MKI-1, an inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 of 9.9 μM, exerts antitumor and radiosensitizer activities through PP2A activation in breast cancer.
体外研究
MKI-1 (5-20 μM) inhibits the activity of MASTL in breast cancer cells.
MKI-1 (100 μM, 72 h) inhibits various oncogenic properties of breast cancer cells but showed much weaker effects on the viability of normal breast cells.
MKI-1 clearly reduces both serine 62-phosphorylation of c-Myc and total c-Myc, with a decrease in ENSA phosphorylation.
MKI-1 (20 μM, 16 h) reduces c-Myc stability through PP2A activation in MCF7 cells.
Western Blot Analysis
Cell Line:
MCF7 and T47D cells.
Concentration:
5-20 μM.
Incubation Time:
24 h.
Result:
Inhibited the phosphorylation of ENSA in MCF7 and T47D cells.
Significantly inhibited the phosphorylation of ENSA in mitotic cells.
体内研究
MKI-1 (50 mg/kg, ip, twice a week) reduces tumor growth and enhances the radiosensitivity of BT549 xenograft model in response to 6 Gy irradiation compared with the control group, with no notable changes in body weight, suggesting the absence of gross toxicity in the treated mice.