Allopole-A | PLK1 PBD inhibitor | Probechem Biochemicals

Chemical Structure : Allopole-A

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Allopole-A (PLK1 PBD inhibitor)

货号: PC-21080Not For Human Use, Lab Use Only.

Allopole-A is the first allosteric, specfic inhibitor of the noncatalytic polo-box domain (PBD) of PLK1 (Polo-like kinase 1) with IC50 of 2.5 nM in FP-based assays, Allopole-A is the active form of Allopole.

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生物&药学活性

Allopole-A is the first allosteric, specfic inhibitor of the noncatalytic polo-box domain (PBD) of PLK1 (Polo-like kinase 1) with IC50 of 2.5 nM in FP-based assays, Allopole-A is the active form of Allopole.
Allopole-A displays no binding affinity for Plk2 and Plk3.
Both F559 and W410 are critical for Allopole-A's Plk1-binding specificity, mutation of Plk1 F559 confers resistance to allopole.
Allopole-A binds to the allosteric W-F pocket occluded by the L2 loop dislodges the loop, consequently stripping several water-mediated interactions critical for phosphoepitope binding.
Allopole-A is sufficient to trigger the dissociation of a phospholigand and to inhibit PBD1-dependent downstream events.
Allopole-A has low cell membrane permeability.

物理化学性质&存储条件

分子量	312.79
分子式	C11H9ClN4OS2
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-thioxo-2,4-dihydrothieno[2,3-e][1,2,4]triazolo[4,3-a]pyrimidin-5(1H)-one

参考文献

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