中文名称:
2-甲基-5-(1-甲基乙基)-2,5-环己二烯-1,4-二酮 1-[O-(2-甲基苯甲酰)肟]
中文同义词:
2-甲基-5-(1-甲基乙基)-2,5-环己二烯-1,4-二酮 1-[O-(2-甲基苯甲酰)肟];POLO-LIKE KINASE1(PLK1)抑制剂(POLOXIN)
英文名称:
2-Methyl-5-(1-methylethyl)-2,5-cyclohexadiene-1,4-dione 1-[O-(2-methylbenzoyl)oxime]
英文同义词:
2-Methyl-5-(1-methylethyl)-2,5-cyclohexadiene-1,4-dione 1-[O-(2-methylbenzoyl)oxime];Poloxin;2-Methyl-5-(1-methylethyl)-1-[O-(2-methylbenzoyl)oxime]-2,5-Cyclohexadiene-1,4-dione;(Z)-2-Isopropyl-5-methyl-4-(((2-methylbenzoyl)oxy)imino)cyclohexa-2,5-dienone;Polo-like Kinase Inhibitor V, Poloxin;Polo-like Kinase Inhibitor V, Poloxin - CAS 321688-88-4 - Calbiochem;2,5-Cyclohexadiene-1,4-dione, 2-methyl-5-(1-methylethyl)-, 1-[O-(2-methylbenzoyl)oxime]
沸点
418.6±55.0 °C(Predicted)
溶解度
DMSO: soluble5mg/mL (clear solution, warmed)
生物活性
Poloxin 是一种 Polo-like Kinase 1 (PLK1) 的 ATP 非竞争性抑制剂，靶作用于 polo-box 结构域，IC50 值约为 4.8 μM。
靶点
PLK1 PBD
4.8 μM (IC 50 )
PLK2 PBD
18.7 μM (IC 50 )
PLK3 PBD
53.9 μM (IC 50 )
PLK1 PBD
4.8 μM (IC 50 )
PLK2 PBD
18.7 μM (IC 50 )
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 IC 50 of ∼4.8 μM. Poloxin exhibits a loose Plk1 PBD specificity with 4-10 times higher IC 50 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.
危险品运输编号
UN 3077 9 / PGIII
