应用 |
A cell-permeable thiophene-benzimidazole compound and reversible PLK inhibitor |
产品介绍 |
GW843682X是PLK1和PLK3抑制剂,IC50分别为2.2 nM和9.1 nM,比对其它30种激酶的抑制性高超过100倍。 |
生化机理 |
Polo-like Kinase Inhibitor III (GW843682X) is a cell-permeable thiophene-benzimidazole compound that acts as a potent and reversible inhibitor against Plk (polo-like kinases) (Ki against Plk1/2/3/4 = 4.8, 3.8, 8.0, and 163 nM , respectively), while exhibiting little or much reduced activity against 39 other commonly studied kinases. Polo-like Kinase Inhibitor III preferentially inhibits the proliferation of a panel of 11 tumor cell lines (IC50 ≤0.7 μM) over normal human diploid fibroblasts (IC50 = 6.14 μM) in culture and is equally potent against the mdr-1-expressing MES-SA/DX5 and its parent non-drug resistant MES-SA uterine sarcoma cell line. |
别名 |
GW 843682X;GW843682;GW-843682X;3-(2-(三氟甲基)苄氧基)-5-(5,6-二甲氧基-1H-苯并(d)咪唑-1-基)-2-噻吩甲酰胺;;GW 843682X;GW843682;GW-843682X; 5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide ; 3-(2-(trifluoromethyl)benzyloxy)-5-(5,6-dimethoxy-1h-benzo(d)imidazol-1-yl)thiophene-2-carboxamide; polo-like kinase inhibitor iii |