Poloppin,683808-78-8

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Poloppin

CAS No. : 683808-78-8

MCE 国际站：Poloppin

产品活性：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 (K_d= 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。

研究领域：Cell Cycle/DNA Damage  |  Autophagy

作用靶点：Polo-like Kinase (PLK)  |  Autophagy

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 K_d of 29.5 μM.
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.
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.
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.

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