Decreases CRTC3 and HDAC4 phosphorylation in macrophages
Enhances sensitivity of eight ovarian cancer cell lines to paclitaxel
Stops cell cycle at G2/M phase
Triggers apoptosis and tetraploidy in SKOV3 cells
Boasts additive tumor reduction when paired with paclitaxel in ovarian cancer mouse model
Description
A SIK2 inhibitor (IC50 ~21.63 and 6.33 nM) that suppresses TNF-a secretion in RAW 264.7 cells (IC50 ~2.5 µM) and reduces CRTC3 and HDAC4 phosphorylation in macrophages at 3 µM. It inhibits growth of 10 ovarian cancer cell lines (IC50s 0.8-2.6 µM) and enhances sensitivity to paclitaxel in eight of them. Halts cell cycle at G2/M phase and induces apoptosis and tetraploidy in SKOV3 cells at 1 µM. Shows additive tumor reduction when combined with paclitaxel in ovarian cancer mouse models at 60 mg/kg per day.