Cysteine Protease

Cysteine Protease製品

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  • Cysteine Protease阻害剤 (23)
  • Cysteine Protease活性剤(1)
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S1013 Bortezomib ボルテゾミブ (Bortezomib (PS-341, LDP-341, MLM341, NSC 681239)) は強力な 20S プロテアソーム (20S proteasome) 阻害剤であり、Ki は 0.6 nM です。正常細胞に比べがん細胞に対してより高い選択性を示します。 ボルテゾミブ (PS-341) は NF-κB を阻害し ERK のリン酸化を誘導することにより、卵巣がんなどの固形腫瘍において カテプシンB (cathepsin B) を抑制し、オートファジー (autophagy) の分解過程を阻害します。
Cell Rep, 2024, 43(2):113769
J Transl Med, 2024, 22(1):208
J Med Chem, 2024, 67(1):572-585
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.
Cancer Sci, 2023, 114(10):4089-4100
Cancer Sci, 2023, 10.1111/cas.15915
Braz J Med Biol Res, 2023, 55:e12206
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%.
Anim Nutr, 2024, 20:16:409-421.
Cell, 2023, 186(4):850-863.e16
BMC Vet Res, 2023, 19(1):60
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.
Nat Commun, 2023, 14(1):4066
Acta Pharm Sin B, 2022, 12(6):2869-2886
Theranostics, 2022, 12(14):6395-6408
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.
J Clin Invest, 2023, 133(15)e166954
J Med Virol, 2023, 95(12):e29280
Front Immunol, 2023, 14:1207121
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.
Anim Nutr, 2024, 20:16:409-421.
Int J Mol Sci, 2023, 24(2)1667
Biosensors (Basel), 2023, 13(7)682
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.
Proc Natl Acad Sci U S A, 2023, 120(43):e2304288120
Proc Natl Acad Sci U S A, 2023, 120(43):e2304288120
EMBO Rep, 2023, e55069.
S3025 PMSF PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor.
Cell Biosci, 2023, 13(1):9
Cell Mol Immunol, 2022, 19(10):1153-1167
EMBO J, 2022, 10.15252/embj.2021109102
S1115 Odanacatib Odanacatib 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.
Commun Biol, 2022, 5(1):962
Carbohydr Polym, 2021, 253:117261
Cancer Res, 2021, canres.3251.2020
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.
Exp Hematol Oncol, 2023, 12(1):77
Exp Hematol Oncol, 2023, 12(1):77
Comput Struct Biotechnol J, 2022, 20:2442-2454
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.
Cancer Cell, 2022, 40(9):1044-1059.e8
Molecules, 2022, 27(6)1755
Nat Nanotechnol, 2021, 10.1038/s41565-021-00988-z
S7391 Z-FA-FMK Z-FA-FMK ((1S)-Z-FA-FMK) is an irreversible cysteine protease inhibitor, and also inhibits effector caspases.
Cancer Res, 2022, can.21.4222
Comput Struct Biotechnol J, 2022, 20:2442-2454
Sci Transl Med, 2021, 13(604)eabb1069
S3692 NEM (N-Ethylmaleimide) NEM (N-Ethylmaleimide) 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 Med, 2023, 10.1016/j.xcrm.2023.101286
Int J Mol Sci, 2023, 25(1)423
Breast Cancer Res Treat, 2023, 200(1):151-162
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.
Phytomedicine, 2024, 125:155250
Life Sci, 2023, 329:121972
Front Cell Neurosci, 2023, 17:1199656
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.
Elife, 2023, 12e79144
EMBO J, 2020, 39(1):e102030
Arterioscler Thromb Vasc Biol, 2020, ATVBAHA120315151
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
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.
Int J Biol Sci, 2022, 18(13):5207-5220
Microorganisms, 2022, 10(7)1421
mBio, 2018, 9(5)
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
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.
E2886 LY3000328 LY 3000328 (Z-FL-COCHO, Compound 5) is a potent and selective Cathepsin S (Cat S) inhibitor with IC50s of 7.7 and 1.67 nM for human Cat S and mouse Cat S, respectively.
E2899New MG132 SSS MG132 SSS(Z-Leu-Leu-Leu-al, MG132) is a potent proteasome and calpain inhibitor with IC50 of 100 nM and 1.2 μM, respectively.
S0194 Balicatib Balicatib (AAE-581) is a potent and selective inhibitor of the osteoclastic enzyme cathepsin K.
S5611 2-cyano-Pyrimidine 2-cyano-Pyrimidine is a cathepsin K inhibitor with an IC50 of 170 nM.
E4453New Cathepsin G Inhibitor I Cathepsin G Inhibitor I exhibits reversible, competitive cathepsin G inhibition with IC50 and Ki values of 53 nM and 63 nM respectively. It can be used in antigen-processing studies and for modulation of T cell response in situ and in vivo.
S1013 Bortezomib ボルテゾミブ (Bortezomib (PS-341, LDP-341, MLM341, NSC 681239)) は強力な 20S プロテアソーム (20S proteasome) 阻害剤であり、Ki は 0.6 nM です。正常細胞に比べがん細胞に対してより高い選択性を示します。 ボルテゾミブ (PS-341) は NF-κB を阻害し ERK のリン酸化を誘導することにより、卵巣がんなどの固形腫瘍において カテプシンB (cathepsin B) を抑制し、オートファジー (autophagy) の分解過程を阻害します。
