Eg5 Inhibitor III, Dimethylenastron-CAS 863774-58-7-Calbiochem

C₁₆H₁₈N₂O₂S

302.39

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.

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

Toxicity: Harmful (C)

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

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

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

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

light yellow

DMSO: 10 mg/mL
methanol: 5 mg/mL

ambient

2-8℃

1, 5 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 3