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Cat. No.: 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 No.: 3057557-03-3
화학식: C₁₁H₉ClN₄OS₂
분자량:312.80

보관:

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

Allopole-A Chemical Structure

CAS No.: 3057557-03-3

Amount: USD 0.00

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Use of MCE Products

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

PLK1 PBD

1.4-2.5 μM (IC₅₀)

All Polo-like Kinase (PLK) Isoforms :

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 No. 3057557-03-3
분자량 312.80
화학식 C₁₁H₉ClN₄OS₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[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.

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

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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MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References

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Allopole-A

All Polo-like Kinase (PLK) Isoforms

Biological Activity

제품 설명

IC50 & Target

In Vitro

Chemical Information

순도&문서

References

Calculators

Help & FAQs

Allopole-A Related Classifications

HY-188141 Related Classifications

Bioz

Keywords

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