MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Poloppin

CAS No. : 683808-78-8

MCE 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.

相关产品：Wortmannin  |  GW843682X  |  LFM-A13  |  Poloxin  |  HMN-214  |  SBE13 Hydrochloride  |  TC-S 7005  |  Poloxime  |  Cyclapolin 9

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。