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Cysteine Protease

Cysteine proteases, also known as thiol proteases, are enzymes that degrade proteins. These proteases share a common catalytic mechanism that involves a nucleophilic cysteine thiol in a catalytic triad or dyad.

  • Leupeptin Hemisulfate
    T6564103476-89-7
    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.
    • $47
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  • LY 3000328
    TQ01161373215-15-6
    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).
    • $97
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  • Papain
    T195039001-73-4
    Papain is a cysteine protease of the peptidase C1 family. Papain is used in food, pharmaceutical, textile, and cosmetic industries.
    • $45
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  • PMSF
    T0789329-98-6
    Phenylmethanesulfonyl fluoride (PMSF (Phenylmethylsulfonyl fluoride)) is an enzyme inhibitor that inactivates IRC-50 arvin, subtilisin, and the fatty acid synthetase complex.
    • $33
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    TargetMol | Citations Cited
  • Acetyl-Calpastatin (184-210)(human) acetate
    TP2056L
    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.
    • $195
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  • MIV-247
    T120511352817-76-5In house
    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.
    • $1,370 TargetMol
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  • MK-0674
    T16089887781-62-6In house
    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.
    • $490 TargetMol
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  • K777
    T15641233277-99-1In house
    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.
    • $78
    In Stock
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  • Cysteine protease inhibitor-2
    T10924612048-23-4In house
    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.
    • $1,520
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  • FMK 9a
    T153031955550-51-2In house
    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.
    • $142
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  • 3,4 Dichloroisocoumarin
    T867751050-59-0
    3,4 Dichloroisocoumarin is a granzyme, cathepsin G, and neutrolphil elastase inhibitor
    • $38
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    TargetMol | Citations Cited
  • E-64
    T603766701-25-5
    E-64 (Proteinase inhibitor E 64) is an irreversible and specific cysteine protease inhibitor. The IC50 of E-64 for papain is 9 nM.
    • $31
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    TargetMol | Citations Cited
  • Aloxistatin
    T604088321-09-9
    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.
    • $36
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    TargetMol | Citations Cited
  • CA-074 methyl ester
    T3420147859-80-1
    CA-074 methyl ester (Cathepsin B Inhibitor IV) is a specific inhibitor of Cathepsin B with neuroprotective, anti-cancer, and anti-inflammatory effects.
    • $54
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  • Calpeptin
    T6432117591-20-5
    Calpeptin is a potent, cell-permeable calpain inhibitor.
    • $30
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    TargetMol | Citations Cited
  • N-Ethylmaleimide
    T3088128-53-0
    N-Ethylmaleimide (NEM) is a sulfhydryl reagent that is widely used in experimental biochemical studies.
    • $39
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    TargetMol | Citations Cited
  • 2-Cyanopyrimidine
    T745114080-23-0
    2-Cyanopyrimidine (m-Hydroxyphenylpropionic acid) is inhibitor of cathepsin K(IC50 : 170 nM)
    • $29
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  • Aureusimine B
    T37753170713-71-0
    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.
    • $148
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  • VBY-825
    T132881310340-58-9
    VBY-825 is a reversible inhibitor of cathepsin with high potency against cathepsins B, L, S and V.
    • $278
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  • Isovalerylcarnitine
    T1938431023-24-2
    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.
    • $80
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  • Z-Lys-OH
    T658682212-75-1
    Z-Lys-OH is a competitive inhibitor of papain, a lysine derivative.
    • $29
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  • Cathepsin X-IN-1
    T608122418577-51-0
    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].
    • $41
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  • E 64c
    T657376684-89-4
    E 64c (EP 475) , a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor.
    • $47
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  • L-006235
    T21616294623-49-7
    L-006235 is a potent and reversible inhibitor of cathepsin K with IC50 of 0.25 nM.
    • $41
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  • Cathepsin Inhibitor 1
    T6015225120-65-0
    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.
    • $41
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  • CA 074
    T21509134448-10-5
    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.
    • $73
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  • MG-101
    T6583110044-82-1
    MG-101 (Calpain inhibitor I) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins.
    • $48
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  • Aurantiamide acetate
    TJS221656121-42-7
    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].
