Ilomastat

Bezeichnung:Ilomastat

CAS-Nr142880-36-2

Englisch Name:Ilomastat

CBNumberCB11178927

SummenformelC20H28N4O4

Molgewicht388.46

MOL-Datei142880-36-2.mol

Ilomastat physikalisch-chemischer Eigenschaften

Dichte	1.228±0.06 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	Soluble in DMSO, and 100% ethanol.
pka	9.16±0.20(Predicted)
Aggregatzustand	Off-white solid
Farbe	White
Sensitive	Moisture Sensitive
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
InChIKey	NITYDPDXAAFEIT-DYVFJYSZSA-N

Sicherheit

S-Sätze:	22-24/25
WGK Germany	3
HS Code	29339900

Gefahreninformationscode (GHS)

Ilomastat Chemische Eigenschaften,Einsatz,Produktion Methoden

S-Sätze Betriebsanweisung:
S22:Staub nicht einatmen.
S24/25:Berührung mit den Augen und der Haut vermeiden.
Beschreibung
Ilomastat (142880-36-2) is a potent pan-specific inhibitor of matrix metalloproteinases (MMPs).1 Ki values have been reported for the following human MMPs: MMP-1, 0.4nM; MMP-2, 0.5nM; MMP-3, 27nM; MMP-7, 3.7nM; MMP-8, 0.1nM; MMP-9, 0.2nM; MMP-12, 3.6nM; MMP-14, 13.4nM; MMP-26, 0.36nM.2-4 Also inhibits MMP-10, MMP-13, MMP-15, MMP-17, MMP-20, MMP-21, TACE and ADAM19.
Verwenden
GM 6001 is a potent, reversible broad spectrum inhibitor of zinc-containing proteases, including matrix metalloproteinases (MMPs). It inhibits zinc-containing thermolysin and elastase from P. aeruginosa, both with Ki values of 20 nM. GM 6001 inhibits MMP-1, -2, -7, -8, -9, -12, -13, -14, -16, and -26 with Ki or IC50 values between 0.1 and 10 nM. It inhibits disintegrin and metalloproteinase domain-containing (ADAM) proteins ADAM9, ADAM10, ADAM12, and ADAM17 at nanomolar concentrations. It less potently inhibits lethal factor from B. anthracis anthrax lethal toxin (Ki = 2.74 μM). GM 6001 also impairs the growth of the human pathogen Chlamydia by inhibiting peptide deformylase, which contains iron rather than zinc (IC50 = 38 nM).
Verwenden
Ilomastat is a metalloprotease inhibitor.
Definition
ChEBI: Ilomastat is an N-acyl-amino acid obtained by formal condensation of the carboxy group of (2R)-2-[2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoic acid with the amino group of N-methyl-L-tryptophanamide. A cell permeable broad-spectrum matrix metalloproteinase (MMP) inhibitor It has a role as an EC 3.4.24.24 (gelatinase A) inhibitor, a neuroprotective agent, an anti-inflammatory agent, an antibacterial agent and an antineoplastic agent. It is a L-tryptophan derivative, a hydroxamic acid and a N-acyl-amino acid.
Allgemeine Beschreibung
A cell-permeable, potent broad-spectrum hydroxamic acid inhibitor of matrix metalloproteinases (MMPs). [K_i = 0.4 nM for skin fibroblast collagenase (MMP-1); K_i = 0.5 nM for gelatinase A (MMP-2); K_i = 27 nM for stromelysin (MMP-3); K_i = 0.1 nM for neutrophil collagenase (MMP-8); and K_i = 0.2 nM for gelatinase B (MMP-9)]. Also prevents the release of TNF-α in vivo and in vitro and abrogates endotoxin-induced lethality in mice.
Biochem/physiol Actions
GM6001 promotes cardiovascular and hepatocellular function.
Lager
Store at -20°C
Einzelnachweise
1) Saghatelian et al. (2004) Activity-based probes for the proteomic profiling of metalloproteases; Proc. Natl. Acad. Sci. USA, 101 10000 2) Galardy et al. (1994) Low molecular weight inhibitors in corneal ulceration; Ann. N.Y. Acad..Sci. 732 315 3) Yamamoto et al.(1998) Inhibition of Membrane-Type 1 Matrix Metalloproteinase by Hydroxamate Inhibitors: An Examination of the Subsite Pocket; J. Med. Chem. 41 1209 4) Park et al. (2003) The intermediate S1- pocket of the endometase/matrilysin-2 active site revealed by enzyme inhibition kinetic studies, protein sequence analyses, and homology modeling; J. Biol. Chem. 278 51646

Ilomastat Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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