| Reaction Details |
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| Target | Matrix Metalloproteinase-14 (MMP-14) |
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| Ligand | TMI-1 |
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| Substrate/Competitor | Wammp-5 |
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| Meas. Tech. | MMP Inhibition Assay |
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| pH | 7.4±n/a |
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| Temperature | 295.15±n/a K |
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| IC50 | 26±n/a nM |
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| Citation |  Zhang, Y; Xu, J; Levin, J; Hegen, M; Li, G; Robertshaw, H; Brennan, F; Cummons, T; Clarke, D; Vansell, N; Nickerson-Nutter, C; Barone, D; Mohler, K; Black, R; Skotnicki, J; Gibbons, J; Feldmann, M; Frost, P; Larsen, G; Lin, LL Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheumatoid arthritis.J Pharmacol Exp Ther.309:348-55(2004)[PubMed] |
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| More Info. |
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, Inhibition_Run data
, Solution Info
, Assay Method
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| Matrix Metalloproteinase-14 (MMP-14) |
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| Name | Matrix Metalloproteinase-14 (MMP-14) |
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| Synonyms | EC 3.4.24.80 | MT-MMP 1 | MTMMP1| MT1-MMP | MT1MMP | MMP-X1 | Membrane-type matrix metalloproteinase 1 | Membrane-type-1 matrix metalloproteinase |
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| Type | Single-pass type I membrane protein;metalloprotease |
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| Mol. Mass. | n/a |
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| Organism | Homo sapiens (human) |
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| Description | The recombinant catalytic domain was used in the assay. |
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| Residue | 177 |
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| Sequence | IQGLKWQHNEITFCIQNYTPKVGEYATYEAIRKAFRVWESATPLRFREVPYAYIREGHEK
QADIMIFFAEGFHGDSTPFDGEGGFLAHAYFPGPNIGGDTHFDSAEPWTVRNEDLNGNDI
FLVAVHELGHALGLEHSSDPSAIMAPFYQWMDTENFVLPDDDRRGIQQLYGGESGFP
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| TMI-1 |
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| Name | TMI-1 |
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| Synonyms: | (3S)-4-{[4-(but-2-yn-1-yloxy)benzene]sulfonyl}-N-hydroxy-2,2-dimethylthiomorpholine-3-carboxamide |
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| Type | Small organic molecule |
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| Emp. Form. | C17H22N2O5S2 |
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| Mol. Mass. | 398.497 |
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| SMILES | CC#CCOc1ccc(cc1)S(=O)(=O)N1CCSC(C)(C)[C@@H]1C(=O)NO |r| |
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| Structure | |
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| Wammp-5 |
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| Name | Wammp-5 |
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| Synonyms: | 7-methoxycoumarin-PQGL-(3-[2,4-dinitrophenyl]-L-2,3-diaminopropionyl)-AR-OH |
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| Type | Fluorogenic substrate |
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| Emp. Form. | n/a |
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| Mol. Mass. | n/a |
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| SMILES | n/a |
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| Structure | |
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