Dnp-GPLGMRGL-NH2 is a peptide substrate for matrix metalloproteinase-13 (MMP-13) with a kcat/Km value of 4,200,000 M-1s-1.
Hydrangenol is an orally active antiphotoaging compound. It can be isolated from Hydrangea serrata leaves. Hydrangenol prevents wrinkle formation by reducing MMP and inflammatory cytokine expression and increasing moisturizing factors and antioxidant genes level[1].
Meloxicam sodium is a non-steroidal anti-inflammatory agent, inhibits COX activity, with IC50s of 0.49 µM and 36.6 µM for COX-2 and COX-1, respectively[1].
Doxycycline monohydrate is an antibiotic and broad-spectrum metalloproteinase (MMP) inhibitor[1][2][3][4].
Ilomastat (Galardin; GM6001) is a broad spectrum matrix metalloprotease (MMP) inhibitor, with Ki of 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM, 0.36 nM for MMP-1/2/3/7/8/9/12/14/26, respectively.
SD-2590 hydrochloride is a potent MMP inhibitor with IC50 values of ﹤0.1, ﹤0.1, 0.18, and 1.7 nM for MMP2, MMP13, MMP9, and MMP8, respectively. SD-2590 hydrochloride inhibits dilation of the left ventricle in rats[1].
GPLGIAGQ, a MMP2-cleavable polypeptide, is used as a stimulus-sensitive linker in both liposomal and micellar nanocarriers for MMP2-triggered tumor targeting. GPLGIAGQ can be used to synthesis unique MMP2-targeted photosensitizer in photodynamic therapy (PDT)[1][2][3].
MMP-9-IN-4 is a MMP-9 inhibitor (IC50: 7.46 nM) that has H-π interactions with MMP-9. MMP-9-IN-4 also inhibits AKT activity (IC50: 8.82 nM). MMP-9-IN-4 shows cell cytotoxicity and induces cell apoptosis. MMP-9-IN-4 can be used in the research of cancers[1].
Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells[1]. Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation[2].
MMP-9-IN-1 is a specific matrix metalloproteinase-9 (MMP-9) inhibitor, which selectively target the hemopexin (PEX) domain of MMP-9, but not other MMPs[1].
TNO211 is a biological active peptide. (Matrix Metalloproteinases (MMPs) are a large family of endopeptidases. Collectively, MMPs can degrade all kinds of extracellular matrix proteins, and can also process a number of bioactive molecules. They are known to be involved in the cleavage of cell surface receptors, the release of apoptotic ligands, and chemokine/cytokine inactivation. MMPs are also thought to play a major role in cell behaviors such as cell proliferation, migration (adhesion/dispersion), differentiation, angiogenesis, apoptosis, and host defense.This peptide is a highly soluble fluorogenic MMP substrate for MMP-2, 8, 12, 13 and 14, containing the MMP cleavable Gly-Leu bond and EDANS/DABCYL. Fluorogenic assays using TNO211 are sensitive and can detect MMP activity in culture medium from endothelial cells and untreated synovial fluid from patients. Abs/Em = 340/490 nm.)
BR351 precursor is a precursor of BR351. BR351 is a brain penetrant MMP inhibitor with IC50s of 4, 2, 11, 50 nM for MMP2, MMP8, MMP9 and MMP13, respectively[1]. Potential tools for the molecular imaging of activated MMPs with PET[2].
CTTHWGFTLC, CYCLIC is a cyclic peptide inhibitor for matrix metalloproteinases MMP-2 and MMP-9[1].
MMP13-IN-31f is a highly potent, selective, orally bioavailable MMP-13 inhibitor with IC50 of 0.036 nM; exhibits 5,000-fold selectivity for MMP-13 over MMP-2, >1,500-fold selectivity over MMP-10, and >27,000-fold selectivity over MMP-1, 3, 7, 8, 9, 14, and TACE; prevents IL-1/OSM induced in vitro degradation of BNC (70.8% inhibition of cartilage degradation at 1 µM).
Isoginkgetin is a MMP-9 inhibitor, also a Pre-mRNA Splicing Inhibitor with IC 50 of 30 uM.target : MMP-9 [1], Pre-mRNA Splicing [2]IC 50: 30 u M (Pre-mRNA Splicing)In vitro: Isoginkgetin inhibits HT1080 tumor cell invasion substantially. Isoginkgetin is also quite effective in inhibiting the activities of Akt and MMP-9 in MDA-MB-231 breast carcinomas and B16F10 melanoma. Isoginkgetin treatment result in marked decrease in invasion of these cells. isoginkgetin inhibit activities of both Akt and NF-κB. Isoginkgetin markedly decrease MMP-9 expression and invasion through inhibition of this pathway. [1] Splicing inhibition is the mechanistic basis of the anti-tumor activity of isoginkgetin. [2] Isoginkgetin inhibits tumor cell invasion by regulating phosphatidylinositol 3-kinase/Akt-dependent matrix metalloproteinase-9 expression. [3]
3,3′-Bisdemethylpinoresinol, lignin, is a nature product and has MMP-1 inhibitory activity in UVA-irradiated human dermal fibroblasts. 3,3′-Bisdemethylpinoresinol can be isolated from the seeds of Morinda citrifolia[1].
