| Identification | Back Directory | [Name]
DAP-81 | [CAS]
794466-17-4 | [Synonyms]
DAP-81
Acetamide, N-[4-[[4-[(2-benzoylphenyl)amino]-5-nitro-2-pyrimidinyl]amino]phenyl]- | [Molecular Formula]
C25H20N6O4 | [MDL Number]
MFCD32173672 | [MOL File]
794466-17-4.mol | [Molecular Weight]
468.46 |
| Hazard Information | Back Directory | [Description]
DAP-81 is a diaminopyrimidine derivative that targets PLKs, destabilizing kinetochore microtubules. Other spindle tubules are stabilized, resulting in monopolar mitotic spindles. In vitro, DAP-81 inhibits Plk1 at an IC50 of 0.9 nM. DAP-81 is currently in ongoing preclinical evaluations. | [Uses]
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. | [References]
[1] Probing cell-division phenotype space and Polo-like kinase function using small molecules |
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