Marimastat

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

Uses

Antineoplastic (matrix metalloproteinase inhibitor).

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