A broad-spectrum inhibitor of MMPs (IC50s = 5

Marimastat – 5 mg

Brand:
Cayman
CAS:
154039-60-8
Storage:
-20
UN-No:
Non-Hazardous - /

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).{38559} 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).{38564} 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.{38560} Marimastat inhibits lymph node metastasis in an oral squamous cell carcinoma (OSCC) OSC-19 mouse xenograft model (30 mg/kg per day).{38561} 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.{38562} Marimastat is an inhibitor of tumor necrosis factor alpha (TNF-α) convertase (TACE), which catalyzes pro-TNF-α conversion into TNF-α (IC50s = 3.8 and 7,000 nM for purified TACE and whole blood, respectively).{38563}  

 

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Description

A broad-spectrum inhibitor of MMPs (IC50s = 5, 6, 230, 16, and 3 nM for MMP-1, MMP-2, MMP-3, MMP-7, and MMP-9, respectively); inhibitor of TACE (IC50s = 3.8 nM and 7 μM for purified TACE and whole blood, respectively); inhibits peritoneal dissemination of implanted human gastric carcinoma TMK-1 cells in nude mice (18 mg/kg per day); inhibits lymph node metastasis of OSC-19 cells implanted in nude mice (30 mg/kg per day); delays tumor growth of human head and neck squamous cells SCC-1 xenografts in nude mice alone and when combined with chemoradiation when used at a dose of 8.7 mg/kg per day

Formal name: (2S,3R)-N4-[(1S)-2,2-dimethyl-1-[(methylamino)carbonyl]propyl]-N1,2-dihydroxy-3-(2-methylpropyl)-butanediamide

Synonyms:  BB-2516|KB-R8898

Molecular weight: 331.4

CAS: 154039-60-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|MMPs||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cell Biology|Cytoskeleton & Motor Proteins||Research Area|Cell Biology|Proteolysis|Cytosolic & Secreted Proteases||Research Area|Immunology & Inflammation|Innate Immunity

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