PLK1
PLK1 is a serine/threonine Polo-like kinase that orchestrates cell division through mitotic entry, spindle-pole functions, and cytokinesis[1]. Mechanistically, mammalian PLK1 controls centrosome maturation, spindle assembly, and microtubule attachment to kinetochores in early mitosis[2]. This mitotic role makes PLK1 relevant to cancer biology, because dysfunction may promote cancerous transformation and drive progression, and overexpression occurs in diverse human cancers with poor prognosis[3]. Compared with related isoforms, PLK1-PLK4 participate in cell-cycle processes, but reported functional emphasis differs: PLK2 and PLK4 regulate centriole duplication, PLK3 regulates DNA replication, and PLK1 regulates centrosome separation and maturation[4]. For experimental applications, PLK1 inhibition provides a direct way to perturb mitosis, because BI 2536 inhibits mammalian PLK1 at low nanomolar concentrations, induces mitotic arrest and apoptosis in human cancer cell lines, and inhibits human tumor xenograft growth in nude mice[5].
References:
- [1]. Barr FA, et al. Polo-like kinases and the orchestration of cell division. Nat Rev Mol Cell Biol. 2004 Jun;5(6):429-40. [Content Brief]
- [2]. Santamaria A, et al. The Plk1-dependent phosphoproteome of the early mitotic spindle. Mol Cell Proteomics. 2011 Jan;10(1):M110.004457. [Content Brief]
- [3]. Liu Z, et al. PLK1, A Potential Target for Cancer Therapy. Transl Oncol. 2017 Feb;10(1):22-32. [Content Brief]
- [4]. de Cárcer G, et al. From Plk1 to Plk5: functional evolution of polo-like kinases. Cell Cycle. 2011 Jul 15;10(14):2255-62. [Content Brief]
- [5]. Steegmaier M, et al. BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo. Curr Biol. 2007 Feb 20;17(4):316-22. [Content Brief]
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PLK1 Related Products (63)
Related Products (63)
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Antibodies (3)
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BDE30671203
0 ImagesCat. No.: HY-181030BDE30671203 is a highly selective PLK1 inhibitor (IC50 = 2.163 nM). BDE30671203 induces G2/M phase arrest and Apoptosis. BDE30671203 downregulates key cell cycle regulators (CDC20, CDK1) and the anti-apoptotic gene Bcl-2. BDE30671203 exhibits anticancer activity against non-small cell lung cancer, large cell lung cancer, and liver cancer.
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TAK-960 hydrochloride
0 ImagesCat. No.: HY-15160ACAS No.: 1137868-96-2TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
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KBJK557
0 ImagesCat. No.: HY-183427CAS No.: 2660138-04-3KBJK557 is a Plk1 PBD inhibitor with a human-derived IC50 value of 3.05 μM. KBJK577 binds to Plk1 PBD through electrostatic interactions, π-π stacking, hydrogen bonds, salt bridges and hydrophobic interactions, thereby disrupting the subcellular localization and function of Plk1. KBJK557 induces mitotic arrest, S-phase delay, G2/M-phase arrest and apoptosis, and inhibits cancer cell proliferation. KBJK557 can be used in research related to cancer and non-small cell lung cancer.
