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Art. -Nr.: HY-188141

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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. Nr.: 3057557-03-3
Formel: C₁₁H₉ClN₄OS₂
Molecular Weight:312.80

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Please store the product under the recommended conditions in the Certificate of Analysis.

Allopole-A Chemical Structure

CAS. Nr.: 3057557-03-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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Beschreibung

IC₅₀ & Target

^[1]

PLK1 PBD

1.4-2.5 μM (IC₅₀)

Alle Polo-like Kinase (PLK) Isoform-spezifische Produkte anzeigen :

In Vitro

Allopole-A inhibits PBD1-dependent phosphopeptide binding to full-length Plk1 with an IC₅₀ of 1.4 μM in the ELISA-based assay^[1].
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.

Related Protocols :

Chemical Information

CAS. Nr. 3057557-03-3
Molecular Weight 312.80
Formel C₁₁H₉ClN₄OS₂
SMILES

S=C1NN=C(N1C2=C3SC(Cl)=C2)N(C3=O)CC4CC4
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Park JE, et al. Specific inhibition of an anticancer target, polo-like kinase 1, by allosterically dismantling its mechanism of substrate recognition. Proceedings of the National Academy of Sciences of the United States of America. 2023 Aug 29;120(35):e2305037120.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Allopole-A

Alle Polo-like Kinase (PLK) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

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IC50 & Target

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Chemical Information

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Allopole-A Related Classifications

HY-188141 Related Classifications

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