S1013 |
Bortezomib
|
Bortezomib 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. |
-
Cell, 2024, 187(18):4905-4925.e24
-
Cell, 2024, S0092-8674(24)00315-5
-
Cell, 2024, S0092-8674(24)00653-6
|
|
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. |
-
Cell Rep Med, 2024, S2666-3791(24)00201-5
-
Biomed Pharmacother, 2024, 180:117468
-
Transl Psychiatry, 2024, 14(1):166
|
|
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%. |
-
Cell Rep Med, 2024, 5(4):101503
-
Anim Nutr, 2024, 20:16:409-421.
-
Cell, 2023, 186(4):850-863.e16
|
|
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. |
-
Transl Psychiatry, 2024, 14(1):166
-
Reprod Biol, 2024, 24(1):100857
-
Res Sq, 2024, rs.3.rs-3979098
|
|
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. |
-
Cell Rep Med, 2024, 5(4):101503
-
Anim Nutr, 2024, 20:16:409-421.
-
Cells, 2024, 13(11)953
|
|
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. |
-
J Atheroscler Thromb, 2024, 10.5551/jat.64579
-
Proc Natl Acad Sci U S A, 2023, 120(43):e2304288120
-
Proc Natl Acad Sci U S A, 2023, 120(43):e2304288120
|
|
S3025 |
PMSF
|
PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor. |
-
Cell Death Discov, 2024, 10(1):171
-
Cell Biosci, 2023, 13(1):9
-
Cell Biosci, 2023, 13(1):9
|
|
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. |
-
Br J Pharmacol, 2024, 10.1111/bph.17312
-
Authorea , 2023,
-
Commun Biol, 2022, 5(1):962
|
|
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.
|
-
Cell Biosci, 2024, 14(1):115
-
Exp Hematol Oncol, 2023, 12(1):77
-
Exp Hematol Oncol, 2023, 12(1):77
|
|
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. |
-
BMC Biol, 2024, 22(1):71
-
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
-
Int J Mol Sci, 2023, 25(1)423
|
|
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
-
Am J Pathol, 2024, S0002-9440(24)00356-0
-
Life Sci, 2023, 329:121972
|
|
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. |
-
Transl Psychiatry, 2024, 14(1):166
-
Int J Biol Sci, 2022, 18(13):5207-5220
-
Microorganisms, 2022, 10(7)1421
|
|
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. |
|
|
A2629 |
Anti-CTSS / Cathepsin S (Fsn0503h)
|
Anti-CTSS / Cathepsin S (Fsn0503h) is an antagonistic monoclonal antibody targeting cathepsin S. It has a potential to inhibit invasion of tumors, and targeting neovascularization in colorectal carcinoma. MW :144.28 KD. |
|
|
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. |
|
|
E2899 |
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
|
Bortezomib 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. |
- Cell, 2024, 187(18):4905-4925.e24
- Cell, 2024, S0092-8674(24)00315-5
- Cell, 2024, S0092-8674(24)00653-6
|
|
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%. |
- Cell Rep Med, 2024, 5(4):101503
- Anim Nutr, 2024, 20:16:409-421.
- Cell, 2023, 186(4):850-863.e16
|
|
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. |
- Transl Psychiatry, 2024, 14(1):166
- Reprod Biol, 2024, 24(1):100857
- Res Sq, 2024, rs.3.rs-3979098
|
|
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. |
- Cell Rep Med, 2024, 5(4):101503
- Anim Nutr, 2024, 20:16:409-421.
- Cells, 2024, 13(11)953
|
|
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. |
- J Atheroscler Thromb, 2024, 10.5551/jat.64579
- Proc Natl Acad Sci U S A, 2023, 120(43):e2304288120
- Proc Natl Acad Sci U S A, 2023, 120(43):e2304288120
|
|
S3025 |
PMSF
|
PMSF (Phenylmethylsulfonyl Fluoride, Benzylsulfonyl fluoride) is an irreversible serine/cysteine protease inhibitor. |
- Cell Death Discov, 2024, 10(1):171
- Cell Biosci, 2023, 13(1):9
- Cell Biosci, 2023, 13(1):9
|
|
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. |
- Br J Pharmacol, 2024, 10.1111/bph.17312
- Authorea , 2023,
- Commun Biol, 2022, 5(1):962
|
|
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.
|
- Cell Biosci, 2024, 14(1):115
- Exp Hematol Oncol, 2023, 12(1):77
- Exp Hematol Oncol, 2023, 12(1):77
|
|
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. |
- BMC Biol, 2024, 22(1):71
- Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
- Int J Mol Sci, 2023, 25(1)423
|
|
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
- Am J Pathol, 2024, S0002-9440(24)00356-0
- Life Sci, 2023, 329:121972
|
|
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. |
- Transl Psychiatry, 2024, 14(1):166
- Int J Biol Sci, 2022, 18(13):5207-5220
- Microorganisms, 2022, 10(7)1421
|
|
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. |
|
|
E2899 |
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. |
|
|