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Marimastat

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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
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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
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Safety Information

WGK Germany 
3
HS Code 
29241990
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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

Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Email
jkinfo@jkchemical.com
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Email
3bsc@sina.com
LGM Pharma
Tel
1-(800)-881-8210
Email
inquiries@lgmpharma.com
Jinan Trio PharmaTech Co., Ltd.
Tel
+86 (531) 88811783
Email
sales@trio-pharmatech.com (International market)
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