Background:

Description: IC50 Value: N/A 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. in vitro: 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]. in vivo: N/A Clinical trial: N/A