    • $123
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  • (1S,2R)-Alicapistat
    T601502221010-57-5
    (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].
    • $147
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  • 2-Aminoethanethiol
    T108060-23-1
    2-Aminoethanethiol (Cysteamine) is a Cystine Depleting Agent. The mechanism of action of cysteamine is as a Cystine Disulfide Reduction.
    • $45
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  • PD150606
    T3525179528-45-1
    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.
    • $30
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  • ONO-5334
    T16394868273-90-9
    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.
    • $199
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  • KGP94
    T277301131456-28-4
    KGP94 is an inhibitor of cysteine protease Cathepsin L(CTSL).
    • $115
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  • GLPG2451
    T137052055015-61-5
    GLPG2451 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator. It effectively potentiates low temperature rescued F508del CFTR (EC50: 11.1 nM).
    • $297
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  • Odanacatib
    T6035603139-19-1
    Odanacatib is an inhibitor of cathepsin K with potential anti-osteoporotic activity.
    • $45
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  • LHVS
    T11846170111-28-1
    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.
    • $987
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  • S130
    T128191160852-22-1
    S130 is a high affinity, selectiveATG4B (a major cysteine protease) inhibitor (IC50 of 3.24 μM).It suppresses autophagy flux.
    • $297
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  • Z-FA-FMK
    T6738197855-65-5
    Z-FA-FMK can irreversibly inhibit cysteine protease and also inhibit effector caspases.
    • $61
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  • JTE-607
    T27695188791-09-5
    JTE-607 is a cytokine production inhibitor. JTE-607 induces apoptosis accompanied by an increase in p21waf1/cip1 in acute myelogenous leukemia cells.
    • $37
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  • Tacalcitol monohydrate
    T1391193129-94-3
    Tacalcitol monohydrate(Curatoderm monohydrate), a vitamin D3 analog that promotes bone development by regulating calcium ions, can be used to study psoriasis.
    • $113
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  • Petesicatib
    T164741252637-35-6
    Petesicatib (RG 7625) is a small molecule histone-S (Cat-S) inhibitor for the study of primary dry syndrome and autoimmune diseases.
    • $129
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  • LV-320
    T118962449093-46-1
    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].
    • $1,430
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  • (S)-(+)-Ibuprofen
    T044851146-56-6
    (S)-(+)-Ibuprofen (Dexibuprofen) , is a non-steroidal anti-inflammatory drug (NSAID), inhibiting cyclooxygenase (COX).
    • $37
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  • SID 26681509
    T12909958772-66-2
    SID 26681509 is a selective, reversible and competitive human cathepsin L inhibitor (IC50 of 56 nM).
    • $60
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  • Cathepsin Inhibitor 2
    T115541017931-53-1
    Cathepsin Inhibitor 2 is a potent Cathepsin S inhibitor (Ki: <20 nM).
    • $1,970
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  • Balicatib
    T1850354813-19-7
    Balicatib (AAE581) is a potent and selective inhibitor of cathepsin K, used in trials studying the treatment of osteoporosis.
    • $35
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  • NSC 185058
    T521139122-38-8
    NSC 185058 is an inhibitor of ATG4B, a major cysteine protease. It also can attenuate the autophagic activity.
    • $60
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  • PD 151746
    T2493179461-52-0
    PD151746 is a calpain inhibitor with a 20-fold selectivity for u-calpain (Ki = 0.26 ± 0.03 μM) over m-calpain (Ki = 5.33 ± 0.77 μM). Its IC50 values are 0.26 ± 0.03 μM (Ki for μ-calpain) and 5.33 ± 0.77 μM (Ki for m-calpain) [1]. In vitro, PD151746 targets calpain and reduces oxLDL-induced cytotoxicity [2].
    • $59
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  • (Rac)-Z-Phe-Phe-FMK
    T38469108005-94-3
    (Rac)-Z-Phe-Phe-FMK (Cathepsin L-IN-2) is a cathepsin L inhibitor that inhibits the tendency of β-amyloid to induce apoptotic changes .
    • $199
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  • (RS)-Butyryltimolol
    T134392320274-78-8
    (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].
    • $61
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