MKI-1

• CAT Number: I044659
• CAS Number: 1190277-80-5
• Molecular Formula: C18H14N4O
• Molecular Weight: 302.33
• Purity: ≥95%
• Synonyms: N-(1H-benzimidazol-2-yl)-3-pyrrol-1-ylbenzamide
• InChI: InChI=1S/C18H14N4O/c23-17(21-18-19-15-8-1-2-9-16(15)20-18)13-6-5-7-14(12-13)22-10-3-4-11-22/h1-12H,(H2,19,20,21,23)
• InChIKey: XKDZPQAMBMLCDQ-UHFFFAOYSA-N
• SMILES: C1=CC=C2C(=C1)NC(=N2)NC(=O)C3=CC(=CC=C3)N4C=CC=C4

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].

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.
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