Cysteine Protease

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.

LY 3000328 (Cathepsin S inhibitor) is a potent, highly selective Cathepsin S (Cat S) inhibitor (IC50s: 7.7 and 1.67 nM for hCat S and mCat S).

Papain is a cysteine protease of the peptidase C1 family. Papain is used in food, pharmaceutical, textile, and cosmetic industries.

Phenylmethanesulfonyl fluoride (PMSF (Phenylmethylsulfonyl fluoride)) is an enzyme inhibitor that inactivates IRC-50 arvin, subtilisin, and the fatty acid synthetase complex.

Acetyl-Calpastatin (184-210)(human) acetate is a potent, selective and reversible calpain inhibitor with Ki values of 0.2 nM and 6 μM for µ-calpain and cathepsin L, respectively.

MIV-247 is a selective and potent inhibitor of cathepsin S (Kis 2.1, 4.2, and 7.5 nM for human, mouse, and wild monkey cathepsin S, respectively), which attenuates mechanical anomalies in preclinical models of neuropathic pain, and can be used to study cardiac muscle injury.

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.

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

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.

FMK 9a is an irreversible inhibitor of ATG4B with IC50 values of 80 and 73 nM in the TR-FRET and cellular-based LRA assays.

E-64 (Proteinase inhibitor E 64) is an irreversible and specific cysteine protease inhibitor. The IC50 of E-64 for papain is 9 nM.

3,4 Dichloroisocoumarin is a granzyme, cathepsin G, and neutrolphil elastase inhibitor

Calpeptin is a potent, cell-permeable calpain inhibitor.

L-006235 is a potent and reversible inhibitor of cathepsin K with IC50 of 0.25 nM.

PD150606 is a selective nonpeptide calpain inhibitor with neuroprotective activity that inhibits μ-calpains and m-calpains. Inhibits erythrocyanine-induced Ca2+ efflux and interferes with excitotoxicity-dependent motor neuron death.

ONO-5334 is a selective, orally active and potent histone K inhibitor with anti-SAR-COV-2 and anti-bone resorption activity for the study of osteoporosis.

JTE-607 is a cytokine production inhibitor. JTE-607 induces apoptosis accompanied by an increase in p21waf1/cip1 in acute myelogenous leukemia cells.

2-Cyanopyrimidine (m-Hydroxyphenylpropionic acid) is inhibitor of cathepsin K(IC50 : 170 nM)

Tacalcitol monohydrate(Curatoderm monohydrate), a vitamin D3 analog that promotes bone development by regulating calcium ions, can be used to study psoriasis.

Aureusimine B, also known as phevalin, is a natural pyrazinone produced by certain fungi and by Staphylococcus spp., including S. aureus. Its synthesis appears to be initiated by a conserved nonribosomal peptide synthetase that creates a dipeptide (phenylalanine-valine) aldehyde, which then undergoes cyclization and oxidation. Aureusimine B inhibits calpain in a casein hydrolysis assay (IC50 = 1.3 μM), contributes to S. aureus infection in mice, and alters human keratinocyte gene expression.

Dazcapistat is a potent calpain inhibitor, with IC50s of <3 μM for calpain 1, calpain 2 and calpain 9, respectively.

E 64c (EP 475) , a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor.

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.

Aloxistatin (E64d) is an inhibitor of cysteine protease with blood platelet aggregation inhibiting activity. Aloxistatin is an irreversible, membrane-permeable inhibitor of lysosomal and cytosolic cysteine proteases with the ability to inhibit calpain activity in intact platelets.

Cathepsin X-IN-1 (compound 25) reduces the migration of PC-3 cell with low cytotoxic that is a potent inhibitor of Cathepsin X (IC 50 = 7.13 μM) [1].

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

Isovalerylcarnitine (3-methylbutyrylcarnitine) is a small molecule compound produced by the catabolism of L-leucine and the accumulation of isovaleric acid. Isovalerylcarnitine is also a selective and effective calpain activator that can promote cell apoptosis. Isovalerylcarnitine is related to isovaleric acidemia and can be used as a marker of isovaleric acidemia.

Z-Lys-OH is a competitive inhibitor of papain, a lysine derivative.

CA-074 methyl ester (Cathepsin B Inhibitor IV) is a specific inhibitor of Cathepsin B with neuroprotective, anti-cancer, and anti-inflammatory effects.

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.

MG-101 (Calpain inhibitor I) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins.

(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is a highly efficient, orally active compound that selectively inhibits human calpains 1 and 2, with promising implications for Alzheimer's disease (AD) therapy [1]. This compound effectively addresses the metabolic liability associated with carbonyl reduction, while demonstrating potent inhibition of calpain 1 with an IC50 value of 395 nM [2].

N-Ethylmaleimide (NEM) is a sulfhydryl reagent that is widely used in experimental biochemical studies.

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].

2-Aminoethanethiol (Cysteamine) is a Cystine Depleting Agent. The mechanism of action of cysteamine is as a Cystine Disulfide Reduction.

Petesicatib (RG 7625) is a small molecule histone-S (Cat-S) inhibitor for the study of primary dry syndrome and autoimmune diseases.

GLPG2451 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator. It effectively potentiates low temperature rescued F508del CFTR (EC50: 11.1 nM).

S130 is a high affinity, selectiveATG4B (a major cysteine protease) inhibitor (IC50 of 3.24 μM).It suppresses autophagy flux.

LHVS effectively blocks T. gondii microneme protein secretion (IC50=10 μM), gliding motility, and cell invasion. LHVS is a potent, non-selective cysteine protease inhibitor.

Z-FA-FMK can irreversibly inhibit cysteine protease and also inhibit effector caspases.

KGP94 is an inhibitor of cysteine protease Cathepsin L(CTSL).

Odanacatib is an inhibitor of cathepsin K with potential anti-osteoporotic activity.

NSC 185058 is an inhibitor of ATG4B, a major cysteine protease. It also can attenuate the autophagic activity.

LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC 50 of 24.5 μM and a K d of 16 μM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo. These findings suggest that LV-320 will serve as a relevant chemical tool to study the various roles of ATG4B in cancer and other contexts [1].

Cathepsin Inhibitor 2 is a potent Cathepsin S inhibitor (Ki: <20 nM).

SID 26681509 is a selective, reversible and competitive human cathepsin L inhibitor (IC50 of 56 nM).

(S)-(+)-Ibuprofen (Dexibuprofen) , is a non-steroidal anti-inflammatory drug (NSAID), inhibiting cyclooxygenase (COX).

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

(RS)-Butyryltimolol is the racemate of Butyryltimolol. Butyryltimolol is an effective prodrug of Timolol that improves the corneal penetration of Timolol [1]. Butyryltimolol is a β-adrenergic blocker [2].

MDL-28170 (Calpain Inhibitor III) is a Cysteine protease.