MMP

Doxycycline (Doxiciclina) belongs to the tetracycline class of antibiotics and is a broad-spectrum metalloproteinase (MMP) inhibitor with oral activity. Doxycycline has antibacterial activity and antitumor activity.

Abietic Acid (Sylvic acid) is the primary component of resin acid isolated from rosin.

Polygalacic acid (Virgaureagenin G)(PA) significantly improves cholinergic system reactivity, as indicated by decreased acetylcholinesterase (AChE) activity, increases choline acetyltransferase (ChAT) activity, and elevates levels of acetylcholine (ACh) in the hippocampus and frontal cortex, PA also significantly ameliorates neuroinflammation and oxidative stress in mice; suggest that PA might exert a significant neuroprotective effect on cognitive impairment, driven in part by the modulation of cholinergic activity and neuroinflammation. Polygalacic acid shows significant postingestive effects on Spodoptera littoralis larvae.

(-)-Epigallocatechin, the predominant flavonoid in green tea, possesses the unique ability to attach to unfolded native polypeptides, thereby inhibiting their transformation into amyloid fibrils.

Glucosamine (Chitosamine) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids. Supplemental glucosamine may help to rebuild cartilage and treat arthritis.

(-)-Arctigenin ((-)-Arctigenin) is found in burdock. (-)-Arctigenin is isolated from Cnicus benedictus, Forsythia viridissima, Arctium lappa, Ipomoea cairica and others (CCD). Arctigenin is a lignan found in certain plants of the Asteraceae, including the Greater burdock (Arctium lappa) and Saussurea heteromalla. It has shown antiviral and anticancer effects. It is the aglycone of arctiin.

Stigmasterol (Stigmasterin) is found in the fats and oils of soybean, calabar bean and rape seed, as well as several other vegetables, legumes, nuts, seeds, and unpasteurized milk. Stigmasterol has been focused on the cholesterol-lowering activity and is valued as an anti-stiffness factor in the therapy of rheumatic diseases.

Astragaloside IV (AS-IV), an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells. Astragaloside IV is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine.1 It dose-dependently inhibits human adenovirus type 3 (HAdV-3) in A549 cells (IC50 = 23 μM; LC50 = 865 μM).It inhibits replication of HAdV-3 and decreases HAdV-3-induced apoptosis. It has diverse protective effects for the cardiovascular, immune, digestive, and nervous systems. In particular, it reduces myocardial infarct size in dogs when administered prior to coronary ligation and reduces reperfusion arrhythmias in isolated rat hearts.

1. ISOGINKGETIN (4',4'''-Dimethylamentoflavone), a compound derived from the leaves of Ginkgo biloba, to up-regulate adiponectin secretion with potency comparable to that of rosiglitazone, a known modulator of adiponectin production. 2. Isoginkgetin has anti-tumor activity, the mechanistic basis is splicing inhibition , thus, pre-mRNA splicing inhibitors may represent a novel avenue for development of new anti-cancer agents.3. Isoginkgetin can inhibit tumor cell invasion by regulating phosphatidylinositol 3-kinase/Akt-dependent matrix metalloproteinase-9 expression. 4. Isoginkgetin (0.3mg/kg ip for 3d) can reduce the level of O2·- in plasma and erythroeyte and sometimes increase the activity of SOD in anoxic rats, the action being stronger than aspirin.

JC-10 is a potent inhibitor of metalloproteinases and is often used as a probe.

BMS-561392 Formic acid is a selective inhibitor of TACE and reduces TNFalpha levels.

CGS 27023A is a non-peptidic, potent, and orally active stromelysin inhibitor.

PG-116800 (PG-530742) is a matrix metalloproteinase (MMP) inhibitor. PG-116800 can be used in studies about the treatment of osteoarthritis.

Astragaloside, one of the main active ingredients in Astragalus membranaceus.

GPLGIAGQ acetate is a MMP2-cleavable polypeptide. GPLGIAGQ acetate can be used as a stimulus-sensitive linker in both liposomal and micellar nanocarriers to synthesis unique MMP2-targeted photosensitizer in photodynamic therapy.

CM-352 is a metalloproteinase inhibitor that reduces brain damage and improves functional recovery in rat models of cerebral hemorrhage.

