Marimastat
Marimastat Basic information
- Product Name:
- Marimastat
- Synonyms:
-
- Marimastat
- (2R,3S)-N1-((S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl)-N4,3-dihydroxy-2-isobutylsuccinamide
- (2S,3R)-N4-[(1S)-2,2-Dimethyl-1-[(methylamino)carbonyl]propyl]-N1,2-dihydroxy-3-(2-methylpropyl)butanediamide
- (2R,3S)-N1-((S)-3,3-diMethyl-1-(MethylaMino)-1-oxobutan-2-yl)-N4
- BB 2516
- GI 5712
- KB-R 8898
- TA 2516
- CAS:
- 154039-60-8
- MF:
- C15H29N3O5
- MW:
- 331.41
- EINECS:
- 251-228-4
- Product Categories:
-
- API
- Mol File:
- 154039-60-8.mol
Marimastat Chemical Properties
- Melting point:
- 148℃
- Density
- 1.140±0.06 g/cm3(Predicted)
- RTECS
- EJ6665000
- storage temp.
- -20°C
- solubility
- DMSO: ≥20mg/mL
- form
- White solid
- pka
- 9.44±0.40(Predicted)
- color
- White to gray
Marimastat Usage And Synthesis
Uses
Antineoplastic (matrix metalloproteinase inhibitor).
Uses
Marimastat acts as a matrix metalloproteinase inhibitor in the treatment of various cancers, and pathological occurrences such as arthritis and atherosclerosis.
Uses
Marimastat has been used as an inhibitor of:
- metalloproteinase 2/9 (MMP2/9), to study its effects on exercise-mediated interleukin-6 (IL-6) release in mice
- metalloproteinase, to determine protease activity in Pseudomonas aeruginosa cultures
- metalloproteinase 10 (MMP10), to study its effect on monoclonal antibody H3 binding to MMP10
Definition
ChEBI: Marimastat is a secondary carboxamide resulting from the foraml condensation of the carboxy group of (2R)-2-[(1S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoic acid with the alpha-amino group of N,3-dimethyl-L-valinamide. It has a role as an antineoplastic agent and a matrix metalloproteinase inhibitor. It is a secondary carboxamide and a hydroxamic acid.
General Description
An orally active peptidyl hydroxamate-based broad-spectrum MMP inhibitor (IC50 in nM = 5, 6, 200, 20, 2, 1.8 and 3.8 for MMP-1, -2, -3, -7, -8, -14 and TACE, respectively) that targets both the substrate binding site and the active-site Zn2+. Marimastate is widely used in studying the involvement of MMPs in various cellular and pathological processes both in vitro and in vivo.
Biological Activity
Broad spectrum inhibitor of matrix metalloprotease (MMP) (IC 50 values are 3, 5, 6, 9 and 13 nM for MMP-9, MMP-1, MMP-2, MMP-14 and MMP-7 respectively). In vivo inhibits peritoneal dissemination of human gastric cancer cells through inhibition of tumor angiogenesis.
Biochem/physiol Actions
Marimastat is a broad spectrum matrix metalloprotease (MMP) inhibitor
storage
Store at -20°C
MarimastatSupplier
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