MASTL/Aurora A-IN-1 (Compound MA4) is a dual inhibitor ofMASTLandAurora Akinases withIC50values of 0.56 μM and 0.16 μM, respectively. MASTL/Aurora A-IN-1 has broad-spectrumanticanceractivity and has potentanticanceractivity against SR (leukemia), K-562 (leukemia), MDA-MB-435 (melanoma), MOLT-4 (leukemia), and SK-MEL-2 (melanoma) cell lines in NCI-60cancercell lines withGI50values of 0.023, 0.032, 0.037, 0.044, and 0.051 μM, respectively. MASTL/Aurora A-IN-1 inhibitsAurora AandMASTLkinases, inducing cell cycle G2/M arrest, thereby inhibitingcancercell proliferation. MASTL/Aurora A-IN-1 can be used incancerresearch, especially for tumors with dysregulatedmitosis[1].
References:
[1].Abdel-Rahman SA, Nada H, Gabr MT. First-in-class dual inhibitors of MASTL and Aurora A kinase: Discovery of selective cyclohexa[b]thiophenes with potent anticancer activity. Eur J Med Chem. 2025 May 8;293:117729.