CTTHWGFTLC, CYCLIC acetate is an inhibitor for matrix metalloproteinases (MMP)-2 and MMP-9. It is also called type IV collagenase or gelatinase. Gelatinases are potential targets of therapeutic intervention in cancer, and inhibitors of these enzymes can prevent tumor progression.

isomer-CM 352 is a metalase inhibitor that can be used to slow brain damage.

BPHA (MMP-2/MMP-9 Inhibitor II) is a potent, selective and orally active inhibitor of MMP-2, MMP-9 and MMP-14 with IC50s of 12 nM, 16 nM and 17 nM, respectively.BPHA does not inhibit MMP-1, -3 and -7 (IC50s of 974, >1000 and 795 nM, respectively).BPHA has anti-angiogenic and BPHA has anti-angiogenic and anti-tumor activities.

Bacoside A has a possible anticancer activity that could be inducing cell cycle arrest and apoptosis through Notch pathway in GBM in vitro. It exerts cytoprotective efficacy by attenuation of ROS generated through oxidative stress by an increase in the concentration of antioxidant enzymes and sustain membrane integrity which leads to restoring the damage caused by tBHP. Bacoside A can able to inhibit the progression of Experimental Autoimmune Encephalomyelitis (EAE) may be by the inhibition of inflammatory cytokines and chemokine evolved during active EAE. Bacoside A also has vasorelaxation.

Histatin 5 acetate inhibits the activity of the host matrix metalloproteinases MMP-2 and MMP-9 with IC50s of 0.57 and 0.25 μM, respectively.

MMP-9-IN-6 is an MMP-9 inhibitor with an IC50 value of 50 μM and good anti-ulcer efficacy.MMP-9-IN-6 has potential anti-tumor activity and can be used to study tissue remodeling, wound repair and atherosclerosis.

JG26 is a potent inhibitor of ADAM17, which can inhibit ADAM8, ADAM17, ADAM10 and MMP-12, with IC50 values of 12 nM, 1.9 nM, 150 nM and 9.4 nM, respectively, and can be used to study the immune system of the body.

DB04760 is a highly selective, non-zinc-chelating inhibitor of MMP-13 (IC50: 8 nM). DB04760 obviously decreases paclitaxel neurotoxicity and has anticancer activity.

MMP-12 Inhibitor is a selective inhibitor of MMP-12 with IC50s of 2, 160, 320, and 22.3 nM for human, mouse, rat, and sheep MMP-12.

PF 00356231 is a selectivity inhibitor MMP-12 and can be used in studies about the treatment of emphysema and chronic obstructive pulmonary disease (COPD).

ND-322 HCl (ND 322 Hydrochloride) is a selective inhibitor of MT1-MMP and MMP2 and reduces in vitro melanoma cell growth, migration and invasion.

Norepinephrine (Levophed) can stimulate apoptosis in adult rat ventricular myocytes by activation of the β-adrenergic pathway. It can up-regulate the expression of vascular endothelial growth factor, matrix metalloproteinase (MMP)-2, and MMP-9 in nasopharyngeal carcinoma tumour cells.

Batimastat (BB94) (BB-94) is an effective, broad-spectrum matrix metalloprotease (MMP) inhibitor. Batimastat induces extracellular matrix degradation and inhibits angiogenesis, tumor growth and invasion, and metastasis.

Ethyl gallate (gallic acid ethyl ester) obviously decreases cell proliferation in MDA-MB-231 and MCF-7 cells in a dose- and time-dependent manner, exhibits cytotoxicity in a dose-dependent manner. Ethyl gallate can inhibit the abilities of invasion of breast cancer in vitro by inhibiting the mRNA levels of MMP-9/MMP-2, phosphorylation of Akt and protein expression of NF-κB and inhibits hydrogen peroxide signaling, may represent an alternative class of vasopressors for use in septic shock. Also, Ethyl gallate suppresses proliferation and invasion in human breast cancer cells by modulating the PI3K/Akt pathway, which may contribute to inhibiting their downstream targets such as NF-κB p-65, Bcl-2/Bax, and mRNA levels of MMP-2 and MMP-9 in breast cancer cells, could be used as potential antioxidants with safe therapeutic application in cancer chemotherapy.

