A potent, selective MMP-2 inhibitor with Ki of 230 nM.

Astragaloside 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.

Batimastat was used to study the role of MMP in proteolytic release of EGF in human follicular thyroid carcinoma cell line FTC-133.

CTS-1027 is a potent small molecule inhibitor of MMPs(IC50=0.4 nM/0.6 nM for MMP2/MMP13); >1,000 fold selectivity over MMP1.

Dnp-GPLG is a peptide for use as a negative control for activity of matrix metalloproteinases (MMPs) that cleave peptides containing the sequence Dnp-GPLG.

Dnp-P-Cha-Abu-Cys(Me)-HA-K(Nma)-NH2 is a fluorogenic substrate for matrix metalloproteinase-1 (MMP-1) and MMP-9.

Dnp-P-Cha-G-Cys(Me)-HA-K(Nma)-NH2 is a fluorogenic substrate for matrix metalloproteinase-1 (MMP-1) and MMP-9

Dnp-PLALWAR is a fluorogenic substrate for matrix metalloproteinase-1 (MMP-1) and MMP-8.

Dnp-PLAYWAR is a fluorogenic substrate for matrix metalloproteinase-8 (MMP-8) and MMP-26.The activity of MMP-8 and MMP-26 can be quantified by measuring tryptophan fluorescence that is unquenched upon peptide hydrolysis that removes the N-terminal dinitro

Dnp-PLG-Cys(Me)-HA-DArg-NH2 is a peptide substrate for matrix metalloproteinase-1 (MMP-1).It has an improved kcat/Km ratio compared with the MMP-1 flurogenic substrate Dnp-PLGLWA-DArg-NH2.

Dnp-PLGMWSR is a fluorogenic substrate for matrix metalloproteinase-2 (MMP-2) and MMP-9.The activity of MMP-2 and MMP-9 can be quantified by measuring tryptophan fluorescence that is unquenched upon peptide hydrolysis that removes the N-terminal dinitroph

Dnp-RPLALWRS is a fluorogenic substrate for matrix metalloproteinase-7 (MMP-7).The activity of MMP-7 can be quantified by measuring tryptophan fluorescence that is unquenched upon peptide hydrolysis that removes the N-terminal dinitrophenol (Dnp) group.

GI254023X is a potent MMP9 and ADAM10 inhibitor with IC50s of 2.5 and 5.3 nM, respectively.

GM6001 (galardin, ilomastat) is a broad spectrum MMPs inhibitor for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with Ki of 0.4-27 nM.

JNJ0966 is a highly selective compound that inhibited activation of MMP-9 zymogen and subsequent generation of catalytically active enzyme.

KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and 5050s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MM

Luteolin 7-O-glucuronide could inhibit Matrix Metalloproteinases (MMP) activities, with IC50s of 17.63, 7.99, 11.42, 12.85, 0.03 μM for MMP-1, MMP-3, MMP-8, MMP-9, MMP-13, respectively.

Marimastat is a broad spectrum MMP inhibitor and selective TACE inhibitor

Mca-PL is a fluorogenic peptide that has been used as a building block in the synthesis of Mca-PLGL-Dpa-AR-NH2, a fluorogenic substrate for matrix metalloproteinase-2 (MMP-2) and MMP-7.

MMP-2/MMP-9 inhibitor II is a dual inhibitor of matrix metalloproteinase-2 (MMP-2) and MMP-9 (IC50s = 17 and 30 nM, respectively).

MMP-2/MMP-9 inhibitor III is a cyclic peptide inhibitor of matrix metalloproteinase-2 (MMP-2) and MMP-9 (IC50s = 10-20 μM for both).

MMP-3 inhibitor is a peptide inhibitor of matrix metalloproteinase-3 (MMP-3) with a Ki value of 95 nM.

NSC 405020 is a noncatalytic inhibitor of MT1-MMP, directly interacts with PEX domain of MT1-MMP, affects PEX homodimerization but not catalytic activity of MT1-MMP.

SB-3CT is an effective and selective gelatinase inhibitor with Ki of 13.9 nM and 600 nM for MMP-2 and MMP-9, respectively.

S-methyl-KE-298 is an active metabolite of KE-298. KE-298 inhibits matrix metalloproteinase (MMP-1) production from rheumatoid arthritis (RA) synovial cells.

Tanomastat is an angiogenesis and Matrix Metalloproteinase inhibitor

TAPI-2 inhibits ADAM8, 10, 12, and TACE with Ki values of 10, 3, 100, and 0.12 µM, respectively.

