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Marimastat is a broad-spectrum matrix metalloproteinase (MMP) inhibitor (IC50s = 5, 6, 230, 16, and 3 nM for MMP-1, MMP-2, MMP-3, MMP-7, and MMP-9, respectively). It also binds to a recombinantly expressed catalytic domain of human MMP-14 (MMP-14cat, Ki = 2.1 nM) and inhibits gelatinases (IC50s = 3-6 nM), fibroblast collagenase (IC50 = 5 nM), and matrylisin (IC50 = 16 nM). It inhibits peritoneal dissemination of implanted human gastric carcinoma TMK-1 cells in nude mice (18 mg/kg per day) but does not affect TMK-1 viability in vitro, providing only 2.64% inhibition when used at a concentration of 10 µM. Marimastat inhibits lymph node metastasis in an oral squamous cell carcinoma (OSCC) OSC-19 mouse xenograft model (30 mg/kg per day). It also delays tumor growth of human head and neck squamous cell SCC-1 xenografts in nude mice alone and when combined with chemoradiation when administered at a dose of 8.7 mg/kg per day. Marimastat is an inhibitor of tumor necrosis factor alpha (TNF-alpha) convertase (TACE), which catalyzes pro-TNF-alpha conversion into TNF-alpha (IC50s = 3.8 and 7,000 nM for purified TACE and whole blood, respectively).Formal Name: (2S,3R)-N4-[(1S)-2,2-dimethyl-1-[(methylamino)carbonyl]propyl]-N1,2-dihydroxy-3-(2-methylpropyl)-butanediamide. CAS Number: 154039-60-8. Synonyms: BB-2516, KB-R8898. Molecular Formula: C15H29N3O5. Formula Weight: 331.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 2 mg/ml. SMILES: CC(C)(C)[C@@H](C(NC)=O)NC([C@H](CC(C)C)[C@@H](C(NO)=O)O)=O. InChi Code: InChI=1S/C15H29N3O5/c1-8(2)7-9(10(19)13(21)18-23)12(20)17-11(14(22)16-6)15(3,4)5/h8-11,19,23H,7H2,1-6H3,(H,16,22)(H,17,20)(H,18,21)/t9-,10+,11-/m1/s1. InChi Key: OCSMOTCMPXTDND-OUAUKWLOSA-N.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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