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Catalog No. Product Name Information Product Use Citations Product Validations
S0194 Balicatib Balicatib (AAE-581) is a potent and selective inhibitor of the osteoclastic enzyme cathepsin K.
S0722 Cruzain-IN-1 Cruzain-IN-1 is a selective inhibitor of trypanosomal cysteine proteases and a covalent and reversible Cruzain inhibitor with IC50 of 10 nM.
S1013 Bortezomib (PS-341) Bortezomib (PS-341, Velcade, LDP-341, MLM341, NSC 681239) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors.
Mol Cell, 2022, S1097-2765(22)00433-6
Sci Immunol, 2022, 7(68):eabi6763
Sci Adv, 2022, 8(4):eabi7711
S1115 Odanacatib (MK-0822) Odanacatib (MK 0822) is a potent, selective, and neutral inhibitor of cathepsin K (human/rabbit) with IC50 of 0.2 nM/1 nM, and demonstrated high selectivity versus off-target cathepsin B, L, S. Phase 3.
Cancer Res, 2021, canres.3251.2020
Cell Chem Biol, 2021, S2451-9456(21)00213-0
Carbohydr Polym, 2021, 253:117261
S2847 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.
EMBO J, 2020, 39(1):e102030
Arterioscler Thromb Vasc Biol, 2020, ATVBAHA120315151
bioRxiv, 2019, 10.1101/537753
S3012 Pazopanib Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.
NPJ Breast Cancer, 2022, 8(1):44
J Pharmacol Exp Ther, 2022, 380(2):114-125
Birth Defects Res, 2022, 10.1002/bdr2.2001
S3025 PMSF PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor.
EMBO J, 2022, 10.15252/embj.2021109102
Cell Rep, 2022, 39(9):110851
J Exp Clin Cancer Res, 2022, 41(1):149
S3692 N-Ethylmaleimide (NEM) N-Ethylmaleimide (NEM) is an organic compound that is derived from maleic acid. It is an irreversible inhibitor of all cysteine peptidases, with alkylation occurring at the active site thiol group. N-Ethylmaleimide (NEM) inactivates endogenous deubiquitinating enzymes (DUBs). N-Ethylmaleimide (NEM) specifically inhibits phosphate transport in mitochondria.
Cell Rep, 2022, 38(12):110538
Invest Ophthalmol Vis Sci, 2022, 63(4):11
EMBO J, 2021, 40(10):e106632
S4591 Nitroxoline Nitroxoline (8-Hydroxy-5-nitroquinoline, 5-nitroquinolin-8-ol, 5-Nitro-8-quinolinol, 5-Nitro-8-hydroxyquinoline) is a urinary antibacterial agent active against susceptible gram-positive and gram-negative organisms commonly found in urinary tract infections. Nitroxoline impairs tumor progression in vitro and in vivo by inhibiting cathepsin B activity.
mBio, 2018, 9(5)
bioRxiv, 2018, 10.1101/331785
S5611 2-cyano-Pyrimidine 2-cyano-Pyrimidine is a cathepsin K inhibitor with an IC50 of 170 nM.
S7379 E-64 E-64 is an irreversible and selective cysteine protease inhibitor, and also inhibits papain, calpain, and cathepsins B and H, but not serine proteases or aspartic proteases. The IC50 for papain is 9 nM. E-64 induces oxidative stress and apoptosis in Filarial Parasite.
Molecules, 2022, 27(6)1755
Sci Adv, 2021, 7(3)eabc6364
Cell Chem Biol, 2021, S2451-9456(21)00213-0
S7380 Leupeptin Hemisulfate Leupeptin Hemisulfate is a reversible inhibitor of serine and cysteine proteases. It inhibits cathepsin B (Ki = 6 nM), calpain (Ki = 10 nM), trypsin (Ki = 35 nM), plasmin (Ki = 3.4 μM), and kallikrein (Ki = 19 μM), and has no effect against chymotrypsin, elastase, renin, or pepsin.
Cell Rep, 2022, 38(4):110302
Comput Struct Biotechnol J, 2022, 20:2442-2454
Elife, 2021, 10e62394
S7381 Pepstatin A Pepstatin A (Pepstatin) is a potent aspartic protease inhibitor, and also inhibits HIV replication. Pepstatin A is also an inhibitor of cathepsins D and cathepsins E. Pepstatin A inhibits autophagy by suppressing lysosomal proteases.
J Immunother Cancer, 2022, 10(3)e004129
PLoS Pathog, 2022, 18(1):e1010204
Pharmacol Res, 2021, S1043-6618(21)00517-X
S7386 MG-101 (ALLN) MG-101 (ALLN, Calpain inhibitor-1, Ac-LLnL-CHO) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins.
