MKI-1

1190277-80-5

302.33

10 mM in DMSO

Others

MKI-1, an inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC₅₀ of 9.9 uM, exerts antitumor and radiosensitizer activities through PP2A activation in breast cancer^[1]. In Vitro: MKI-1 (5-20 uM) inhibits the activity of MASTL in breast cancer cells^[1].
MKI-1 (100 uM, 72 h) inhibits various oncogenic properties of breast cancer cells but showed much weaker effects on the viability of normal breast cells^[1].
MKI-1 clearly reduces both serine 62-phosphorylation of c-Myc and total c-Myc, with a decrease in ENSA phosphorylation^[1].
MKI-1 (20 uM, 16 h) reduces c-Myc stability through PP2A activation in MCF7 cells^[1].
In Vivo: 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^[1].