM against cathepsin L and an IC₅₀ of 0.062 μM against cathepsin S, while it shows weak inhibitory activity against cathepsin B. Cathepsin L-IN-7 binds to the active site of cysteine proteases and blocks their proteolytic function. Cathepsin L-IN-7 can be used in research on viral infections and cancer.

BI-1124 is a cathepsin S inhibitor that exhibits simulated sufficient ocular pharmacokinetic-pharmacodynamic coverage in rabbit models via topical ocular administration. BI-1124 can be used for the research of age-related dry eye disease.

VBY-825 is an orally available novel reversible cathepsin inhibitor that has high inhibitory potency against cathepsin B, L, S and V, and possesses anti-tumor, anti-inflammatory and analgesic effects.

Cathepsin Inhibitor 2 is a potent Cathepsin S inhibitor extracted from patent WO2009123623A1, has a K_i of <20 nM.

Cathepsin L/S-IN-1 is a dual inhibitor of Cathepsin L and Cathepsin S with IC₅₀s of 4.10 μM and 1.79 μM, respectively. Cathepsin L/S-IN-1 shows a significant antimetastatic and invasive effects on pancreatic cancer BxPC-3 and PANC-1 cells.

TS-24 is an inhibitor for cathepsin S, with an IC₅₀ of 4.3 μM. TS-24 exhibits radiosensitizing activity in wild type breast cancer susceptibility gene 1 (BRCA1) and in TNBC xenograft mice model, through induction of apoptosis.

MIV-247 is a selective cathepsin S inhibitor with K_is of 2.1, 4.2 and 7.5 nM for human, mouse and cynomolgus monkey cathepsin S, respectively.

Cathepsin Inhibitor 4 (Compound 45) is a selective inhibitor for Cathepsin S with K_i of 0.04 nM.

JNJ 10329670 is a potent and selective noncovalent cathepsin S inhibitor with a K_i value of 34 nM for human cathepsin S. JNJ 10329670 blocks invariant chain proteolysis in B cells and dendritic cells, as well as antigen-induced T cell proliferation.

Cathepsin L-IN-6 (Compound 6a) is a selective cathepsin L inhibitor with an IC₅₀ of 0.021 μM. Cathepsin L-IN-6 suppresses cathepsin L activity by directly binding to cathepsin L. Cathepsin L-IN-6 inhibits IL-6 and IL-8. Cathepsin L-IN-6 shows a high anti-inflammatory activity. Cathepsin L-IN-6 can be used in the research of acute lung injury.

ASPER-29 is Asperphenamate HY-129578 analog. ASPER-29 also is a dual cathepsin L and S inhibitor with IC₅₀ value of 6.03 μM and 5.02 μM, respectively. ASPER-29 can be used for the research of the migration and invasion of cancer.

Alkyne-GRWHPM-CONH-NH-CMK is a covalent Cathepsin S inhibitor (IC₅₀=82 nM). Alkyne-GRWHPM-CONH-NH-CMK has an N-terminal alkyne handle for CuAAC functionalization that engages off-target protein disulfide isomerase PDIA1. Alkyne-GRWHPM-CONH-NH-CMK can be used for the research of autoimmune disorders.

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.