cysteine protease inhibitor

Cysteine protease inhibitors are inhibitors of cysteine proteases. Target: Cysteine Protease

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.

Cysteine Protease inhibitor hydrochloride is a cysteine protease inhibitor.

Cysteine protease inhibitor-3 (Compound 15), a cysteine protease inhibitor, exhibits anti-plasmodial activity by effectively inhibiting Pf3D7 (IC50 = 0.74 μM), PfW2 (IC50 = 1.05 μM), PfFP2 (IC50 = 3.5 μM), and PfFP3 (IC50 = 4.9 μM), demonstrating efficacy against both drug-sensitive and drug-resistant parasites [1].

N-Ethylmaleimide (NEM) is a reagent for alkylation of free sulfhydryl groups, a cysteine protease inhibitor used in experimental biochemistry. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor that specifically inhibits phosphate transport in mitochondria.

CA-074 methyl ester (Cathepsin B Inhibitor IV) is a selective inhibitor of Cathepsin B (IC50=36.3 nM). CA-074 methyl ester has neuroprotective, anti-inflammatory and anti-cancer effects.

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.

LY 3000328 (Cathepsin S inhibitor) is a selective inhibitor of cathepsin S with IC50 values ​​of 7.7 and 1.67 nM for human and mouse cathepsin S, respectively. LY 3000328 (Cathepsin S inhibitor) may slow or prevent abdominal aortic aneurysm (AAA) expansion and/or reduce the risk of AAA rupture by inhibiting cathepsin S-mediated degradation of extracellular matrix proteins, elastin and collagen.

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.

K777 is a potent, orally active, and irreversible inhibitor of cysteine protease, functioning as a potent CYP3A4 inhibitor (IC50 = 60 nM) and a selective CCR4 antagonist, which inhibits chemotaxis. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypanosoma cruzi, and cathepsins B and L, targeting cathepsin-mediated cell entry and exhibiting broad-spectrum antiviral activity. It inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.

Calpain Inhibitor XII (Z-L-Nva-CONH-CH2-2-Py) is a selective and potent inhibitor of calpain I, inhibits calpain II and cathepsin B. Calpain Inhibitor XII shows antiviral activity against coronavirus in cell culture.

SARS-CoV-2 Mpro-IN-9 (compound c7), a nonpeptidic, noncovalent inhibitor of SARS-CoV-2 main protease (Mpro), exhibits potent inhibitory action (IC50 = 0.085 μM) and improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. It effectively suppresses viral replication in SARS-CoV-2-infected Vero E6 cells (EC50 = 1.10 μM) and demonstrates low cytotoxicity (CC50 > 50 μM) [1].

(S)-(+)-Ibuprofen (Dexibuprofen) , is a non-steroidal anti-inflammatory drug (NSAID), inhibiting cyclooxygenase (COX).

PMSF (Phenylmethylsulfonyl fluoride) is an irreversible inhibitor of serine/cysteine protease and is often used in the preparation of cell lysates.

Papain, a cysteine protease of the peptidase C1 family, is utilized in the food, pharmaceutical, textile, and cosmetic industries.

Esomeprazole is the S-isomer of omeprazole, inhibits the lysosomal cysteine protease legumain to prevent cancer metastasis. Esomeprazole is a proton pump inhibitors (PPI).

2-Cyanopyrimidine (m-Hydroxyphenylpropionic acid) is inhibitor of cathepsin K(IC50 : 170 nM)

KGP94 is an inhibitor of cysteine protease Cathepsin L(CTSL).

Cathepsin Inhibitor 2 is a potent Cathepsin S inhibitor (Ki: <20 nM).

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.

S130 is a high affinity, selectiveATG4B (a major cysteine protease) inhibitor (IC50 of 3.24 μM).It suppresses autophagy flux.

SID 26681509 is a selective, reversible and competitive human cathepsin L inhibitor (IC50 of 56 nM).

VBY-825 is a reversible inhibitor of cathepsin with high potency against cathepsins B, L, S and V.

BI-1230 is a potent inhibitor of HCV NS3 protease, exhibiting efficacy in the low nanomolar range, and notably suppresses viral replication. This compound demonstrates high selectivity, distinguishing effectively between other serine/cysteine proteases. Additionally, BI-1230 exhibits favorable pharmacokinetic (PK) properties[1].