matrix metalloproteinase-12 (mmp-12)

PF-00356231 hydrochloride is an inhibitor of matrix metalloproteinase MMP-12 with IC50 of 1.4 μM.

ARP-100 (MMP-2 Inhibitor III) is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC50=12 nM). ARP-100 interacts with the S1' pocket of MMP-2 and exhibits anti-invasive properties in an in vitro invasion Matrigel model. ARP-100 has low inhibitory activity against MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM) and MMP-9 (0.2 μM)[1][2].

MMP-9-IN-12 is an inhibitor of matrix metalloproteinase-9 (MMP-9) with an IC50 value of 6.57 μM. It demonstrates an IC50 of 1.54 μM in HCT-116 cells and can induce apoptosis, reactive oxygen species (ROS) generation, and mitochondrial depolarization. Additionally, MMP-9-IN-12 inhibits cell migration and disrupts cell cycle progression, making it useful for colorectal cancer (CRC) research.

MMP2-IN-2 (compound 42) is a potent and selective inhibitor of MMP-2 (matrix metalloproteinases) with an IC50 of 4.2 μM, and it also shows inhibitory activity against MMP-13, MMP-9, and MMP-8 with IC50 values of 12, 23.3, and 25 μM, respectively [1].

Aderamastat (FP-025) is an orally active matrix metalloproteinase 12 (MMP-12) inhibitor used for research in allergic asthma, COPD, and pulmonary fibrosis.

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.

Ageladine A dihydrochloride, derived from the marine sponge Agelas nakamurai, serves as a matrix metalloproteinase (MMP) inhibitor with anti-angiogenic properties. It inhibits MMP-2, MMP-1, MMP-8, MMP-9, MMP-12, and MMP-13, with IC50 values of 4.65 μM, 2.79 μM, 907.12 nM, 1.83 μM, 767.57 nM, and 1.09 μM, respectively. As a pH-sensitive membrane-permeable dye, it emits fluorescence in the blue-green range when excited by ultraviolet light, with a maximum absorption peak at 370 nm. Additionally, Ageladine A dihydrochloride is used as a reliable and stable fluorescent pH sensor to detect intracellular pH changes.