| 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. This compound 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.
|
-
J Proteomics, 2026, 322:105536
-
Signal Transduct Target Ther, 2025, 10(1):81
-
Cell Host Microbe, 2025, 33(4):512-528.e7
|
|
| 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.
|
-
Mol Cancer, 2025, 24(1):253
-
Cell Stem Cell, 2025, S1934-5909(25)00330-3
-
NPJ Vaccines, 2025, 10(1):184
|
|
| 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. This compound 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
|
|
| 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. This compound induces cathepsin B activation and autophagy.
|
-
Nucleic Acids Res, 2025, 53(4)gkaf107
-
Commun Biol, 2025, 8(1):1185
-
Sci Rep, 2025, 15(1):35889
|
|
| 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.
|
-
Adv Mater, 2025, e18445.
-
Nat Commun, 2025, 16(1):4069
-
J Adv Res, 2025, S2090-1232(25)00056-6
|
|
| 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. This compound induces oxidative stress and apoptosis in Filarial Parasite.
|
-
Nat Commun, 2025, 16(1):5403
-
Elife, 2025, 14RP104057
-
bioRxiv, 2024, 2024.09.30.615241
|
|
| 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.
|
-
bioRxiv, 2025, 2025.09.08.674976
-
Cell Mol Life Sci, 2024, 81(1):442
-
Elife, 2023, 12e79144
|
|