Poloxin 是一种 polo 样激酶 1 的 ATP 非竞争性抑制剂，靶向 polo-box 结构域，IC50值约为 4.8 μM。

Poloxin is a non-ATP competitive Polo-like Kinase 1 inhibitor. It targets the polo-box domain (IC50: appr 4.8 μM).

Poloxin inhibits proliferation in both cell lines with a comparable efficiency through a 72 h period. Poloxin inhibits the polo-box domain (PBD) interaction (apparent IC50: ～4.8 μM). Poloxin (25 μM) causes 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 shows 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[1][2][3].

Poloxin (40 mg/kg) reduces the proliferation of MDA-MB-231 cells. It also suppresses the growth of the tumor nude mice bearing established xenografts of MDA-MB-231[1].

321688-88-4

C18H19NO3

297.35

DMSO:14 mg/mL (43.72 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years