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SBE13 HCl

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Chemical Structure| 1052532-15-6 同义名 : SBE 13 (hydrochloride);SBE13 Hydrochloride;SBE13
CAS号 : 1052532-15-6
货号 : A527359
分子式 : C24H28Cl2N2O4
纯度 : 98%
分子量 : 479.396
MDL号 : MFCD20036266
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(219.03 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 5 mg/mL(10.43 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • PLK1

    PLK1, IC50:200 pM
描述 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.43mL

2.09mL

1.04mL

20.86mL

4.17mL

2.09mL
参考文献

[1]Keppner S, Proschak E, et al. Fate of primary cells at the G₁/S boundary after polo-like kinase 1 inhibition by SBE13. Cell Cycle. 2011 Feb 15;10(4):708-20.

[2]Keppner S, Proschak E, et al.Biological impact of freezing Plk1 in its inactive conformation in cancer cells. Cell Cycle. 2010 Feb 15;9(4):761-73.

[3]Keppner S, et al. Fate of primary cells at the G1/S boundary after polo-like kinase 1 inhibition by SBE13. Cell Cycle. 2011. 10(4),708-20.

[4]Keppner S, et al. Identification and validation of a potent type II inhibitor of inactive polo-like kinase 1. ChemMedChem. 2009. 4(11), 1806-9.

[5]Sarah Keppner,et al. Biological impact of freezing Plk1 in its inactive conformation in cancer cells. Cell Cycle. 2010. 9(4), 761-73.