GW 843682X是一种PLK抑制剂，作用于PLK1和PLK3时， IC50分别为2.2 nM何9.1 nM。GW 843682X是一种能加入培养基中抑制大多数肿瘤细胞增殖的亚微摩尔级抑制剂，但是无法抑制前列腺癌细胞系PC-3的增殖。对比正常二倍体成纤维细胞(HDF)来说GW 843682X对肿瘤细胞具有选择性抑制，这种抑制效果比正常二倍体成纤维细胞(HDF)强10倍多。GW 843682X(约200 nM)对MES-SA/DX5和亲本系MES-SA效果一样，说明该化合物没有被细胞内P-糖蛋白外排泵有效排出细胞。

>98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

GW843682

类白色粉末

10 mM in DMSO

Polo-like Kinase (PLK)

GW843682X (compound 1) is effective on inhibition of growth of tumor cells, with IC50s of 0.41, 0.57, 0.11, 0.38, and 0.70 μM for A549, BT474, HeLa, H460 and HCT116 cell lines. GW843682X dose-dependently inhibits PLK1 phosphorylation of Ser15-p53, with an IC50 of 0.14 μM. GW843682X (3 μM) causes a strong G2-M arres in HDF cells and H460 cells after treatment for 24, 48, and 72 h. GW843682X (5 μM) leads to apoptosis in H460 cells instead of HDF cells. GW843682X inhibits proliferation of U937 cells with an EC50 of 120 nM. GW843682X (500 nM) in combination with 5 µM VP-16 suppresses 50% of entry into mitosis in U937 cells. GW843682X (0.06-1 μM) has inhibitory activities against proliferation of acute leukemia cells, and potentiates the anti-proliferative activity of vincristine. Moreover, GW843682X (0.1-1 μM) induces apoptosis of leukemia cells in a dose- and time-dependent manner. GW843682X (0.5-1 μM) dephosphorylates Bcl-xl in leukemia cells.