MONASTROL Struktur

MONASTROL

Bezeichnung:MONASTROL

CAS-Nr254753-54-3

Englisch Name:MONASTROL

CBNumberCB7745337

SummenformelC14H16N2O3S

Molgewicht292.35

MOL-Datei254753-54-3.mol

MONASTROL physikalisch-chemischer Eigenschaften

Schmelzpunkt	185-185.9 °C(lit.)
Siedepunkt	441.3±55.0 °C(Predicted)
Dichte	1.34±0.1 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	DMSO: 100 mg/mL
Aggregatzustand	White solid
pka	9.63±0.10(Predicted)
Farbe	white to off-white
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
CAS Datenbank	254753-54-3(CAS DataBase Reference)

Sicherheit

S-Sätze:	22-24/25
WGK Germany	3

Gefahreninformationscode (GHS)

MONASTROL Chemische Eigenschaften,Einsatz,Produktion Methoden

S-Sätze Betriebsanweisung:
S22:Staub nicht einatmen.
S24/25:Berührung mit den Augen und der Haut vermeiden.
Beschreibung
Monastrol (254753-54-3) is a potent, cell-permeable, small molecule inhibitor of mitosis. Monastrol-arrested cells are characterized by monopolar spindles.1?Does not affect other motor proteins or tubulin. Specifically inhibits the mitotic molecular motor kinesin Eg5, a motor protein required for spindle formation (IC50?= 14 μM).2?Mimics the effect of amyloid β on long term potentiation in a cellular model of learning and memory.3?Enhances regeneration of adult axons.4
Chemische Eigenschaften
Crystalline Solid
Verwenden
Monastrol has been used:
- to treat MDA-MB-231 cells as a non-microtubule-targeting agent
- as a antineoplastic agent, to treat mouse myeloma cell line SP 2/0, to induce apoptosis and to elucidate the role of metabotropic glutamate receptor 3 (Grm3) in apoptosis
- as an inhibitor of pteridine reductase in GFP-transfected promastigotes infected macrophages for flow cytometer-based growth inhibition assay and to evaluate anti-leishmanial activity of Leishmania donovani hamster model in vivo
Verwenden
A cell-permeablesmall molecule inhibitor of the mitotic kinesin, Eg5, arrests cells in mitosis with monoastral spindles
Verwenden
Inhibitor of mammalian cell mitosis.
Definition
ChEBI: Monastrol is a racemate comprising equimolar amounts of R- and S-monastrol. It has a role as an antineoplastic agent, an EC 3.5.1.5 (urease) inhibitor, an antileishmanial agent and an antimitotic. It contains a (R)-monastrol and a (S)-monastrol.
Biologische Aktivität
Potent, cell-permeable, small molecule mitosis inhibitor that does not interact with tubulin. Arrests cells in mitosis and specifically inhibits the motility of the mitotic kinesin Eg5, a motor protein required for mitotic spindle formation and maintenance (IC 50 = 14 μ M).
Biochem/physiol Actions
Monastrol is a potent, cell-permeant inhibitor of mitosis. Monastrol arrested cells are characterized by monopolar spindles. This phenotype is induced through specific disruption of mitotic molecular motor kinesin Eg5 with IC50 at 14 μM. No effect on other motor proteins and tubulin.
Lager
Store at RT
Einzelnachweise
1) Mayer?et al. (1999), Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen; Science,?286?971 2) Kapoor?et al.?(2000),?Probing spindle assembly mechanisms with monastrol, a small molecule inhibitor of mitotic kinesin, Eg5; J. Cell Biol.,?150?975 3) Ari?et al.?(2014),?Alzheimer amyloid beta inhibition of Eg5/kinesin 5 reduces neurotrophin and/or transmitter receptor function; Neurobiol. Aging,?35?1839 4) Lin?et al. (2011),?Inhibition of Kinesin-5, a microtubule-based motor protein, as a strategy for enhancing regeneration of adult axons; Traffic,?12?269

MONASTROL Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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