Comput Struct Biotechnol J, 2022, 20:2442-2454
Stem Cells, 2021, 10.1002/stem.3332
Front Cell Dev Biol, 2021, 9:684857
S7391 Z-FA-FMK Z-FA-FMK ((1S)-Z-FA-FMK) is an irreversible cysteine protease inhibitor, and also inhibits effector caspases.
Comput Struct Biotechnol J, 2022, 20:2442-2454
Sci Transl Med, 2021, 13(604)eabb1069
Nat Commun, 2021, 12(1):6786
S7392 Loxistatin Acid (E-64C) Loxistatin Acid (E-64C, NSC 694279, EP 475), a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry.
ACS Chem Biol, 2021, 16(9):1628-1643
Sci Signal, 2018, 11(518)eaao0422
Sci Signal, 2018, 11(518)eaao0422
S7393 Aloxistatin (E64d) Aloxistatin (E64d) is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry, and aloxistatin treatment reduced cellular entry of SARS-CoV-2 pseudovirions by 92.3%.
J Immunother Cancer, 2022, 10(3)e004129
Mol Plant Pathol, 2022, 10.1111/mpp.13192
EMBO J, 2021, e108050
S7394 MDL-28170 MDL-28170 (Calpain Inhibitor III) is a potent and selective calpain inhibitor of calpain that penetrates the blood-brain barrier and inhibits brain cysteine protease activity after systemic administration. MDL-28170 is also an inhibitor of γ-secretase.
S7396 Calpeptin Calpeptin is a potent, cell-permeable calpain inhibitor with ID50 of 52 nM, 34 nM, 138 nM, and 40 nM for Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papainb, and Calpain I (human platelets), respectively. Calpeptin attenuates apoptosis and intracellular inflammatory changes in muscle cells.
Cell Rep, 2022, 39(6):110792
Oxid Med Cell Longev, 2022, 2022:2566917
Comput Struct Biotechnol J, 2022, 20:2442-2454
S7420 CA-074 methyl ester (CA-074 Me) CA-074 methyl ester (CA-074 Me, Cathepsin B Inhibitor IV) is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor.
Cell Rep, 2022, 38(4):110302
J Hazard Mater, 2022, 436:129093
Toxicol Lett, 2022, 357:73-83
S7424 PD 151746 PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 μM for μ-Calpain, about 20-fold selectivity over m-calpain.
PLoS Pathog, 2021, 17(9):e1009889
Cell, 2019, 177(5):1262-1279
Life Sci, 2019, 222:195-202
S0194 Balicatib Balicatib (AAE-581) is a potent and selective inhibitor of the osteoclastic enzyme cathepsin K.
S0722 Cruzain-IN-1 Cruzain-IN-1 is a selective inhibitor of trypanosomal cysteine proteases and a covalent and reversible Cruzain inhibitor with IC50 of 10 nM.
S1013 Bortezomib (PS-341) Bortezomib (PS-341, Velcade, LDP-341, MLM341, NSC 681239) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors.
Mol Cell, 2022, S1097-2765(22)00433-6
Sci Immunol, 2022, 7(68):eabi6763
Sci Adv, 2022, 8(4):eabi7711
S1115 Odanacatib (MK-0822) Odanacatib (MK 0822) is a potent, selective, and neutral inhibitor of cathepsin K (human/rabbit) with IC50 of 0.2 nM/1 nM, and demonstrated high selectivity versus off-target cathepsin B, L, S. Phase 3.
Cancer Res, 2021, canres.3251.2020
Cell Chem Biol, 2021, S2451-9456(21)00213-0
Carbohydr Polym, 2021, 253:117261
S2847 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.
EMBO J, 2020, 39(1):e102030
Arterioscler Thromb Vasc Biol, 2020, ATVBAHA120315151
bioRxiv, 2019, 10.1101/537753
S3012 Pazopanib Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.
NPJ Breast Cancer, 2022, 8(1):44
J Pharmacol Exp Ther, 2022, 380(2):114-125
Birth Defects Res, 2022, 10.1002/bdr2.2001
S3025 PMSF PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor.
EMBO J, 2022, 10.15252/embj.2021109102
Cell Rep, 2022, 39(9):110851
J Exp Clin Cancer Res, 2022, 41(1):149
S3692 N-Ethylmaleimide (NEM) N-Ethylmaleimide (NEM) is an organic compound that is derived from maleic acid. It is an irreversible inhibitor of all cysteine peptidases, with alkylation occurring at the active site thiol group. N-Ethylmaleimide (NEM) inactivates endogenous deubiquitinating enzymes (DUBs). N-Ethylmaleimide (NEM) specifically inhibits phosphate transport in mitochondria.
