MMP

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

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.

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.

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

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

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

Doxycycline hyclate (WC2031) belongs to the tetracycline class of antibiotics and is a broad-spectrum metalloproteinase (MMP) inhibitor with oral activity. Doxycycline hyclate has antibacterial activity and antitumor activity.

Nobiletin (Hexamethoxyflavone) is a natural polymethoxylated flavone isolated from citrus peels with anti-inflammatory and anti-tumor activities. Nobiletin is practically insoluble (in water) and an extremely weak acidic compound (based on its pKa).

Salvianolic acid A (Dan Phenolic Acid A) is a natural product and an inhibitor of matrix metalloproteinase 9 (MMP-9). Salvianolic acid A has antioxidant and anti-inflammatory activity and protects the blood-brain barrier.

Calycosin-7-O-β-D-glucoside (calycosin-7-O-beta-D-glucopyranoside) exhibits a protective effect on rat hepatocytes, inhibits COX-2 activity, has antimicrobial properties, and is a promising anti-HIV agent. Additionally, it demonstrates scavenging activity against DPPH radicals and superoxide anions, alleviates osteoarthritis, and increases brain cell membrane fluidity in ischemia-reperfusion rats.

Hinokiflavone, a novel modulator of pre-mRNA splicing activity both in vitro and in cellulo, inhibits the assembly of the spliceosome, particularly blocking the formation of the B complex. Additionally, it acts as a SUMO protease inhibitor by impeding the activity of sentrin-specific protease 1 (SENP1). Hinokiflavone also demonstrates significant cytotoxicity, including the inhibition of MMP-9.

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.

IK-862 is a selective inhibitor of TACE (ADAM17).

Methyl rosmarinate is a noncompetitive tyrosinase inhibitor isolated from Rabdosia serra, with an IC50 of 0.28 mM for mushroom tyrosinase. It exhibits antioxidative and antifungal activities, and also inhibits tyrosinase, α±-glucosidase, and matrix metalloproteinase-1 (MMP-1).

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.

Cordycepin (3'-Deoxyadenosine) is a purine nucleoside antimetabolite and antibiotic derived from the fungus [Cordyceps militaris], exhibiting potential antineoplastic activity.

S-methyl-KE-298 is the second main metabolite in plasma,is a methyl conjugate of deacetyl-KE-298.KE-298 inhibits matrix metalloproteinase (MMP-1) production from  rheumatoid arthritis (RA) synovial cells.

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.

CP-544439 is an orally active and potent MMP-13 inhibitor that prevents diet-induced obesity and inhibits adipogenesis in 3T3-L1 preadipocytes in mice, and can be used for the study of obesity.

CL-82198, a selective MMP-13 inhibitor, serves as a pharmacological intervention to halt the progression of osteoarthritis (OA). Its mechanism of action involves binding to the S1’ pocket of MMP-13, ensuring its selectivity and preventing inhibition of other MMPs.

TAPI1 (TAPI) , an ADAM17 TACE inhibitor, inhibits shedding of cytokine receptors.

Chemically modified tetracyclines (CMTs) can inhibit MMPs, but lack antimicrobial activity. Nonantimicrobial derivative of tetracycline called incyclinide (COL-3, CMT-3). Incyclinide (CMT-3) has been shown to experimentally suppress prostate cancer, colon adenocarcinoma and melanoma invasiveness in cell culture and to inhibit tumor growth and metastasis.

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

AGPS-IN-2i is a potent and high-affinity inhibitor of alkylglycerol phosphate synthase that controls ether lipid utilization and metabolism in cells, reduces ether lipid levels and cell migration, and promotes proliferation and motility of cancer cells. AGPS-IN-2i had an inhibitory effect on cancer cell proliferation.

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.

Isoliquiritin apioside, isolated from Glycyrrhizae radix rhizome, significantly decreases PMA-induced increases in MMP9 activities and suppresses PMA-induced activation of MAPK and NF-κB. Isoliquiritin apioside auppresseses invasiveness and angiogenesis o

GI254023X is a MMP9 and ADAM10 inhibitor with IC50 values ​​of 2.5 and 5.3 nM, respectively. GI254023X can also significantly inhibit the proliferation of Jurkat cells and induce apoptosis.

MMP-3 Inhibitor is a peptide matrix metalloproteinase-3 (MMP-3) inhibitor with a Ki value of 95 nM.MMP-3 inhibitor has anticancer and antitumor activity.

GW280264X (Carbamic acid) is an inhibitor of ADAM17 .

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

Chondroitin sulfate (Chonsurid) is extracted from shark bone;Store the product in sealed, cool and dry condition

Marimastat (BB2516) (BB-2516) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor. MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM)and MMP-7 (IC50=13 nM).

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.

Apigenin-7-glucuronide (Apigenin 7-O-glucuronide) possesses multiple activities, including antioxidant, anti-inflammatory, and aldose reductase inhibitory activities, it can inhibit MMP activities (IC50s: 12.87, 22.39, 17.52, 0.27 μM for MMP-3, MMP-8, MMP-9, MMP-13, respectively).

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

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.

KP-457 is a specific inhibitor of a disintegrin-metalloproteinase 17 (ADAM17) and a TNFα converting enzyme TACE inhibitor that blocks the production of soluble TNF (sTNF).

Stigmasterol (Stigmasterin) is a phytosterol with major functions in the maintenance of cell membrane structure and physiology. Stigmasterol lowers cholesterol levels and has anti-tumor, anti-inflammatory, and immunomodulatory effects.

Luteolin 7-O-glucuronide (Luteolin-7-glucuronide) possesses antioxidant activities.

Auraptene is a coumarin derived from citrus plants that bears a geranyloxyl moiety at its C-7. It has anti-inflammatory, anti-carcinogenic, anti-bacterial, neuroprotective, and hepatoprotective activities. It inhibits leukocyte activation and induces phas

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

o-Phenanthroline (1,10-Phenanthroline) , a metal chelator, prevents the induction of chromosomal aberrations in streptozotocin-treated cells.o-Phenanthroline protects mammalian cells from hydrogen peroxide-induced gene mutation and morphological transformation.

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.

MMP-9-IN-1 is an inhibitor of specific matrix metalloproteinase-9 (MMP-9).

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.

Polygalacic acid (Virgaureagenin G) is a triterpenoid isolated from the root of Polygala tenuifolia Willd that inhibits MMP expression. Polygalacic acid (Virgaureagenin G) can significantly improve the responsiveness of the cholinergic system, such as decreased acetylcholinesterase (AChE) activity, increased choline acetyltransferase (ChAT) activity, and increased acetylcholine (ACh) levels in the hippocampus and frontal cortex. Polygalacic acid (Virgaureagenin G) can also inhibit IL-1β-induced Wnt β-catenin activation and mitogen-activated protein kinase (MAPK) signaling pathways in chondrocytes, and is used in osteoarthritis (OA) related research.

MMP13-IN-3 is >1000 selective over other MMPs. MMP13-IN-3 is an effective, selective, and orally active MMP-13 inhibitor (IC50=1 nM) for the potential treatment of osteoarthritis.

T-26c is a highly potent and selective matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 6.75 pM.