Allopole-A
Allopole-A is a Plk1 inhibitor with an IC50 of 1.4-2.5 μM against human Plk1 PBD1. Allopole-A binds to the allosteric W-F pocket in Plk1 PBD1, displacing the L2 loop, thereby disrupting water-mediated phospho-ligand binding interactions and promoting inhibitory interactions between the kinase domain and PBD to suppress Plk1 kinase activity. Allopole-A can be used in studies of human cancers with plk1 overexpression.
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- CAS No.: 3057557-03-3
- Formule: C11H9ClN4OS2
- Masse moléculaire:312.80
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
PLK1 PBD 1.4-2.5 μM (IC50) |
In Vitro
Allopole-A (2.5 μM; 30 min) displays strong specificity for inhibiting phosphopeptide binding to Plk1 PBD (PBD1) over PBD2 and PBD3, with an IC50 of 2.5 μM in the fluorescence polarization assay[1].
Allopole-A (20 min pre-incubation at 25 °C, followed by 30 min kinase reaction at 30 °C) directly inhibits the intrinsic catalytic activity of purified recombinant human Plk1 in an in vitro kinase assay[1].
Mutation of the Plk1 PBD1 residue F559 to charged residues completely abolishes Allopole-A's capacity to inhibit phosphopeptide binding to PBD1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3057557-03-3
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Masse moléculaire 312.80
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Formule C11H9ClN4OS2
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SMILES
S=C1NN=C(N1C2=C3SC(Cl)=C2)N(C3=O)CC4CC4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Allopole-A Related Classifications
HY-188141 Related Classifications
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