MilliporeSigma™ Calbiochem™ MELK Inhibitor, OTSSP167

Description

• A cell permeable, orally bioavailable 1, 5-naphthyridine based compound that acts as a highly potent and specific inhibitor of maternal embryonic leucine zipper kinase (MELK; IC 50 = 410 pM)
• Inhibits mammospheres formation of MDA-MB-231 and MCF-7 cells by blocking MELK-dependent phosphorylation of proteasome subunit a1 (PSMA1)
• Also diminishes the phosphorylation of Ser269 on drebin-like (DBNL) in BT549 cells and reduces their invasiveness
• Suppresses the growth of xenografted MDA-MD-231 cells in a murine model (20mg/kg, once every 2 days for 14 days, i.v)
• Induces the formation of autophagosome-like vesicles in cytoplasm of BT549 breast cancer cells
• Also shown to suppress the growth of lung, pancreatic, and prostate cancer cells expressing high levels of MELK
• Please note that the molecular weight for this compound is batch-specific due to variable water content.