| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. Western Blot Analysis[1] Cell Line: | ||||||||||||
| 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]. Animal Model: | ||||||||||||
| Name | MKI-1 | ||||||||||||
| CAS | 1190277-80-5 | ||||||||||||
| Formula | C18H14N4O | ||||||||||||
| Molar Mass | 302.33 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |