360A

Names

[ Name ]:
360A

[Synonym ]:
360A

Biological Activity

[Description]:

360A is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay.

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> G-quadruplex

Signaling Pathways >> Cell Cycle/DNA Damage >> Telomerase

Research Areas >> Cancer

[Target]

IC50: 300 nM (Telomerase)[1] G-quadruplex[1]

[In Vitro]

360A inhibits telomerase activity and stabilizes G-quadruplex, with an IC50 of 300 nM for telomerase in TRAP-G4 assay. 360A reduces the viability of glioma cell lines, such as T98G, CB193, U118-MG, SAOS-2 and Primary astrocytes, with IC50s of 4.8 ± 1.1 μM, 3.9 ± 0.4 μM, 8.4 ± 0.5 μM, >15 μM and 17.4 ± 1.2 μM, respectively[1]. 360A causes Rad51-dependent telomere aberrations preferentially involving the lagging strand telomeres, including telomere losses or telomere doublets, and induces DNA-PKcs-dependent sister telomere fusions[2].

[Cell Assay]

The cell proliferation reagent WST-1 assay is performed. In brief, cells are seeded at various densities, depending on cell type (0.25-4 × 103 cells/well in 100 μL complete medium), in 96-well culture plates and treated with various concentrations (0.1-20 μM) of 360A or the corresponding concentrations of DMSO (control wells) for 3 or 7 days at 37°C in an atmosphere containing 5% CO2. For 7-day assays, the medium is changed on day 3. Experiments are performed in triplicate[1].

[References]

[1]. Pennarun G, et al. Apoptosis related to telomere instability and cell cycle alterations in human glioma cells treated by new highly selective G-quadruplex ligands. Oncogene. 2005 Apr 21;24(18):2917-28.

[2]. Gauthier LR, et al. Rad51 and DNA-PKcs are involved in the generation of specific telomere aberrations induced by the quadruplex ligand 360A that impair mitotic cell progression and lead to cell death. Cell Mol Life Sci. 2012 Feb;69(4):629-40.

[Related Small Molecules]

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₇H₂₃N₅O₂

[ Molecular Weight ]:
449.5

[ Storage condition ]:
-20°C

Related Compounds

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