NSC 689534 can form copper chelate with Cu2+. NSC 689534/Cu2+ complex is a potent oxidative stress inducer, and has antitumor activity.
NSC 689534/Cu2+ complex (48 h) inhibits cell viability of HL60 and PC3 cell with IC50s of 0.2 and 0.4 μM respectively, which is about 4 times more potent than NSC 689534 alone[1].NSC 689534/Cu2+ complex (2.5 μM, 24 h) induces oxidative stress and depletes GSH in PC3 cells, whereas with no effect by NSC 689534 alone[1].NSC 689534/Cu2+ complex (2.5 μM, 24 h) induces macroautophagy (indicated by LC3 accumulation into large autophagosomes) and an ER-stress response (upregulation of GRP78 and CHOP) in PC3 cells[1].
NSC 689534/Cu2+ complex (3 mg/kg, i.p., once or twice a day for 5 days) inhibits tumor growth in HL60 xenograft model, whereas with no statistical significance by NSC 689534 alone[1].
References:
[1]. Chad N Hancock, et al. A copper chelate of thiosemicarbazone NSC 689534 induces oxidative/ER stress and inhibits tumor growth in vitro and in vivo. Free Radic Biol Med. 2011 Jan 1;50(1):110-21.
[2]. Hancock CN, et al. A copper chelate of thiosemicarbazone NSC 689534 induces oxidative/ER stress and inhibits tumor growth in vitro and in vivo. Free Radic Biol Med. 2011 Jan 1;50(1):110-21.