cathepsin-b

CA-074 methyl ester (Cathepsin B Inhibitor IV) is a selective inhibitor of Cathepsin B (IC50=36.3 nM). CA-074 methyl ester has neuroprotective, anti-inflammatory and anti-cancer effects.

MK-0674 is an orally available, selective and potent cathepsin K inhibitor (IC50: 0.4 nM) that inhibits Cat B, Cat F, Cat L, and Cat S. It can be used in metabolism-related diseases.

L-873724 inhibits bone resorption. L-873724 is an effective, selective, and reversible non-basic cathepsin K inhibitor (IC50s: 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively). L-873724 also shows an IC50 of

CA 074 is a potent inhibitor of cathepsin B with a Ki value of 2 to 5 nM.CA 074 inhibits ischemic hippocampal neuronal death in primates and attenuates retinopathy and optic neuritis in experimental autoimmune encephalomyelitis induced by SJL/J mice.

Cathepsin B is a cysteine protease located within the subcellular endosomes and lysosomal compartments that mediates apoptosis and can be used in cancer research.

Aurantiamide acetate (Asperglaucide) was isolated from the fermentation broth of Aspergillus penicilloides for the first time. Aurantiamide acetate is a selective and orally active cathepsin inhibitor. Aurantiamide acetate has anti-inflammatory activities and can be used for the study of inflammatory diseases[1][2].

Balicatib (AAE581) is a potent and selective inhibitor of cathepsin K, used in trials studying the treatment of osteoporosis.

FGA145 is a dual inhibitor of Mpro and human Cathepsin L, with Ki values of 3.71 μM for Mal-Mpro, 9.82 μM for pET21-Mpro, and 53 nM for Cathepsin L. Additionally, FGA145 exhibits multi-target antiviral activity.

AM 4299 B is a novel inhibitor of a thiol protease.

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.

NAAA-IN-2 (Compound 9), a potent and selective inhibitor of NAAA, exhibits an IC50 of 50 nM. NAAA, a cysteine amidase, primarily breaks down the endogenous biolipids palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). This compound demonstrates promise for inflammation and pain research [1].

SPR38, a potent inhibitor of the SARS-CoV-2 main protease, exhibits a Ki value of 0.260 μM. Additionally, it effectively inhibits human cathepsin L (hCatL) and human cathepsin B (hCatB), displaying Ki values of 1.92 μM and 11.1 μM, respectively.

Ac-Leu-Val-Lys-Aldehyde is a potent inhibitor of cathepsin B, with an inhibitory concentration (IC50) of 4 nM. It significantly reduces quinolinic acid-induced cell death in the striatum and results in the accumulation of LC3-II [1].

Leupeptin hemisulfate is a protease inhibitor with cell membrane-permeable, reversible, competitive, and oral activities. Leupeptin hemisulfate inhibits the activity of Cathepsin B, Cathepsin H, and Cathepsin L, and blocks fusion of amphipathic lysosomes. Leupeptin hemisulfate also has anti-inflammatory activity.

Cysteine protease inhibitor 2 is a cysteine protease inhibitor. Cysteine protease inhibitor 2 inhibited DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.

K777 is a potent, orally active, and irreversible inhibitor of cysteine protease, functioning as a potent CYP3A4 inhibitor (IC50 = 60 nM) and a selective CCR4 antagonist, which inhibits chemotaxis. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypanosoma cruzi, and cathepsins B and L, targeting cathepsin-mediated cell entry and exhibiting broad-spectrum antiviral activity. It inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.

Calpain Inhibitor XII (Z-L-Nva-CONH-CH2-2-Py) is a selective and potent inhibitor of calpain I, inhibits calpain II and cathepsin B. Calpain Inhibitor XII shows antiviral activity against coronavirus in cell culture.

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

β-Secretase Inhibitor IV is a potent, cell-active inhibitor of BACE-1, with IC50 values of 15.6 nM and 16.3 nM at BACE-1 concentrations of 2 nM and 100 pM, respectively.

DBCO-NHCO-PEG4-NHS ester ester is a MMP-2- and cathepsin B- (CatB) cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

Compound 3 (diABZI-V/C-DBCO) functions as an efficient STING agonist. This compound acts by releasing diABZI-amine under the action of cathepsin B to activate STING, thereby inducing the production of interferon and other immune-activating molecules, which enhances the immune system's response to tumors. In THP1-Dual cells, the EC50 values for STING activation by diABZI-V/C-DBCO and diABZI-amine are 1.47 nM and 0.144 nM, respectively, and in primary mouse splenic cells, the EC50 values are 7.7 µM and 0.17 µM, respectively. diABZI-V/C-DBCO is useful for research in the field of cancer immunotherapy.

SARS-CoV-2 Mpro-IN-31 (Compound 18) is an inhibitor of SARS-CoV-2 MPro with an IC50 of 11 nM. Additionally, this compound effectively inhibits the enzymatic activity of the cysteine proteases cathepsin B and cathepsin L, with IC50 values of 24 nM and 1.8 nM, respectively.

TB-9, a derivative of Tasiamide B, is a potent inhibitor of protease D (cathepsin D), protease E (cathepsin E), and BACE1, with IC50 values of 0.0783 nM, 0.724 nM, and 54.2 nM, respectively.

Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) is an active molecular conjugate used in antibody-drug conjugates (ADCs), consisting of the ADC linker Mal-N(Me)-C6-N(Me) and the potent cytotoxin PNU-159682. This compound selectively delivers its payload to cells expressing CD46 and releases PNU-159682 through cathepsin B cleavage of the linker, inducing DNA damage and apoptosis. Mal-N(Me)-C6-N(Me)-PNU-159682 has demonstrated sustained tumor regression in patient-derived xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC).