Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) inhibitor that targets the polo-box domain, with an IC50 of appr 4.8 μM.
IC50&Target
PLK1 PBD
4.8 μM (IC50)
PLK2 PBD
18.7 μM (IC50)
PLK3 PBD
53.9 μM (IC50)
体外研究
Poloxin (25 μM) induces defects in centrosome integrity, spindle formation, and chromosome alignment in mitosis. Centrosomal fragmentation induced by Poloxin is partially rescued by Kiz T379E. Poloxin (25 μM) activates the mitotic checkpoint, induces apoptosis and inhibits proliferation of MDA-MB-231 cells. Poloxin inhibits proliferation in both cell lines with a comparable efficiency through 72 h period. Poloxin inhibits the polo-box domain (PBD) interaction with an apparent IC50 of ∼4.8 μM. Poloxin exhibits a loose Plk1 PBD specificity with 4-10 times higher IC50 values for Plk2 and Plk3, and does not significantly inhibit other types of phosphopeptide-binding domains such as FHA, WW, and SH2 domains.
体内研究
Poloxin (40 mg/kg) decreases the proliferation of MDA-MB-231 cells, and surpresses the growth of the tumor nude mice bearing established xenografts of MDA-MB-231.
分子式
C18H19NO3
分子量
297.35
CAS号
321688-88-4
运输条件
Room temperature in continental US; may vary elsewhere.