产品描述:
Maternal embryonic leucine zipper kinase (MELK) is a serine/threonine kinase that regulates signaling central to cell cycling, stem cell renewal, apoptosis, and other cellular processes.{27684} MELK is overexpressed in some forms of cancer, particularly those with aggressive undifferentiated tumors.{27683,24926,24930} OTSSP167 is a potent inhibitor of MELK (IC50 = 0.41 nM).{27685} It suppresses the growth of diverse cancer cell lines at low nanomolar concentrations.{27685} It also blocks the phosphorylation of MELK-specific substrates and reduces the ability of MCF-7 breast cancer cells to invade and form spheroids in Matrigel.{27685} OTSSP167 is also effective in vivo when delivered either orally or intravenously, suppressing the growth of xenograft tumors in mice.{27685,27686}