MKI-1 是微管相关丝氨酸/苏氨酸样激酶 (MASTL) 的抑制剂，其IC50 为9.9 μM。MKI-1 通过激活乳腺癌中的PP2A 发挥抗肿瘤和放射增敏活性。
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[1].
MKI-1 (5-20 μM) inhibits the activity of MASTL in breast cancer cells[1].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[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 μM, 16 h) reduces c-Myc stability through PP2A activation in MCF7 cells[1].
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].
[1]. Ah-Young Kim, et al. MKI-1, a Novel Small-Molecule Inhibitor of MASTL, Exerts Antitumor and Radiosensitizer Activities Through PP2A Activation in Breast cancer. Front Oncol. 2020 Sep 29;10:571601.
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