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Sigma-Aldrich

Eg5 Inhibitor III, Dimethylenastron

The Eg5 Inhibitor III, Dimethylenastron, also referenced under CAS 863774-58-7, controls the biological activity of Eg5. This small molecule/inhibitor is primarily used for Membrane applications.

Synonim(y):

Eg5 Inhibitor III, Dimethylenastron, 7,7-Dimethyl-4-(3-hydroxyphenyl)-5-oxo-3,4,5,6,7,8-hexahydroquinazolin-2(1H)-thione

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About This Item

Wzór empiryczny (zapis Hilla):
C16H18N2O2S
Numer CAS:
Masa cząsteczkowa:
302.39
Kod UNSPSC:
12352200
NACRES:
NA.77

Poziom jakości

Próba

≥95% (HPLC)

Postać

solid

producent / nazwa handlowa

Calbiochem®

warunki przechowywania

OK to freeze
protect from light

kolor

white to light yellow

rozpuszczalność

DMSO: 10 mg/mL
methanol: 5 mg/mL

Warunki transportu

ambient

temp. przechowywania

2-8°C

InChI

1S/C16H18N2O2S/c1-16(2)7-11-13(12(20)8-16)14(18-15(21)17-11)9-4-3-5-10(19)6-9/h3-6,14,19H,7-8H2,1-2H3,(H2,17,18,21)

Klucz InChI

RUOOPLOUUAYNPY-UHFFFAOYSA-N

Opis ogólny

A cell-permeable quinazoline-thione compound that acts as a potent, specific, and reversible inhibitor of the microtubule-stimulated ATPase activity of the mitotic motor, Eg5 (IC50 = 200 nM). Exhibits little effect on the ATPase activity of kinesin-1, -4, -7 and -10 and is ~100-fold more potent than Monastrol (Cat. No. 475879). Also inhibits bipolar spindle formation in both HeLa cells and in Xenopus egg extracts and induces cell cycle arrest (~1 µM). Shown to induce mitotic arrest and apoptosis and upregulate Hsp70 in human multiple myeloma cells.
A cell-permeable quinazoline-thione compound that acts as a potent, specific, and reversible inhibitor of the microtubule-stimulated ATPase activity of the mitotic motor, Eg5 (IC50 = 200 nM). Exhibits little effect on the ATPase activity of kinesin-1, -4, -7 and -10 and is ~100-fold more potent than Monastrol (Cat. No. 475879). Also inhibits bipolar spindle formation in both HeLa cells and in Xenopus egg extracts and induces cell cycle arrest (~1 µM). Shown to induce mitotic arrest and apoptosis and upregulate Hsp70 in human multiple myeloma cells.

Działania biochem./fizjol.

Cell permeable: yes
Primary Target
Microtubule-stimulated ATPase activity of the mitotic motor
Product does not compete with ATP.
Reversible: yes
Target IC50: 200 nM inhibiting the microtubule-stimulated ATPase activity of the mitotic motor, Eg5

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Harmful (C)

Rekonstytucja

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Inne uwagi

Liu, M., et al. 2006. J. Biol Chem.in press.
Gartner, M., et al. 2005. Chembiochem6, 1173.

Informacje prawne

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
This page may contain text that has been machine translated.

Kod klasy składowania

11 - Combustible Solids

Klasa zagrożenia wodnego (WGK)

WGK 3

Temperatura zapłonu (°F)

Not applicable

Temperatura zapłonu (°C)

Not applicable


Certyfikaty analizy (CoA)

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Proceedings of the National Academy of Sciences of the United States of America, 113(22), 6289-6294 (2016-05-18)
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