mmp inhibitor i

MMP inhibitor I is a peptide inhibitor of matrix metalloproteinase-1 (MMP-1), MMP-2, and MMP-3 (IC50s = 1.3, 30, and 150 μM, respectively). It is selective for MMP-1, MMP-2, and MMP-3 over the proteases thermolysin, urease, trypsin, α-chymotrypsin, plasmin, and elastase at concentrations up to 4 mM.

MMP-9/MMP-13 Inhibitor I is a dual inhibitor of MMP-9 and MMP-13 with IC50 of 0.9 nM for both enzymes. It is over 20 times more selective for MMP-9/MMP-13 than for other MMPs.

MMP-8 Inhibitor I is a selective inhibitor of the neutrophil collagenase matrix metalloproteinase-8 (MMP-8) with an IC50 value of 4 nM.

ALK5-IN-82 is a potent and selective inhibitor of activin receptor-like kinase 5 (ALK5), demonstrating an IC50 value of 9.1 nM. This compound effectively suppresses the expression of α-smooth muscle actin (α-SMA), collagen I, and the proteinases tissue inhibitor of metalloproteinase 1 (TIMP-1) and matrix metalloproteinase 13 (MMP-13) in human umbilical vein endothelial cells induced by transforming growth factor-β. ALK5-IN-82 shows potential for use in research related to cardiac fibrosis.

MMP-2/MMP-9-IN-1 is a potent, highly selective, and orally bioavailable inhibitor of type IV collagenases [MMP-9 and MMP-2], exhibiting IC50 values of 0.24 μM for MMP-9 and 0.31 μM for MMP-2, which can be used to study cancer.

Picroside I (6'-Cinnamoylcatalpol), a hepatoprotective agent, is reported to be antimicrobial and used against hepatitis B. It has antioxidant, and anti-inflammatory activities, it may be the valuable anti-invasive drug candidates for cancer therapy by suppressing Collagenases and Gelatinases. Picroside I can enhance basic fibroblast growth factor(bFGF)-, staurosporine- or dbc-mitogen-activated protein (MAP)-induced neurite outgrowth from PC12D cells.

MMP-9 Inhibitor I is an inhibitor of matrix metalloproteinase-9 (MMP-9) that is selective over MMP-1 and MMP-13 (IC50s = 5, 1,050, and 113 nM, respectively). MMP-9 Inhibitor I also decreases activity of TNF-α converting enzyme (TACE) in a dose-dependent manner (IC50 = 0.54 μM). MMP-9 Inhibitor I decreases TNF-α secretion stimulated by LPS in BV-2 microglial cells at concentrations of 50 and 100 μM. MMP-9 Inhibitor I is therefore used in neuroinflammatory and extracellular matrix regulation research to investigate metalloproteinase selectivity, cytokine shedding pathways, and microglial activation responses in cellular inflammation models.

(R)-ND-336 is a highly potent and selective MMP-9 inhibitor with a K_i value of 19 nM and also exhibits inhibitory activity against MMP-2 (K_i = 127 nM) and MMP-14 (K_i = 119 nM). With significant potential, (R)-ND-336 is being investigated in diabetic foot ulcers (DFUs) research [1].

Imidapril (TA-6366 free base) is an orally active angiotensin-converting enzyme (ACE) and MMP-9 inhibitor. It impedes the conversion of angiotensin I to angiotensin II, thereby reducing total peripheral resistance and systemic blood pressure. Imidapril has research value in hypertension, type 1 diabetic nephropathy, and chronic heart failure.

Homouridine, an analogue of uridine, functions as an intermediate in the synthesis of MMP-2 inhibitor (compound I, IC50 = 150 μM). Moreover, the derivative of homouridine (compound I) inhibits the interaction of TNF-α with its receptor, TNF-αR1 [1].

SCAL-255 is a mitochondrial complex I (CI) inhibitor, exhibiting potent inhibition with an IC50 of 1.14 μM. It impedes mitochondrial function by blocking oxygen consumption rate (OCR), inducing reactive oxygen species (ROS) production, and diminishing mitochondrial membrane potential (MMP). Furthermore, SCAL-255 significantly hampers the proliferation of cancer cells reliant on oxidative phosphorylation (OXPHOS) [1].

SCAL-266, a potent inhibitor of mitochondrial complex I (CI), exhibits an IC50 of 0.83 μM. This compound impairs mitochondrial function by blocking oxidative phosphorylation (OXPHOS), inhibiting oxygen consumption rate (OCR), increasing reactive oxygen species (ROS) production, and diminishing mitochondrial membrane potential (MMP). Furthermore, SCAL-266 demonstrates significant antiproliferative activity against OXPHOS-dependent cancer cells [1].