Proteases/Proteasome

KB-R7785 is a novel ADAM12/MMP inhibitor improving heart function and insulin sensitivity by blocking HB-EGF and TNF-alpha.

MDL 101146 is an orally active neutrophil elastase inhibitor.

O-Benzoyl hydroxylamine exhibits properties as a dipeptidyl peptidase-IV (DPP-IV) inhibitor and demonstrates antidiabetic effects[1].

Neurodegenerative Disorder-Targeting Compound 1 is an inhibitor of calpain [1].

MMP-145 is used as a protease inhibitor.

BMS-189664 is an inhibitor of thrombin.

MMP-7-IN-3 (compound 15) is a potent and selective MMP-7 inhibitor, inhibiting renal fibrosis in a unilateral ureteral obstruction mouse model.

Matrix metalloproteinase-3 (MMP-3), also known as stromelysin-1, is a critical enzyme involved in tissue remodeling and repair through its role in degrading extracellular matrix proteins, facilitating cell migration. This enzyme has been implicated in various physiological processes including vascular remodeling associated with aneurysm formation, wound healing, the progression of atherosclerosis, and tumor initiation. MMP-3 inhibitor VIII, a cell-permeable sulfonamide-based hydroxamic acid, effectively inhibits MMP-3 by binding to its active site (Ki = 23 nM), thus blocking its enzymatic activity. Additionally, this inhibitor has been demonstrated to suppress the activity of mouse macrophage metalloelastase MME/MMP-12, with an IC50 value of 13 nM, highlighting its potential utility in research on tissue remodeling and disease processes involving MMPs.

Ro 31-9790 is a synthetic inhibitor of metalloproteinase (MMP).

Dim16, a dual inhibitor of PCSK9/HMG-CoAR, demonstrates potent activity with an IC50 of 19 nM against PCSK9 and significantly impedes PCSK9-LDLR interaction

Mergetpa, a carboxypeptidase inhibitor, impedes the conversion of kinins and B2 receptor antagonists into metabolites devoid of the C-terminal arginine [1].

HCV-IN-43 (compound 2), an HCV NS5B protein inhibitor, efficiently inhibits HCV virus replication and is utilized in the study of HCV infection [1].

LU-002i is a selective inhibitor targeting the human proteasome subunits β2c and β2i, demonstrating an inhibitory concentration (IC50) of 220 nM for β2i [1].

Beclabuvir (BMS-791325) is an HCV inhibitor targeting NS5B polymerase with sub-28 nM potency for genotypes 1, 3, 4, 5.

Paltimatrectinib (PBI-200) is a tyrosine kinase inhibitor with anticancer activity, and is used in the study of bladder, breast, and colorectal cancers.

Proteasome-IN-5, also known as compound 5, acts as a proteasome inhibitor [1].

M867 is a selective, reversible caspase-3 inhibitor, possessing an IC50 of 1.4 nM and a Ki value of 0.7 nM, demonstrating anti-apoptotic activity [1].

Proteasome β2c/i-IN-1 (compound 37) serves as a selective inhibitor targeting the β2c and β2i subunits of the human proteasome [1].

Reverse transcriptase-IN-1 is a diarylbenzopyrimidine (DABP) analogue and a potent inhibitor of HIV-1 nonnucleoside reverse transcriptase with an IC50of 13.7

MMP3 inhibitor 1 is a potent and highly selective inhibitor of MMP-3 (IC50 of 1 nM).