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Chemical Structure : Allopole
Catalog No.: PC-21081Not For Human Use, Lab Use Only.
Allopole is the first allosteric, specfic and cell-permeable inhibitor of the noncatalytic polo-box domain (PBD) of PLK1 (Polo-like kinase 1), Allopole is the prodrug of Allopole-A.
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Allopole is the first allosteric, specfic and cell-permeable inhibitor of the noncatalytic polo-box domain (PBD) of PLK1 (Polo-like kinase 1), Allopole is the prodrug of Allopole-A.
Allopole converted rapidly into the active Allopole-A form (presumably by intracellular GSH) and antagonized the PBD1 function.
Allopole-A displays no binding affinity for Plk2 and Plk3.
Allopole inhibited PLK1 PBD (PBD1)-dependent interactions and subcellular localizations, consequently inducing mitotic block in HeLa cells.
Allopole shows anti-cell-proliferation activity with a 50% cell growth inhibition (GI50) value of 4.1 μM in multiple myeloma-derived L363 cells.
| M.Wt | 437.88 | |
| Formula | C15H12ClN7O3S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Park JE, et al. Proc Natl Acad Sci U S A. 2023 Aug 29;120(35):e2305037120.
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