737763-37-0

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

360a is a 2,6-pyridine-dicarboxamide derivative displaying strong affinity and selectivity for g-quadruplex structures and selective telomerase inhibition in vitro assays. 360a is a g-quadruplex ligand, which can influence the consequence of g-quadruplex formation and/or stabilization.

we found a s-phase accumulation in atm-proficient, but not in atm-deficient ebv-lymphocytes treated with 360a before induction of cell death. however, atm status did not modify cell cycle distribution in 360a-treated sv40-fibroblasts and hela cells compared to dmso treated controls [1]. dna-pkcs-dependent nhej was responsible for sister telomere fusions as a direct consequence of g-quadruplex formation and/or stabilization induced by 360a on parental telomere g strands. nhej and hr activation at telomeres altered mitotic progression in treated cells [2]. this compound was shown to display a potent affinity and selectivity for telomeric g-quadruplex dna over duplex dna and to induce delayed growth inhibition in ht1080 tumor cell line [3].

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[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. DOI:10.1038/sj.onc.1208468
[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. DOI:10.1007/s00018-011-0767-6