Suprafenacine is an inhibitor of tubulin polymerization (IC50 = 0.38 μM) with anticancer activity.1 It inhibits the proliferation of HeLa, Jurkat, SNU-16, MDA-MB-231, A549, SH-SY5Y, HCT15, and KB-3-1 cells (IC50s = 83-381.2 nM) and P-glycoprotein-enriched KB-VI cells (IC50 = 215.7 nM). Suprafenacine (10 μM) increases phosphorylation of JNK and Bcl-2 and induces apoptosis and cell cycle arrest at the G2/M phase in HeLa cells. Suprafenacine (20 mg/kg) reduces tumor growth in an HCT15 colon adenocarcinoma mouse xenograft model.
1.Choi, B.-H., Chattopadhaya, S., Thanh, L.N., et al.Suprafenacine, an indazole-hydrazide agent, targets cancer cells through microtubule destabilizationPLoS One9(10)e110955(2014)