MASTL Inhibitor

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.

MASTL-IN-2 is an MASTL (microtubule-associated serine/threonine kinase-like) inhibitor. MASTL-IN-2 inhibits human epithelial MIA PaCa cancer cell proliferation with IC₅₀ of 2.8 nM.

MASTL-IN-1 is a selective and orally active MASTL inhibitor with a K_i <0.03 nM. MASTL-IN-1 inhibits phosphorylation of ENSA and inhibits proliferation in cancer cells. MASTL-IN-1 induces tumor growth inhibition and stasis in pancreatic cancer xenograft models.

MASTL-IN-4(compound 70) is a potent MASTL inhibitor with a pIC₅₀ value of 9.15. MASTL-IN-4 shows anti-proliferative activity.

MASTL/Aurora A-IN-1 (Compound MA4) is a dual inhibitor of MASTL and Aurora A kinases with IC₅₀ values of 0.56 μM and 0.16 μM, respectively. MASTL/Aurora A-IN-1 has broad-spectrum anticancer activity and has potent anticancer activity against SR (leukemia), K-562 (leukemia), MDA-MB-435 (melanoma), MOLT-4 (leukemia), and SK-MEL-2 (melanoma) cell lines in NCI-60 cancer cell lines with GI₅₀ values of 0.023, 0.032, 0.037, 0.044, and 0.051 μM, respectively. MASTL/Aurora A-IN-1 inhibits Aurora A and MASTL kinases, inducing cell cycle G2/M arrest, thereby inhibiting cancer cell proliferation. MASTL/Aurora A-IN-1 can be used in cancer research, especially for tumors with dysregulated mitosis.

MKI-2 is a selective MASTL inhibitor with an IC₅₀ of 37.44 nM. MKI-2 induces mitotic catastrophe resulting from the modulation of the MASTL-PP2A axis in breast cancer cells. MKI-2 reduces phospho-ENSA, total, phospho-c-Myc levels. MKI-2 inhibts cancer cells proliferation, migration and induces DNA damage. MKI-2 inhibits germinal vesicle breakdown in mouse oocytes. MKI-2 can be used for the research of cancer, such as breast cancer.

MKI-3 is a selective microtubule-associated serine/threonine kinase-like (MASTL) inhibitor with an IC₅₀ of 5.72 nM and a K_d of 1.89 nM. MKI-3 disrupts the MASTL-ENSA-Aurora A signaling axis. MKI-3 induces chromosomal instability, mitotic catastrophe and apoptosis (apoptosis) in cancer cells. MKI-3 is applicable to research related to triple-negative breast cancer.

MASTL-IN-3 (compound 60) is a potent MASTL inhibitor with a pIC₅₀ value of 9.10 M. MASTL-IN-3 shows anti-proliferative activity.