360A

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

360A 

360A 是一种 G-四联体 (G-quadruplex) 的稳定剂,同时可抑制端粒酶 (telomerase) 的活性,在 TRAP-G4 实验中,IC50 值为 300 nM。

360A

360A Chemical Structure

CAS No. : 794458-56-3

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360A 的其他形式现货产品:

360A iodide

生物活性

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.

IC50 & Target

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

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

449.50

Formula

C27H23N5O22+

CAS 号

794458-56-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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.

Cell Assay
[1]

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [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.

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