Poloxin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Poloxin 是一种非 ATP 竞争性 Polo 样激酶 1 抑制剂。它针对 polo-box 结构域（IC50：约 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 (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.

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.

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Cell Cycle/DNA Damage

PLK

PLK1|PLK2|PLK3

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321688-88-4

297.35

C18H19NO3

>98% (HPLC)

DMSO:14 mg/mL (43.72 mM; Need ultrasonic)

CC(C)C(C(C=C1C)=O)=C/C1=N/OC(c1c(C)cccc1)=O

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(-20℃)

With Ice Pack

≥ 2 years