Cell Rep, 2024, 43(2):113769
J Transl Med, 2024, 22(1):208
J Med Chem, 2024, 67(1):572-585
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%.
Anim Nutr, 2024, 20:16:409-421.
Cell, 2023, 186(4):850-863.e16
BMC Vet Res, 2023, 19(1):60
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.
Nat Commun, 2023, 14(1):4066
Acta Pharm Sin B, 2022, 12(6):2869-2886
Theranostics, 2022, 12(14):6395-6408
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.
J Clin Invest, 2023, 133(15)e166954
J Med Virol, 2023, 95(12):e29280
Front Immunol, 2023, 14:1207121
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.
Anim Nutr, 2024, 20:16:409-421.
Int J Mol Sci, 2023, 24(2)1667
Biosensors (Basel), 2023, 13(7)682
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.
Proc Natl Acad Sci U S A, 2023, 120(43):e2304288120
Proc Natl Acad Sci U S A, 2023, 120(43):e2304288120
EMBO Rep, 2023, e55069.
S3025 PMSF PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor.
Cell Biosci, 2023, 13(1):9
Cell Mol Immunol, 2022, 19(10):1153-1167
EMBO J, 2022, 10.15252/embj.2021109102
S1115 Odanacatib Odanacatib 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.
Commun Biol, 2022, 5(1):962
Carbohydr Polym, 2021, 253:117261
Cancer Res, 2021, canres.3251.2020
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.
Exp Hematol Oncol, 2023, 12(1):77
Exp Hematol Oncol, 2023, 12(1):77
Comput Struct Biotechnol J, 2022, 20:2442-2454
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.
Cancer Cell, 2022, 40(9):1044-1059.e8
Molecules, 2022, 27(6)1755
Nat Nanotechnol, 2021, 10.1038/s41565-021-00988-z
S7391 Z-FA-FMK Z-FA-FMK ((1S)-Z-FA-FMK) is an irreversible cysteine protease inhibitor, and also inhibits effector caspases.
Cancer Res, 2022, can.21.4222
Comput Struct Biotechnol J, 2022, 20:2442-2454
Sci Transl Med, 2021, 13(604)eabb1069
S3692 NEM (N-Ethylmaleimide) NEM (N-Ethylmaleimide) 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 Med, 2023, 10.1016/j.xcrm.2023.101286
Int J Mol Sci, 2023, 25(1)423
Breast Cancer Res Treat, 2023, 200(1):151-162
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.
Phytomedicine, 2024, 125:155250
Life Sci, 2023, 329:121972
Front Cell Neurosci, 2023, 17:1199656
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.
Elife, 2023, 12e79144
EMBO J, 2020, 39(1):e102030
Arterioscler Thromb Vasc Biol, 2020, ATVBAHA120315151
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
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.
Int J Biol Sci, 2022, 18(13):5207-5220
Microorganisms, 2022, 10(7)1421
mBio, 2018, 9(5)
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
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.
E2886 LY3000328 LY 3000328 (Z-FL-COCHO, Compound 5) is a potent and selective Cathepsin S (Cat S) inhibitor with IC50s of 7.7 and 1.67 nM for human Cat S and mouse Cat S, respectively.
E2899New MG132 SSS MG132 SSS(Z-Leu-Leu-Leu-al, MG132) is a potent proteasome and calpain inhibitor with IC50 of 100 nM and 1.2 μM, respectively.
S0194 Balicatib Balicatib (AAE-581) is a potent and selective inhibitor of the osteoclastic enzyme cathepsin K.
S5611 2-cyano-Pyrimidine 2-cyano-Pyrimidine is a cathepsin K inhibitor with an IC50 of 170 nM.
E4453New Cathepsin G Inhibitor I Cathepsin G Inhibitor I exhibits reversible, competitive cathepsin G inhibition with IC50 and Ki values of 53 nM and 63 nM respectively. It can be used in antigen-processing studies and for modulation of T cell response in situ and in vivo.
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.
Cancer Sci, 2023, 114(10):4089-4100
Cancer Sci, 2023, 10.1111/cas.15915
Braz J Med Biol Res, 2023, 55:e12206
E2899New MG132 SSS MG132 SSS(Z-Leu-Leu-Leu-al, MG132) is a potent proteasome and calpain inhibitor with IC50 of 100 nM and 1.2 μM, respectively.
E4453New Cathepsin G Inhibitor I Cathepsin G Inhibitor I exhibits reversible, competitive cathepsin G inhibition with IC50 and Ki values of 53 nM and 63 nM respectively. It can be used in antigen-processing studies and for modulation of T cell response in situ and in vivo.

Cysteine Protease阻害剤の選択性比較

Tags: Cysteine Protease inhibitor|Cysteine Protease agonist|Cysteine Protease activator|Cysteine Protease inducer|Cysteine Protease antagonist|Cysteine Protease signaling pathway|Cysteine Protease assay kit