MRIA9 is a potent, selective dual SIK/PAK inhibitor, inhibits SIK1/2/3 with cellular IC50 of 586/180/127 nM, respectively.
MRIA9 displays excellent selectivity in scanMAX kinase assay panel of 468 kinases.
MRIA9 sensitizes ovarian cancer cells to treatment with the mitotic agent paclitaxel.
MRIA9-induced inhibition of SIK2 blocks the centrosome disjunction, impairs the centrosome alignment, and causes spindle mispositioning during mitosis.
MRIA9 increases chromosomal instability in ovarian cancer cell lines.
