794466-17-4
Chemical Structure
DAP-81
- CAS. Nr.: 794466-17-4
- Formula:C25H20N6O4
- Molecular Weight:468.46
IUPAC Name: N-(4-((4-((2-benzoylphenyl)amino)-5-nitropyrimidin-2-yl)amino)phenyl)acetamide
InChIKey: LOMJSEHTDFISSP-UHFFFAOYSA-N
SMILES: CC(NC1=CC=C(C=C1)NC2=NC=C(C(NC3=CC=CC=C3C(C4=CC=CC=C4)=O)=N2)[N+]([O-])=O)=O
Biological Activity: DAP-81 is an inhibitory agent targeting Polo-like kinases (Plks), a class of evolutionarily conserved serine/threonine kinases. DAP-81 dose-dependently increases the number of monopolar spindles in treated cells. High-resolution live-cell microscopy revealed that Plk activity is required for the assembly and maintenance of bipolar mitotic spindles. Plk inhibition destabilizes centromeric microtubules while stabilizing other spindle microtubules, leading to the formation of monopolar spindles. Further testing of compounds based on "privileged scaffolds" such as the DAP scaffold may lead to the discovery of new cell division probes and anti-microtubule agents.
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DAP-81 | DAP-81 is an inhibitory agent targeting Polo-like kinases (Plks), a class of evolutionarily conserved serine/threonine kinases. DAP-81 dose-dependently increases the number of monopolar spindles in treated cells. High-resolution live-cell microscopy revealed that Plk activity is required for the assembly and maintenance of bipolar mitotic spindles. Plk inhibition destabilizes centromeric microtubules while stabilizing other spindle microtubules, leading to the formation of monopolar spindles. Further testing of compounds based on "privileged scaffolds" such as the DAP scaffold may lead to the discovery of new cell division probes and anti-microtubule agents. | |||||||||||||||||||||
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Keywords