ARP-100 is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC50=12 nM). ARP-100 interacts with S1＇ pocket of MMP-2 and shows anti-invasive properties in an in vitro model of invasion on matrigel. ARP-100 shows the less inhibitory activity towards MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM), and MMP-9 (0.2 μM).

UK-370106 is a potent and highly selective MMP-3 (IC50 of 23 nM) and MMP-12 (IC50 of 42 nM) inhibitor with >1200-fold higher potency than MMP-1, MMP-2, MMP-9, and MMP-14, and about 100-fold than MMP-13 and MMP-8. UK-370106 potently inhibits cleavage of [3H]-fibronectin by MMP-3 (IC50 of 320 nM) and has little effect on keratinocyte migration in vitro.

XL-784 free base is a selective matrix metalloproteinases (MMP) inhibitor, with IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1，MMP-2，MMP-3，MMP-8，MMP-9，MMP-13，respectively.

PF-00356231 hydrochloride is a specific, non-peptidic, non-zinc chelating ligand and inhibitor of matrix metalloproteinase MMP-12 (IC50=1.4 μM). PF-00356231 hydrochloride binds to MMP-12 and forms PF-00356231/MMP-12 complex. PF-00356231 hydrochloride shows potency against MMP-13, MMP-8, MMP-9, MMP-3 with IC50s of 0.00065, 1.7, 0.98, 0.39 μM, respectively.

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.

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).

GPLGIAGQ TFA, a MMP2-cleavable polypeptide, is used as a stimulus-sensitive linker in both liposomal and micellar nanocarriers for MMP2-triggered tumor targeting. GPLGIAGQ TFA can be used to synthesis unique MMP2-targeted photosensitizer in photodynamic therapy (PDT).

CTTHWGFTLC, CYCLIC TFA is a cyclic peptide inhibitor for matrix metalloproteinases MMP-2 and MMP-9. The IC50 value for MMP-9 is ~8 μM.

FFAGLDD is MMP9 selective cleavage peptides, which used for cytosolic delivery of Doxorubi-cin (DOX) and achieve temporally and spatially controlled slow drug delivery and release.

FFAGLDD TFA is MMP9 selective cleavage peptides, which used for cytosolic delivery of Doxorubi-cin (DOX) and achieve temporally and spatially controlled slow drug delivery and release.

CP-544439 is a potent and orally active matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 0.75 nM.

ADAM8-IN-1 is a potent ADAM8 inhibitor with an IC50 value of 73 nM.

GLPG1972 (Aldumastat, S201086) is a potent and selective small-molecule inhibitor of ADAMTS5 with IC50 of 19 and <23 nM against human and rat ADAMTS5, respectively.

ADAM17 inhibitor SN-4 is a novel specific inhibitor of A disintegrin and metalloproteinase 17 (ADAM17), inhibits TNF-α cleavage by SN-4 in cells with IC50 of 3.22 uM.SN-4 showed slightly higher activity than the well-studied ADAM17 inhibitor marimastat.SN-4 inhibited the ability of ADAM17 to cleave tumor necrosis factor α (TNF-α) in vitro, inhibited cleavage of CD44 by ADAM17, but not by ADAM10, and to suppress cell invasion.

MMP-13i is a potent, highly-selective inhibitor of MMP-13 catalytic activity with IC50 of 2.7 nM, no inhibitory effect against MMP1/2/8/9/14 (IC50>5,000 nM).MMP-13i potently suppressed wild-type osteoclast formation in vitro at concentrations <100 nM.MMP-13i strongly inhibited multiple myeloma viability.MMP-13i treatment delayed multiple myeloma growth in immunocompetent syngeneic mouse model of multiple myeloma, inhibited multiple myeloma promotes systemic skeletal bone disease.

PG-116800 is a selective, oral matrix metalloproteinase (MMPs) inhibitor with significant antiremodeling effects in animal models of MI and ischemic heart failure.

Prinomastat (AG3340) is a potent, selective MMP inhibitor with pM affinities for inhibiting gelatinases (MMP-2 and -9, Ki=50-150 pM), MMP-14 and MMP-13; demonstrates broad antitumor activity in a number of tumor models, inhibits glioma invasion or growth of the human malignant glioma cell line U87; also suppresses tumor growth in a malignant glioma tumor model.

Rebimastat (BMS-275291, D2163) is a potent, broad spectrum matrix metalloproteinase (MMPs) inhibitor with potential antineoplastic activity, shows nM potency against MMP-1/2/7/9/14.BMS-275291 inhibits tumor growth in a B16BL6 model of experimental metastasis, BMS-275291 treatment results in a dose-dependent reduction in the number of lung metastases.BMS-275291 also inhibits angiogenesis in a murine angiogenesis model with a dose-dependent inhibition of endothelial cell migration.Rebimastat (BMS-275291) induces extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis.

