Home > Inhibitors & Agonists > Metabolic Enzyme/Protease > Cathepsin
Cat. No. Product name CAS No.
DC7371 Balicatib Featured

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.

354813-19-7
DC7697 CA-074-Me Featured

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

147859-80-1
DCAPI1119 Cathepsin Inhibitor 1

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.

225120-65-0
DC8485 E-64d(Aloxistatin) Featured

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)

88321-09-9
DC7934 L-006,235 Featured

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

294623-49-7
DC8688 Leupeptin hemisulfate Featured

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.

103476-89-7
DC6401 Odanacatib (MK 0822) Featured

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.

603139-19-1
DC11907 Petesicatib

1252637-35-6
DC28138 JPM-OEt

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.

262381-84-0
DC28152 SID 26681509 Featured

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.

958772-66-2
DC28396 K777

K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively.

233277-99-1
DC29008 Cysteine protease inhibitor-2

Cysteine protease inhibitor-2 is a cysteine protease inhibitor extracted from patent US20070032499A1, compound 12. Cysteine protease inhibitor-2 inhibits the cells growth of DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.

612048-23-4
DC40098 Z-LVG-CHN2

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.

119670-30-3
DC41091 VBY-825

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

1310340-58-9
DC42000 Cathepsin D and E FRET Substrate

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.

839730-93-7
DC42335 SID 26681509 quarterhydrate

SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective of human cathepsin L with an IC50 of 56 nM. SID 26681509 quarterhydrate 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 quarterhydrate shows noy activity against cathepsin G.

DC46395 Z-FY-CHO Featured

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

167498-29-5
DC46978 Cathepsin D and E FRET Substrate acetate

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.

DC47708 Cathepsin L-IN-2

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

108005-94-3
DC47709 ABP 25

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

DC48795 GSK-2793660

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

DC49733 Cathepsin K inhibitor 2

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).

2672478-52-1
DC49734 Cathepsin G Inhibitor I

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

429676-93-7
DC70084 GSK 2793660

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..

1613458-79-9
DC70248 BI-1124

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.

752237-69-7
DC70249 BI-1915

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).

752237-67-5
DC70524 JNJ-39641160

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.

1049809-89-3
DC70741 RO-5459072

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.

DC70927 Z-Arg-Lys-AOMK

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.

DC71381 Gü1303

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.

1043922-53-7
DC71382 Gü2602

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.

1627094-88-5
DC72665 ASPER-29

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.

2630388-03-1
DC73718 Dutacatib

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.

501000-36-8
DC73719 MK-1256

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.

919109-76-5
DC73720 Z-Tyr-Ala-CHN2

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

114515-99-0
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