MMP13-IN-4 (compound 13) is a potent and selective inhibitor of MMP-13 (IC50=14.6 μM)，involved in osteoarthritis (OA)[1].
Glucocorticoid receptor-IN-1 (Compound WX002) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-1 exhibits very good transcriptional repressive activity with an IC50 of 2.11 nM against hMMP1, and transcriptional activation activity with an EC50 of 5.59 nM against MMTV[1].
Edaravone D5 is a deuterium labeled Edaravone. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator[1][2][3][4].
MMP-2 Inhibitor II (compound 2) is a selective MMP-2 inhibitor. The Kinetic parameters for MMP inhibition are 2.4 μM (MMP-2), 45 μM (MMP-1), and 379 μM (MMP-7), respectively[1].
WAY-170523 is a potent and selective MMP-13 (matrix metalloproteinase-13) inhibitor, with an IC50 of 17 nM. WAY-170523 can directly attenuate ERK1/2 phosphorylation. WAY-170523 inhibits the invasion of PC-3 cells, can be used for prostate cancer research[1][2].
Tubulin/MMP-IN-2 is dual inhibitor of tubulin and matrix metalloproteinases. Tubulin/MMP-IN-2 can strongly inhibit tubulin polymerization and induces cell Apoptosis. Tubulin/MMP-IN-2 has inhibitory activities against MMP-2, MMP-3 and MMP-9 with IC50 values of 24.95 μM, 31.60 μM and 22.37 μM, respectively. Tubulin/MMP-IN-2 can be used for the research of cancer[1].
CL-82198 is a selective inhibitor of MMP-13.In vitro: In the presence of 10 and 20 μM of the specific MMP-13 inhibitor, CL-82198, migration of the LS174 cells was significantly reduced by 55 and 52%, respectively. . CL-82198 binds to the S1' pocket of MMP-13 leading to 89% enzyme inhibition at a concentration of 10 μg/ml. The addition of the specific MMP-13 inhibitor CL-82198 at a concentration of 10 μM resulted in a 45±5.6% reduction in the migration of LS174 cells.
Glucocorticoid receptor-IN-2 (Compound WX019) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-2 exhibits very good transcriptional repressive activity with an IC50 of 0.171 nM against hMMP1, and comparable transcriptional activation activity with an EC50 of 0.94 nM against MMTV[1].
MMP-9/MMP-13 Inhibitor I is a potent MMP-9 and MMP-13 inhibitor with IC50s of both 0.9 nM. MMP-9/MMP-13 Inhibitor I shows >20-folds selectivity for MMP-9/MMP-13 over other MMPs[1].
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 (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively.
JNJ0966 is a highly selective MMP-9 zymogen inhibitor with an IC50 of 440 nM.
SEMBL is a potent NF-κB inhibitor that inhibits DNA binding of NF-κB component p65; inhibits LPS-induced NF-κB activation, iNOS expression, and inflammatory cytokine secretions; also inhibits NF-κB and cellular invasion in ovarian carcinoma ES-2 cells; enhances stability in aqueous solution compared with (-)-DHMEQ.
Triolein-d5 is the deuterium labeled Triolein. Triolein is a symmetrical triacylglycerol, reduces MMP-1 upregulation, with strong antioxidant and anti-inflammatory properties[1].
MMP Inhibitor II (compound 4e) is a potent, reversible pan-MMP inhibitor with IC50 values of 24 nM, 18.4 nM, 30 nM, and 2.7 nM for MMP-1,MMP-3, MMP-7, and MMP-9, respectively[1].
CP-471474 is an orally active and pan MMP inhibitor, with IC50 values of 1170 nM (MMP-1), 0.7 nM (MMP-2), 16 nM (MMP-3), 13 nM (MMP-9) and 0.9 nM (MMP-13), respectively[1][2].
2-Methoxy-2,4-diphenylfuran-3-one is a fluorescent compound which can be used to label gelatin as a substrate for detection of the gelatin degrading MMP-2 and MMP-9 by zymography[1].
Doxycycline, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor[1].
Mca-P-Cha-G-Nva-HA-Dap(DNP)-NH2 is a fluorogenic substrate for matrix metalloproteinase-1 (MMP-1), MMP-3, and MMP-26. Mca-P-Cha-G-Nva-HA-Dap(DNP)-NH2 can be used to quantify MMP-1, MMP-3 and MMP-26 activity[1][2].
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[1].
Inotilone is an inhibitor of matrix metalloproteinase MMP-2 and MMP-9, to against metastatic in lung cancer cells. Inotilone enhances the activity of the antioxidant enzymes to support its anti-metastatic activity. Inotilone also inhibits IκBα phosphorylation and NFκB p65 nuclear translocation, involving in FAK, PI3K/AKT, MAPKs and NFκB pathways[1].
β-Neo-Endorphin is an endogenous opioid peptide. β-Neo-Endorphin is a hypothalamic “big” Leu-enkephalin of porcine origin. β-Neo-Endorphin shows activation of the Erk1/2, MMP-2 and MMP-9[1][2].
ARP101 is a potent and selective inhibitor matrix metalloproteinase-2 (MMP-2). ARP101 induces autophagy-associated cell death in cancer cells. ARP101 is effective in inducing the formation of autophagosome and conversion of LC3I into LC3II[1].
Abametapir is a metalloproteinase (MMP) inhibitor which is able to target metalloproteinases critical to egg hatching and louse development. Abametapir can inhibit hatching of both head and body louse[1][2].
Lucidenic acid C is a natural compound isolated from Ganoderma lucidum, inhibits PMA-induced MMP-9 activity, with anti-invasive effect on hepatoma cells[1].
FN-439 is a selective collagenase-1 inhibitor. FN-439 inhibits collagenase-1 with an IC50 value of 1 μM. FN-439 can be used for the research of cancer and inflammation[1][2].
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[1].
Communic acid ((+)-Communic acid) is a natural compound isolated from the branches of Platycladus orientalis. Communic acid displays minimum inhibitory concentration of 31 μM and IC50 of 15 μM against M. tuberculosis H37Ra.Communic acid exhibits protective effects against UVB-induced skin aging[1][2][3].
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[1][2].
BAY-7598 (BAY7598) is a potent, selective MMP12 inhibitor.
MMP2-IN-2 (compound 42) is a potent and selective MMP-2 (matrix metalloproteinases) inhibitor, with an IC50 of 4.2 μM. MMP2-IN-2 also shows inhibitory activity against MMP-13, MMP-9 and MMP-8, with IC50 values of 12, 23.3, and 25 μM, respectively[1].