SC-78080 (SD-2590) is a potent, selective inhibitor of MMP2/9/13 with IC50 of <0.1/0.18/<0.1 nM, respectively.SC-78080 shows weaken inhibitory effect on MMP3/8, and no inhibition on MMP1/7.

NNGH is a stromelysin-1 (MMP-3) inhibitor. MMP-3 is both a direct transcriptional target and a necessary contributor of the Wnt/β-catenin signaling pathway. Matrix metalloproteinases (MMPs) play a well-defined role in later stages of tumor progression.

ONO-4817 is a potent inhibitor of matrix metalloproteinase (MMP). Inhibition of matrix metalloproteinases (MMPs) is expected to suppress atherosclerotic neointimal proliferation and thus limits atheromatous plaque progression. ONO-4817 suppresses the development of aortic intimal hyperplasia in experimental hyperlipidemic rabbit.

JG26 is an ADAM17 inhibitor, with IC50 values of 12 nM, 1.9 nM, 150 nM and 9.4 nM for ADAM8, ADAM17, ADAM10 and MMP-12, respectively.

TP0556351 is a potent and selective matrix metalloproteinase-2 (MMP2) inhibitor with an IC50 value of 0.2 nM. TP0556351 reduces the amount of collagen in the lungs of a Bleomycin-induced pulmonary fibrosis mouse model. TP0556351 can be used for researching idiopathic pulmonary fibrosis (IPF).

(Rac)-Tanomastat ((Rac)-BAY 12-9566) is the racemate of Tanomastat. Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models.

PPNDS tetrasodium is a selective and competitive meprin β inhibitor (IC50: 80 nM, Ki: 8 nM), and also inhibits ADAM10 (IC50: 1.2 μM). PPNDS tetrasodium is also a P2X1 receptor antagonist. PPNDS is an agonist for the ATP receptor of Paramecium. PPNDS tetrasodium potently inhibits polymerases from viruses. PPNDS tetrasodium can be used in the research of infection and cancers.

TP0597850 is a selective inhibitor of MMP2 (IC50=0.22 nM). TP0597850 has a long MMP2 dissociation half-life (t1/2=265 min).

cis-ACCP is an orally active antimetastatic matrix metalloproteinase-2 (MMP-2) selective inhibitor. cis-ACCP can inhibit MMP-2 and MMP-9 with IC50 values of 4 μM and 20 μM, respectively. cis-ACCP can be used for the research of a variety of chronic diseases.

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.

ADAM9i is a specific small molecule inhibitor of ADAM9 protein with binding KD of 5.9 uM and enzyme IC50 of 5.2 uM, promotes the selective degradation of KRAS and sensitizes pancreatic cancers to chemotherapy.

AZD1236 is a potent, selective MMP-9 and MMP-12 inhibitor with IC50 of 4.5 and 6.1 nM respectively, >10-fold selectivity to MMP-2 and MMP-13 and >350-fold selectivity to other MMPs.

BAY-9835 is the first orally bioavailable ADAMTS7 inhibitor with IC50 of 6 nM, which is selective against a range of off-targets and metalloproteases except for ADAMTS12.

CID 3117694 is a selective, non-competitive inhibitor of ADAM10 with IC50 of 1.1 uM, does not inhibit ADAM17.

IPR-179 (ACT-03) is a potent, BBB-permeable, selective gelatinase (MMP2 and MMP9) inhibitor with IC50 of 656 nM and 310 nM, respectively.

JTP-96193 (JTP96193) is a potent, selective TNF-α converting enzyme (TACE/ADAM17) inhibitor with IC50 of 5.4 nM, >1800-fold selectivity against ADAM10.

MMP118 is a potent, selective and orally bioavailable matrix metalloproteinase-12 (MMP-12) inhibitor with IC50 of 1.0 nM (hMMP-12), 1980- and 154-fold selectivity over MMP-13 and MMP-8 respectively.

MMP408 (MMP 408) is a potent, selective matrix metalloprotease 12 (MMP-12) inhibitor with IC50 of 2.0 nM (human MMP-12), 60-fold selectivity over MMP-13.

TAPI-0 is a potent, selective inhibitor of TNFalpha converting enzyme (TACE, ADAM7) with IC50 of 100 nM.

TP0628103 is a highly potent, selective matrix metalloproteinase-7 (MMP-7) inhibitor with IC50 of 0.17 nM and 4.1 nM for human and mouse MMP-7, respectively.