Ilomastat (GM6001) (GM6001, Galardin) is a broad spectrum matrix metalloprotease (MMP) inhibitor.

Muscone (3-Methylcyclopentadecanone) is an organic compound that is the primary contributor to the odor of musk.

1. β-Anhydroicaritin exhibits immunosuppressive effect on the mouse macrophages stimulated by LPS. 2. β-Anhydroicaritin phytosomes can inhibit enhanced bone turnover induced by ovariectomy, improve BMD the biomechanical properties of vertebrae, without any stimulation on uterus. 3. β-Anhydroicaritin possesses significant protective effects on the zymosan-induced peritonitis mice, which might be associated with the regulation of Ca(2+); influx in macrophages and iNOS expression.

Edaravone (MCI-186)(MCI-186) is a potent new free radical scavenger used for the therapy of patients with acute brain infarction.

Cordycepin (3'-Deoxyadenosine) is a purine nucleoside antimetabolite and antibiotic isolated from the fungus Cordyceps militaris with potential antineoplastic activity.

T-5224 is a transcription factor c-Fos/AP-1 inhibitor, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors.

SB-3CT is a potent and specific gelatinase inhibitor for MMP-2(Ki=13.9 nM) and MMP-9(Ki=600 nM).

MMP-7-IN-3 is a potent, selective MMP-7 inhibitor that effectively suppresses the progression of kidney fibrosis in a mouse model with unilateral ureteral obstruction [1].

Histatin 5 (TFA)(115966-68-2,free) (Histatin 5 (TFA)) inhibits the activity of the host matrix metalloproteinases MMP-2 and MMP-9 with IC50s of 0.57 and 0.25 μM, respectively.

Ginsenoside F4 has inhibitory effect on human lymphocytoma JK cell by inducing its apoptosis, the mechanism is related to the mitochondrial dysfunction and the increase of Bax expression and decrease of Bcl-2 expression.

Pimaric acid has potent anti-atherosclerotic activity with inhibitory action on matrix metalloproteinase-9 production and cell migration in TNF-α±-induced human aortic smooth muscle cells.

Isoangustone A has antitumor activity, it can induce G1 cycle arrest in DU145 human prostate and 4T1 murine mammary cancer cells, it inhibits cell proliferation by targeting PI3K, MKK4, and MKK7 in human melanoma. Isoangustone A dampens mesangial sclerosis associated with inflammation in response to high glucose through hindering TGF-β and NF-κB signaling. Isoangustone A also shows strong ferric reducing activities and effectively scavenged DPPH, ABTS(+), and singlet oxygen radicals.

MMP-7-IN-2 acts as a selective and potent MMP7 inhibitor and can be used to study inflammatory responses and vascular-related diseases.

Epitheaflagallin 3-O-gallate is a promising functional food material with potential antiobesity and antiperiodontal disease activities, it suppresses tumor growth through the suppression of angiogenesis.

Andecaliximab is a recombinant IgG4 monoclonal antibody targeting matrix metalloproteinase 9 (MMP9). Andecaliximab showed antifibrotic effects in a mouse model of idiopathic pulmonary fibrosis. Andecaliximab can be used to study gastric adenocarcinoma and idiopathic pulmonary fibrosis (IPF), as well as dengue virus.

Communic acid has antibacterial activity, including against mycobacterial. trans-Communic acid has potential to be utilized as anti-wrinkling agents and cosmetic ingredients, as they suppress UVB-induced MMP-1 expression.

Leucodin shows high anti-hypercholesterolemic potential. Leucodin may have anti-allergic activity, it shows a potent inhibitory activity upon the beta-hexosaminidase release from RBL-2H3 cells in a dose-dependent manner with IC50 of 80 microM.

Lucidenic acid C has anti-invasive effect, it shows significant inhibitory effects on PMA-induced MMP-9 activity and invasion of HepG(2 )cells.

2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-κB signaling to limit the inflammation and oxidative stress for preservation of BBB integrity. 2-Methoxystypandrone concomitant

Licorisoflavan A shows weak scavenging activity against superoxide anion radical, it and licoricidin have potential for the development of novel host-modulating strategies for the treatment of cytokine and/or MMP-mediated disorders such as periodontitis.L