RAD51 Inhibitor B02 specifically inhibits human RAD51 (IC
50
=27.4 μM), but not its
E. coli
homologue RecA (IC
50
>250 μM). The combination of B02 with cisplatin has the strongest killing effect on the human breast cancer cells MDA-MB-231.
B02 significantly enhances the therapeutic effect of cisplatin on tumor cells
in vivo
. B02 is tolerated by mice at doses up to 50 mg/kg without obvious body weight loss. No inhibition of tumor growth is observed on mice solely treated by B02. Mice treated with 4 mg/kg cisplatin, however, shows a 33% inhibition of tumor growth. Finally, mice treated with 50 mg/kg B02 and 4 mg/kg cisplatin shows a 66% inhibition of tumor growth.
