Allopole | PLK1 PBD inhibitor | Probechem Biochemicals

Chemical Structure : Allopole

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Allopole (PLK1 PBD inhibitor)

货号: 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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100 mg		Get quote
200 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	437.88
分子式	C15H12ClN7O3S2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	7-chloro-4-(cyclopropylmethyl)-1-((1-methyl-4-nitro-1H-imidazol-5-yl)thio)thieno[2,3-e][1,2,4]triazolo[4,3-a]pyrimidin-5(4H)-one

参考文献

1. Park JE, et al. Proc Natl Acad Sci U S A. 2023 Aug 29;120(35):e2305037120.