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MKI-1

CAS No. : 1190277-80-5

產品活性：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.

研究領域：Others

作用靶點：Others

In Vitro: 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.

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.

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