Poloppin

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Poloppin 

Poloppin 是一种有效的细胞渗透抑制剂，可抑制有丝分裂的 polo 样激酶 (PLK) (IC50=26.9 μM)，并可通过Polo-box 结构域 (PBD) 阻止蛋白之间的相互作用 (Kd= 29.5 μM)。Poloppin 选择性地杀死表达突变 KRAS 的细胞，增强有丝分裂中的死亡。Poloppin 可用作 KRAS 突变型癌症的研究，可作为单一试剂，或与 c-MET 抑制剂联合使用。

Poloppin

Poloppin Chemical Structure

CAS No. : 683808-78-8

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生物活性

Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC50=26.9 μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (Kd= 29.5 μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis. Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors[1].
IC50 & Target

IC50: 26.9 μM (mitotic Polo-like kinase (PLK))
Kd: 26.9 μM (protein-protein interaction via the Polo-box domain (PBD))[1]
体外研究
(In Vitro)

Poloppin (0-200 μM) competitively inhibits the binding of a TAMRA-labeled substrate peptide to the PLK1 PBD, exhibiting an IC50 value of 26.9 μM in an FP assay; the isothermal titration calorimetry of Poloppin binding to the PBD domain of PLK1 with a Kd of 29.5 μM[1].
Poloppin (0-100 μM) triggers a dose-dependent mitotic arrest and induces multiple anomalies in mitosis in cells, the EC50 value is 29.9 μM. In representative images of U2OS cells with 12.5 μM Poloppin, <5% of cells exhibit normal metaphase chromosome alignment, and shows bipolar or disordered spindles and non-congressed chromosomes in cells[1].
Poloppin (0-200 μM; 24 hours) inhibits SW48 isogenic parental or KRAS G12D cells growth with GI50 values of 13.7 μM and 5.3 μM, respectively. It inhibits KRAS wild-type p53 and KRAS MUT p53 MEFs cells with GI50 values of 51.1 and 49.5 μM, respectively. When the medium is added 500nM 4-OH Tamoxifen to the culture media overnight, Poloppin inhibits KRAS wild-type p53 and KRAS MUT p53 MEFs cells with GI50 values of 43.7 μM and 17.6 μM, respectively[1].
Poloppin (0-10 μM; 72 hours) sensitizes mutant KRAS-expressing cells to inhibitors of the c-MET tyrosine kinase. SW48 cell bearing mutant KRAS are sensitized to Poloppin after inhibition of c-MET, the GI50 values of Poloppin combination with Crizotinb (HY-50878) are 0.23 uM and 0.08 uM, respectively in SW48 KRAS WT and KRAS G12D cells. In the contrast, the GI50 values are 0.56 uM and 0.63 uM in SW48 KRAS WT or KRAS MUT cells when treated with Crizotinib alone[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: SW48 isogenic parental or KRAS G12D cells
Concentration: 0-200 μM
Incubation Time: 24 hours
Result: Inhibited cell growth expressing mutant KRAS in two-dimensional and organoid Cultures.

Cell Cytotoxicity Assay[1]

Cell Line: SW48 isogenic parental or KRAS G12D cells
Concentration: 0-200 μM
Incubation Time: 24 hours
Result: Selectively increased sensitization of mutant KRAS-expressing cells to inhibitors of the c-MET tyrosine kinase.

分子量

438.24

Formula

C20H15BrF3NO2
CAS 号

683808-78-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Ana J Narvaez, et al. Modulating Protein-Protein Interactions of the Mitotic Polo-like Kinases to Target Mutant KRAS. Cell Chem Biol. 2017 Aug 17;24(8):1017-1028.e7.

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