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.

Abietic Acid (Sylvic acid) is a diterpene extracted from Pimenta racemosavar. grissea with antimicrobial, antiproliferative and anti-obesity activities. It inhibits lipoxygenase activity and may be studied in allergic diseases.

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.

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

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

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.

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.

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

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.

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

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.

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).

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.

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.

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).

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).

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.

Cedrelone is a citrulline analog and a phenazine biosynthesis-like domain protein (PBLD) activator.Cedrelone induces apoptosis in cancer cells.Cedrelone is a very potent inducer of apoptosis, causing cell cycle arrest.Cedrelone has insecticidal activity, inhibiting the growth of arrowhead venom of P. saucia and inhibiting moulting of the milkweed bug (Oncopeltus fasciatus). Cedrelone has insecticidal activity, inhibiting the growth of P. saucia and inhibiting moulting of the milkweed bug (Oncopeltus fasciatus).Cedrelone has antitumor effects and exhibits significant cytotoxicity against cancer cell lines such as -60, SMMC-7721, A-549, MCF-7, and SW480.Cedrelone is a very potent inducer of apoptosis, causing cell cycle arrest.Cedrelone is a very potent inducer of apoptosis, leading to cell cycle arrest.

GW280264X (Carbamic acid) is an inhibitor of ADAM17 .

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.

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

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.

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.

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

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.

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.

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).

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

Glyceryl Trioleate has been investigated for the treatment of Adrenoleukodystrophy.

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

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

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

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).

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.

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

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

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

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.

ALOIN Inhibits Interleukin (IL)-1β-Stimulated IL-8 Production in KB Cells.

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

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

Ginkgolide C (BN-52022), a natural product, can enhance the cardiac function of rats in the body.

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).

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.

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.