Incyclinide (CMT-3, COL-3) is a matrix metalloproteinase (MMP) inhibitor, thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis.
Andecaliximab is a recombinant chimeric IgG4 monoclonal antibody (mAb) targets matrix metalloproteinase 9 (MMP9). Andecaliximab shows the antifibrotic efficacy in idiopathic pulmonary fibrosis mouse models. Andecaliximab can be used for the research of gastric adenocarcinoma and idiopathic pulmonary fibrosis (IPF)[1][2].
MMP-9-IN-7 is a potent MMP9 inhibitor with an IC50 of 0.52 μM in proMMP9/MMP3 P126 activation assay. MMP-9-IN-7 is extracted from patent WO2012162468 (example 59), and can be used for MMP9/MMP13 mediated syndrome research[1].
Nudol is a phenanthrene compound that has anti-cancer activity. Nudol inhibits cell proliferation, induces cell apoptosis. Nudol inhibits MMP-2M and MMP-9 activity (Ki: 988.9 nM, 1.76 μM, respectively). Nudol can be used in the research of cancers, such as osteosarcoma[1][2].
Phosphoramidon, a microbial metabolite, is a specific metalloprotease thermolysin inhibitor with an IC50 of 0.4 μg/mL. Phosphoramidon also inhibits endothelin-converting enzyme (ECE), neutral endopeptidase (NEP), and angiotensin-converting enzyme (ACE) with IC50 values of 3.5, 0.034, and 78 μM, respectively[1][2][3].
INCB3619 is a selective and orally active ADAM inhibitor with IC50 of 22 nM and 14 nM for ADAM10 and ADAM17, respectively. INCB3619 has anti-tumor activity[1].
TAPI-1 is a specific TACE (TNF-α-converting enzyme) inhibitor.IC50 value:Target: TAPI-1 inhibited LL-37-induced TGF-α production, EGFR activation and subsequent MUC5AC mucin production, whereas TGF-α-neutralizing antibody, but not AR- or HB-EGF-neutralizing antibody, inhibited LL-37-induced EGFR activation and subsequent MUC5AC mucin production in NCI-H292 cells [1]. Using the TNF-alpha converting enzyme (TACE) inhibitor, TAPI-1, TPA-stimulated TNFalpha shedding could be completely prevented in PKCepsilon transgenic mice and isolated keratinocytes [2]. Pretreatment with antibody against FcγRII or with CD32 siRNA, p47(phox) siRNA, apocynin, N-acetylcysteine, tumor necrosis factor-α protease inhibitor 1 (TAPI-1) or TACE siRNA attenuated sLOX-1 release induced by CRP. CRP also elevated serum sLOX-1 levels in a rabbit model of atherosclerosis [3].
MMP2-IN-1 is a moderate potenet MMP2 inhibitor with IC50 of 6.8 µM. MMP2-IN-1 exhibits remarkable antiproliferative activity in certain cancer cells by arresting the cell cycle and inducing apoptosis[1].
Auraptene is the most abundant naturally occurring geranyloxycoumarin. Auraptene is primarily isolated from plants in the Rutaceae family, such as citrus fruits. Auraptene decreases the secretion of matrix metalloproteinase 2 (MMP-2) as well as key inflammatory mediators, including IL-6, IL-8, and chemokine (C-C motif) ligand-5(CCL5)[1].
Ganoderic acid Mk (GA-Mk) is a triterpenoid acid, that can be isolated from the mycelia of Ganoderma lucidum. Ganoderic acid Mk is efficiently anti-proliferative and can induce apoptosis of HeLa cells by mitochondria-mediated pathway. Ganoderic acid Mk can be used for cervical cancer research[1][2].
Isozedoarondiol can be isolated from the rhizomes of Curcuma xanthorrhiza Roxb. Isozedoarondiol inhibits MMP-1 expression in UVB-treated human keratinocytes[1].
Ac-Pro-Leu-Gly-[(S)-2-mercapto-4-methyl-pentanoyl]-Leu-Gly-OEt is a MMP12 substrate, and can be used to detect MMP12 enzyme activity[1].
Aderamastat (FP-025) is an orally active matrix metalloproteinase 12 (MMP-12) inhibitor. Aderamastat can be used for the research of asthma, chronic obstructive pulmonary disease (COPD), and pulmonary fibrosis[1].
Imidapril (TA-6366 free base) is an orally active angiotensin-converting enzyme (ACE) and MMP-9 inhibitor. Imidapril suppresses the conversion of angiotensin I to angiotensin II and thereby reduces total peripheral resistance and systemic blood pressure. Imidapril can be used for hypertension, type 1 diabetic, nephropathy and chronic heart failure research[1][2].