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MKI-1 (Synonyms: MASTL Kinase Inhibitor-1)

Cat. No.: HY-137552
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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.

For research use only. We do not sell to patients.

MKI-1 Chemical Structure

MKI-1 Chemical Structure

CAS No. : 1190277-80-5

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Description

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].

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

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.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Five-week-old female BALB/c nude mice (BT549 cells)[1].
Dosage: 50 mg/kg.
Administration: Twice per week by intraperitoneal (i.p.) injection.
Result: Reduced tumor growth.
Molecular Weight

302.33

Formula

C₁₈H₁₄N₄O

CAS No.

1190277-80-5

SMILES

O=C(NC1=NC2=CC=CC=C2N1)C3=CC=CC(N4C=CC=C4)=C3

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

MKI-1MASTL Kinase Inhibitor-1MKI1MKI 1MASTL Kinase Inhibitor1MASTL Kinase Inhibitor 1OthersMASTLbreastcancerPP2AMCF7T47DBT549lowtoxicityInhibitorinhibitorinhibit

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