OTS514

Description: OTS514 is a novel and highly potent inhibitor of the TOPK (T-LAK cell-originated protein kinase) with an IC50 value of 2.6 nM. It strongly suppressed the growth of TOPK-positive cancer cells. It also shows significant growth-inhibitory effect on ovarian cancer cell lines with IC50 values of 3.0 to 46 nM. OTS514 displays growth inhibitory effects against small cell lung cancer with IC50 in the range of 0.4 ca. 42.6 nM and can lead to their apoptotic cell death. OTS514 also suppressed forkhead box protein M1 (FOXM1) activity, a protein involved in stemness of CSC. Furthermore, treatment with OTS514 reduced CD90-positive SCLC cells and exhibited higher cytotoxicity against lung sphere-derived CSC-like SCLC cells.

References: Clin Cancer Res. 2016 Dec 15; 22(24):6110-6117.

Related CAS #: 1338544-87-8 (HBr) 1338540-63-8 (free base) 1338541-25-5 (s-isomer) 1338545-92-8 (S-isomer HCl)