SBE13 HCl is a potent and selective PLK1 inhibitor with IC50 of 0.2 nM while 875 nM and 66 μM for PLK3 and PLK2. SBE 13 could also induce cell cycle arrest, reduce cell proliferation with EC50 of 5-60 µM, and induce apoptosis in a broad range of human cancer cell lines.
Human polo-like kinase 1 (Plk1), a key regulator of mitosis, is over-expressed in various human tumors. It is a negative prognostic factor for cancer patients and a measure for the aggressiveness of a tumor. SBE13 (10 and 100 μM) reduces pRb staining in primary cells, and this indicates a G0/G1 arrest. After treatment with SBE13 the G₁//S checkpoint was intact, indicated by reduced pRb, resulting in slower cell cycle progression but overall cell proliferation was not significantly impaired[3].SBE13 Hydrochloride is a potent and selective Plk1 inhibitor, with an IC50 of 200 pM. SBE13 significantly reduce cell proliferation and induce apoptosis in HeLa cells, with an EC50 of 18 μM[4]. SBE13 (66 and 100 μM) increases levels of cyclin B1, phospho histone H3, Wee1, Emi1 and securin, and results in cleavage of Cdc27 in HeLa cells. Decreased cell proliferation, delayed progression through the cell cycle in lower SBE13 concentrations, a G(2)/M arrest using higher SBE13 concentrations followed by apoptosis, and abnormal mitotic figures[5].
搜索
