Dimethylenastron

Description: Dimethylenastron, a quinazoline-thione analog, is a potent, cell-permeable, specific, and reversible mitotic kinesin 5 (Eg5) inhibitor with IC50 of 200 nM. Eg5 is the the mitotic motor of microtubule-stimulated ATPase activity. As an Eg5 Inhibitor III, Dimethylenastron has potential anticancer activity and shows little effect on the ATPase activity of kinesin-1, -4, -7 and -10. Dimethylenastron also inhibits bipolar spindle formation in both HeLa cells and in Xenopus egg extracts and induces cell cycle arrest (ca.1 uM). Dimethylenastron (3 and 10 uM) concentration-dependently suppresses the migratory ability of the cancer cells in PANC1 pancreatic cancer cells after treatment for 24 h, but does not inhibit the proliferation of cancer cells at 24 h until 72 h. Dimethylenastron also reduces invasion ability of the cancer cells.

References: Acta Pharmacol Sin. 2011 Dec; 32(12):1543-8; Curr Eye Res. 2010 Dec; 35(12):1090-8.