Cell Rep, 2022, 38(12):110538
Invest Ophthalmol Vis Sci, 2022, 63(4):11
EMBO J, 2021, 40(10):e106632
S4591 Nitroxoline Nitroxoline (8-Hydroxy-5-nitroquinoline, 5-nitroquinolin-8-ol, 5-Nitro-8-quinolinol, 5-Nitro-8-hydroxyquinoline) is a urinary antibacterial agent active against susceptible gram-positive and gram-negative organisms commonly found in urinary tract infections. Nitroxoline impairs tumor progression in vitro and in vivo by inhibiting cathepsin B activity.
mBio, 2018, 9(5)
bioRxiv, 2018, 10.1101/331785
S5611 2-cyano-Pyrimidine 2-cyano-Pyrimidine is a cathepsin K inhibitor with an IC50 of 170 nM.
S7379 E-64 E-64 is an irreversible and selective cysteine protease inhibitor, and also inhibits papain, calpain, and cathepsins B and H, but not serine proteases or aspartic proteases. The IC50 for papain is 9 nM. E-64 induces oxidative stress and apoptosis in Filarial Parasite.
Molecules, 2022, 27(6)1755
Sci Adv, 2021, 7(3)eabc6364
Cell Chem Biol, 2021, S2451-9456(21)00213-0
S7380 Leupeptin Hemisulfate Leupeptin Hemisulfate is a reversible inhibitor of serine and cysteine proteases. It inhibits cathepsin B (Ki = 6 nM), calpain (Ki = 10 nM), trypsin (Ki = 35 nM), plasmin (Ki = 3.4 μM), and kallikrein (Ki = 19 μM), and has no effect against chymotrypsin, elastase, renin, or pepsin.
Cell Rep, 2022, 38(4):110302
Comput Struct Biotechnol J, 2022, 20:2442-2454
Elife, 2021, 10e62394
S7381 Pepstatin A Pepstatin A (Pepstatin) is a potent aspartic protease inhibitor, and also inhibits HIV replication. Pepstatin A is also an inhibitor of cathepsins D and cathepsins E. Pepstatin A inhibits autophagy by suppressing lysosomal proteases.
J Immunother Cancer, 2022, 10(3)e004129
PLoS Pathog, 2022, 18(1):e1010204
Pharmacol Res, 2021, S1043-6618(21)00517-X
S7386 MG-101 (ALLN) MG-101 (ALLN, Calpain inhibitor-1, Ac-LLnL-CHO) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins.
Comput Struct Biotechnol J, 2022, 20:2442-2454
Stem Cells, 2021, 10.1002/stem.3332
Front Cell Dev Biol, 2021, 9:684857
S7391 Z-FA-FMK Z-FA-FMK ((1S)-Z-FA-FMK) is an irreversible cysteine protease inhibitor, and also inhibits effector caspases.
Comput Struct Biotechnol J, 2022, 20:2442-2454
Sci Transl Med, 2021, 13(604)eabb1069
Nat Commun, 2021, 12(1):6786
S7392 Loxistatin Acid (E-64C) Loxistatin Acid (E-64C, NSC 694279, EP 475), a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry.
ACS Chem Biol, 2021, 16(9):1628-1643
Sci Signal, 2018, 11(518)eaao0422
Sci Signal, 2018, 11(518)eaao0422
S7393 Aloxistatin (E64d) Aloxistatin (E64d) is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry, and aloxistatin treatment reduced cellular entry of SARS-CoV-2 pseudovirions by 92.3%.
J Immunother Cancer, 2022, 10(3)e004129
Mol Plant Pathol, 2022, 10.1111/mpp.13192
EMBO J, 2021, e108050
S7394 MDL-28170 MDL-28170 (Calpain Inhibitor III) is a potent and selective calpain inhibitor of calpain that penetrates the blood-brain barrier and inhibits brain cysteine protease activity after systemic administration. MDL-28170 is also an inhibitor of γ-secretase.
S7396 Calpeptin Calpeptin is a potent, cell-permeable calpain inhibitor with ID50 of 52 nM, 34 nM, 138 nM, and 40 nM for Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papainb, and Calpain I (human platelets), respectively. Calpeptin attenuates apoptosis and intracellular inflammatory changes in muscle cells.
Cell Rep, 2022, 39(6):110792
Oxid Med Cell Longev, 2022, 2022:2566917
Comput Struct Biotechnol J, 2022, 20:2442-2454
S7420 CA-074 methyl ester (CA-074 Me) CA-074 methyl ester (CA-074 Me, Cathepsin B Inhibitor IV) is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor.
Cell Rep, 2022, 38(4):110302
J Hazard Mater, 2022, 436:129093
Toxicol Lett, 2022, 357:73-83
S7424 PD 151746 PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 μM for μ-Calpain, about 20-fold selectivity over m-calpain.
PLoS Pathog, 2021, 17(9):e1009889
Cell, 2019, 177(5):1262-1279
Life Sci, 2019, 222:195-202
Tags: Cysteine Protease inhibitor|Cysteine Protease agonist|Cysteine Protease activator|Cysteine Protease inducer|Cysteine Protease antagonist|Cysteine Protease signaling pathway|Cysteine Protease assay kit