MELK-T1 (JNJ-47117096) hydrochloride is a cell-permeable, potent and selective inhibitor of MELK kinase domain with IC50 of 37 nM.
MELK-T1 shows >50% inhibition at 1 uM against 6 kianses in a panel of 235 kinases (Flt3 IC50=18 nM);.
MELK-T1 triggers a rapid and proteasome-dependent degradation of the MELK protein, induces the accumulation of stalled replication forks and DSBs in MCF-7 cells.
MELK-T1 induces a strong phosphorylation of p53, a prolonged up-regulation of p21 and a down-regulation of FOXM1 target genes.
