mmp-1

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

Prinomastat hydrochloride is a orally active inhibitor of metalloproteinase (MMP)(MMP-1, MMP-3 and MMP-9 with IC50s of 79, 6.3 and 5.0 nM , respectively),with Antitumor avtivity.

Prinomastat (AG3340) is an orally active and selective inhibitor of metalloproteinases (MMPs) that crosses the blood-brain barrier.

MMP-1-IN-1 is a highly potent MMP-1 inhibitor with an IC 50 of 0.034 μM .

MMP-13-IN-1, with an IC50 value of 16 nM, is a potent and selective inhibitor of MMP-13, suitable for atherosclerosis research [1].

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

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.

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-2 9-IN-1 (Compound 4a) is a potent dual inhibitor of MMP-2 (IC50: 56 nM) and MMP-9 (IC50: 38 nM), leading to DNA fragmentation.

Tubulin MMP-IN-1, a potent inhibitor of both tubulin and MMP, holds promise for cancer research. It effectively suppresses tubulin polymerization, induces G2 M phase cell cycle arrest, and promotes reactive oxidative stress (ROS) generation in HepG2 cells, ultimately triggering apoptosis via the mitochondrial-dependent apoptotic pathway.

MMP-13 Substrate, a compound utilized in osteoarthritis (OA) research [1], functions as a substrate for MMP-13.

MMP-145 is used as a protease inhibitor.

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.

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).

(S,S)-TAPI-1, an isomer of TAPI-1, is a metalloproteinase (MMP) inhibitor and a TACE (ADAM17) inhibitor known for its potent inhibition of various cell surface protein shedding.

Chloramphenicol (Chloromycetin) is a broad-spectrum antibiotic that inhibits the biosynthesis of bacterial proteins. Chloramphenicol acts primarily on the 50S subunit of the bacterial 70S ribosome and is active against peptidyltransferases, inhibiting the formation of peptide bonds.

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

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.

Glyceryl Trioleate has been investigated for the treatment of Adrenoleukodystrophy.

o-Phenanthroline monohydrate (1, 10-Phenanthroline monohydrate) is an inhibitor of metallopeptidases, inhibits zinc-dependent hydrolysis of Fa-Gly-Leu-NH2 by B. subtilis neutral protease and B. thermoproteolyticus thermolysin.

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8 9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26 DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630 624 and the boron of talabostat[3]. Talabostat can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20 2J lymphoma models, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. [1]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [2]. Okondo MC, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. [3]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [4]. Egger C, et al. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72.

Siramesine (Lu 28-179)(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.lysosome-destabilizing agent siramesine can induce rapid cell death in a number of cell lines at concentrations above 20 μM. In HaCaT cells, cell death was accompanied by caspase activation, rapid loss of mitochondrial membrane potential (MMP), cytochrome c release, cardiolipin peroxidation and typical apoptotic morphology, whereas in U-87MG cells most apoptotic hallmarks were not notable, although MMP was rapidly lost

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.

1. Gycitein has weak estrogenic activity. 2. Glycitein (Glycetein) inhibits glioma cell invasion through down-regulation of MMP-3 and MMP-9 gene expression.