Cathepsin G Inhibitor I is a potent, selective, reversible, competitive, non-peptide inhibitor of cathepsin G.

GSK 2793660(GSK2793660) is a potent, selective, irreversible and orally bioavailable cathepsin C inhibitor, but not the activity of downstream neutrophil serine proteases, for the treatment of cystic fibrosis, non-cystic fibrosis bronchiectasis, ANCA-associated vasculitis and bronchiectasis..

BI-1124 (BI 1124) is a highly potent, selective inhibitor of Cathepsin S (CatS) with IC50 of 7 nM, >40-fold selectivity over Cathepsin L/K/B; BI-1124 had a superior PK profile and showed dose-dependent inhibition of the ovalbumin induced IL-2 secretion in a T cell receptor transgenic DO11 mouse model with an IC50 of 0.3 mg/kg.

BI-1915 (BI 1915) is a highly potent, selective inhibitor of Cathepsin S (CatS) with IC50 of 17 nM for in vitro use, no significant inhibition on Cathepsin L/K/B (IC50>10 uM); BI-1915 effectively blocks the specific ovalbumin induced IL-2 secretion in T-cells with an EC50 value of 2.8 nM. BI-1915 shows excellent selectivity against related cathepsins with IC50 values of >10 µM (Cat K and Cat B) and >30 µM (Cat L).

JNJ-39641160 (JNJ39641160) is a peripherally restricted, non-covalent, potent, selective, orally-available Cathepsin S (CatS) inhibitor with Ki of 38 nM (hCatS).JNJ-39641160 maintains a high selectivity against other closely related cysteine proteases including cathepsins B, C, F, V (L2), K, Z, C, or legumain and the aspartic proteases such as cathepsins E or D.JNJ-39641160 showed similar potency against human and monkey CatS enzymes, and it exhibited less, albeit significant, activity against mouse and dog CatS enzymes (Ki=160-207 nM).JNJ-39641160 is only weakly active against rat cathepsin S (Ki=9.6 uM). JNJ-39641160 induced accumulation of the p10Ii with an average IC50 of 294 ± 28 nM, showed similar potency in purified human PBMC with IC50 of 327 nM.JNJ-39641160 dose-dependently blocked the proteolysis of the invariant chain, and inhibited both T-cell activation and antibody production to a vaccine antigen in C57BL/6 mice.JNJ-39641160 fully reversed tactile allodynia in wild-type mice but was completely ineffective in the same model in CatS knockout mice.

RO 5459072 (RG-7625) is a potent, highly selective of cathepsin S with IC50 of 0.1 nM and 0.3 nM for human and murine Cathepsin S, respectively; shows no sub-micro molar inhibition against others cathepsins (Cat L, B, K, and F) with the exception of Cat V (IC50=700  nM); dose-dependently reverses aberrant systemic autoimmunity, e.g. plasma cytokines, activation of myeloid cells and hypergammaglobulinemia, especially suppresses IgG autoantibody production.

Z-Arg-Lys-AOMK is a potent, selective, irreversible neutral pH 7.2 inhibitor of Cathepsin B with IC50 of 13 nM, >100-fold higher potent than at pH 4.6 (IC50=1,830 nM). Z-Arg-Lys-AOMK displayed high specificity for cathepsin B compared to other lysosomal cysteine cathepsins. Z-Arg-Lys-AOMK selectively inhibits cathepsin B cleavage of peptides at neutral cytosolic pH compared to acidic lysosomal pH conditions. Z-Arg-Lys-AOMK completely inhibited cathepsin B in human neuroblastoma cell lysates at 1 uM. Z-Arg-Lys-AOMK is cell permeable and inhibits intracellular cathepsin B.

Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a Ki of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen.

Gü2602 is a potent, reversible cathepsin K (CatK) inhibitor with a Ki of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsin K zymogen.

ASPER-29 is Asperphenamate 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.

Dutacatib (AFG495) is potent, selective and non-covalent cathepsin K inhibitor with IC50 of 3-6 nM (human CatK), shows excellent selectivity profile versus human cathepsins L and S.

MK-1256 (MK1256) is a potent, selective cathepsin K (Cat K) inhibitor with IC50 of 0.62 nM, >1100-fold selectivity over Cat B, L, S, C, H, Z, and V, 110-fold over Cat F.

Z-Tyr-Ala-CHN2 is a potent cathepsin L inhibitor with EC50 of <50 nM, has broad-spectrum coronavirus antiviral activity.