The Polo-like Kinase Inhibitor V, Poloxin, also referenced under CAS 321688-88-4, controls the biological activity of Polo-like Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
A thymoquinone derivative, non-ATP competitive Polo-like Kinase 1 (Plk1) inhibitor specifically targeting the polo-box domain (PBD) of Plk1 (IC50) = 4.8 µM. Reduces both chromosome and kinetochoral localization of Plk1, induces chromosome congression defects , mitotic arrest in prometaphase, and apoptosis in HeLa cells at 25 µM. Exhibits anti-proliferative effects in a range of cancer cell lines, and in a mouse Xenograft model involving HeLa and MDA-MB-231 cells at 40 mg/kg.
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Reindl, W., et al. 2008. Chem Biol.15, 459. Yuan, J., et al. 2011, Am J Pathol179, 2091.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
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Journal of cellular physiology, 230(12), 3057-3067 (2015-05-16)
The expression of polo-like kinase 1 (Plk1) correlates with malignancy and is thus recognized as a target for cancer therapy. In addition to the development of ATP-competitive Plk1 inhibitors, the polo-box domain (PBD), a unique functional domain of PLKs, is
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