otssp167

Description: OTSSP167 (also known as OTS167) is a highly potent, orally bioavailable inhibitor of MELK (maternal embryonic leucine zipper kinase) with IC50 of 0.41 nM. OTSSP167 inhibits A549, T47D, DU4475, and 22Rv1 cancer cells, in which MELK is highly expressed, with IC50 values of 6.7, 4.3, 2.3, and 6.0 nM, respectively. OTSSP167 inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like), which are novel MELK substrates and are important for stem-cell characteristics and invasiveness. Since MELK is upregulated in a variety of human tumors, and is considered an attractive molecular target for cancer treatment.Thus, MELK promotes cell growth and invasiveness by inhibiting apoptosis and promoting G2/M transition and EMT in GC. These results suggest that MELK may be a promising target for GC treatment.

References: Oncotarget. 2012 Dec; 3(12):1629-40; Oncotarget. 2016 Feb 2; 7(5):6266-80.

Related CAS#: 1431698-10-0 (HCl); 1431697-89-0 (free base)