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.
性状
Solid
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
MRIA9 shows high oral bioavailability (F = 75-80%). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Roberta Tesch, et al. Structure-Based Design of Selective Salt-Inducible Kinase Inhibitors. J Med Chem. 2021 Jun 24;64(12):8142-8160.[2]. Monika Raab, et al. The Small-Molecule Inhibitor MRIA9 Reveals Novel Insights into the Cell Cycle Roles of SIK2 in Ovarian Cancer Cells. Cancers 2021, 13(15), 3658.
溶解度数据
In Vitro: DMSO : 66.67 mg/mL (134.17 mM; Need ultrasonic)配制储备液