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MELK-In-7
- Development stage
- Preclinical
- Lead developer
- University of Texas at Austin
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
MELK-In-7 (also known as MELK-IN-17 or MELK-IN-1) is a selective, small-molecule inhibitor of maternal embryonic leucine zipper kinase (MELK), developed through a collaboration between the University of Texas at Austin and MD Anderson Cancer Center. MELK is a serine/threonine kinase that is overexpressed in various aggressive malignancies, including triple-negative breast cancer (TNBC) and glioblastoma multiforme, where it plays a critical role in promoting cancer stem-like cell (CSC) maintenance, epithelial-to-mesenchymal transition (EMT), and tumor metastasis. By targeting MELK, MELK-In-7 suppresses cell proliferation, migration, invasion, and mammosphere formation in TNBC cells, and has demonstrated dose-dependent tumor growth inhibition in preclinical mouse models.
- Other names
- MELK inhibitor 17Methyl (Z)-3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-5-carboxylateNintedanib Impurity Linhibitor 17inhibitor17inhibitor-17
02
Targets
CAMK2G (Calcium/calmodulin-dependent protein kinase II gamma chain)CAMK2D (Calcium/calmodulin-dependent protein kinase II delta)FLT3 (Fms related receptor tyrosine kinase 3)MKNK2 (MAP kinase-interacting serine/threonine-protein kinase 2)MELK (Maternal embryonic leucine zipper kinase)MLCK (Myosin light chain kinase)
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