MELK Inhibitor, OTSSP167 - Calbiochem

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; IC₅₀ = 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 (20 mg/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.

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; IC₅₀ = 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 (20 mg/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.

Cell permeable: yes

Primary Target
MELK

Reversible: yes

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Chung, S., et al. 2013. Cell Cycle.12, 1655.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)