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324622

Eg5 Inhibitor III, Dimethylenastron

Name: Eg5 Inhibitor III, Dimethylenastron
Brand: MM

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.

别名:

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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关于此项目

经验公式（希尔记法）:

C₁₆H₁₈N₂O₂S

化学文摘社编号:

863774-58-7

分子量:

302.39

MDL number:

MFCD09264157

UNSPSC Code:

12352200

NACRES:

NA.77

Assay:

≥95% (HPLC)

Form:

solid

Storage condition:

OK to freeze, protect from light

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属性

Quality Segment

100

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

white to light yellow

solubility

DMSO: 10 mg/mL, methanol: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

S=C1NC(C3=C(N1)CC(CC3=O)(C)C)c2cc(ccc2)O

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)

InChI key

RUOOPLOUUAYNPY-UHFFFAOYSA-N

说明

General description

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.

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Preparation Note

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

Other Notes

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Harmful (C)

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c