ARN-3236 (ARN3236) is a novel potent, selective, and orally active SIK2 inhibitor with IC50 of <1 nM.
ARN-3236 does not significantly inhibit SIK1 and SIK3, as well as other AMPK family members.
ARN-3236 inhibits the growth of 10 ovarian cancer cell lines with IC50 of 0.8-2.6 uM.
ARN-3236 increasess centrosome uncoupling from nucleus, and inhibits centrosome splitting in mitotic cells.
ARN-3236 induces cell cycle arrest, apoptosis and tetraploidy, also inhibits AKT phosphorylation and attenuates survivin expression.
ARN-3236 sensitizes ovarian cancer to paclitaxel in SKOv3ip xenograft model.
