Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively.

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.

Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific cathepsin L (CTSL) inhibitor.

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

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.

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.

Leupeptin hemisulfate is a reversible, competitive serine/cysteine protease inhibitor, which has been shown to inhibit cathepsins B, H, L, and S, calpain, and trypsin. Leupeptin hemisulfate is an orally active, antioxidant and anti-inflammatory agent.

SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G.

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.

Odanacatib (MK 0822) is a potent, selective, and neutral inhibitor of human and rabbit cathepsin K with IC50 of 0.2 nM and 1 nM , respectively.

L 006235 is a reversible and potent cathepsin K inhibitor that displays more than a 4000 fold selectivity over cathepsins B, L and S.

E-64D is an inhibitor of cathepsins B and L; also thought to inhibit calpain,showed a potent activity for COVID-19(SARS-COV-2)with EC50: MERS-COV(1.275),SARS-COV(0.760)

CA-074 Me is a selective and cell-permeable inhibitor of cathepsin B.

Balicatib(AAE-581) is a potent and selective inhibitor of cathepsin K; 10-100-fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S.

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.

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.

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.

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.

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).

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.

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..

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

Cathepsin K inhibitor 2 is a potent inhibitor of cathepsin K. Cathepsin K, Cat K is a cysteine protease expressed under the control of CTSK gene and closely related to osteoporosis, whose main function is to hydrolyze collagen. Cathepsin K inhibitor 2 has the potential for the research of osteoarthfitis (extracted from patent WO2021147882A1, compound 78).

GSK-2793660 is an orally active and irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 can be used for the research of bronchiectasis.

Cathepsin L-IN-2 (Z-Phe-Phe-FMK) is a potent and irreversible cathepsin L and cathepsin B inhibitor.

ABP 25 is an activity-based probe for cathepsin K imaging with excellent potency and selectivity.

Cathepsin D and E FRET Substrate acetate is a fluorogenic substrate for cathepsins D and E and not for B, H or L. The cleavage occurs at the Phe-Phe amide bond resul. Cathepsin D and E FRET Substrate is a valuable tool for routine assays and for mechanistic studies on cathepsins E and D.

Cathepsin D and E FRET Substrate is a fluorogenic substrate for cathepsins D and E and not for B, H or L. The cleavage occurs at the Phe-Phe amide bond resul. Cathepsin D and E FRET Substrate is a valuable tool for routine assays and for mechanistic studies on cathepsins E and D.

VBY-825 is a novel, reversible cathepsin inhibitor with high potency against cathepsins B, L, S and V.

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.