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Centrinone LCR-263

Centrinone (LCR-263) 是选择性,可逆的 PLK4 抑制剂,Ki 值为 0.16 nM。

  • 货号:
    TK0635
  • 规格:
    2mg
    5mg
  • 价格:
    0.00

产品参数

CAS No.1798871-30-3
生物活性Centrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 (PLK4) with a Ki of 0.16 nM.
分子式C26H25F2N7O6S2
分子量633.65
运输条件Room temperature in continental US; may vary elsewhere.
储存条件 Powder -20°C 3 years
溶解性数据DMSO : ≥ 31 mg/mL (48.92 mM)
体外研究Centrinone (LCR-263) exhibits more than 1000-fold selectivity for Plk4 over Aurora A/B and does not affect cellular Aurora A or B substrate phosphorylation at concentrations that deplete centrosomes. Centrinone (LCR-263) treatment of HeLa human cervical carcinoma cells leads to a progressive reduction in foci containing centriolar and pericentriolar material markers at each round of cell division, until most cells lack centrioles and centrosomes. Treatment with Centrinone (LCR-263) reduces centriole number in multiciliated Xenopus epithelial cells, which indicates that Plk4 also controls centriole amplification in differentiated cells. Centrinone (LCR-263) treatment causes centrosome depletion in human and other vertebrate cells. Centrosome loss irreversibly arrests normal cells in a senescence-like G1 state by a p53-dependent mechanism that is independent of DNA damage, stress, Hippo signaling, extends mitotic duration, or segregation errors.
文献•Nat Cell Biol. 2019 Dec;21(12):1544-1552. •Nat Commun. 2019 Apr 18;10(1):1810. •EMBO J. 2020 Jan 15;39(2):e102378. •J Cell Biol. 2019 Nov 4;218(11):3537-3547. •Elife. 2021 Jan 25;10:e62640. •Int J Mol Sci. 2021 Sep 7;22(18):9680. •J Cancer Res Clin Oncol. 2020 Nov;146(11):2871-2883. •Biol Open. 2019 Sep 18;8(9):bio047175. •University of Zürich. Department of Dermatology. 2021 Dec. • Combined Faculty of Natural Sciences and Mathematics of the Ruperto Carola University Heidelberg
纯度及产品资料95%