MRIA9 is an ATP-competitive, pan Salt-Inducible kinase (SIK) and PAK2/3 inhibitor, with IC 50 values of 516 nM, 180 nM and 127 nM for SIK1 , SIK2 and SIK3 , respectively
In Vitro
MRIA9 (5 μM) MRIA9 sensitizes SKOV3 cells to paclitaxel treatment through inducing pronounced apoptosis. MRIA9 (5 μM) with paclitaxel (2 nM) significantly enhances cell death in HeLa cells. MRIA9 strongly impedes centrosome function, causes mitotic spindle mispositioning in ovarian cancer cell lines, prevents the centrosome disjunction during the late G2 phase, and sensitized ovarian cancer cells and patient derived 3D-spheroids to paclitaxel treatment. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: SKOV3 cells. Concentration: 0.5-5 μM (1 nM paclitaxel). Incubation Time: 9 days. Result: Inhibited cell growth.
In Vivo
MRIA9 shows high oral bioavailability (F = 75-80%) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
