化学性质:
规格 | 10mM (in 1mL DMSO) 10mg 50mg |
CAS | 789-61-7 |
别名 |
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化学名 | (2R,3S,5R)-2-(hydroxymethyl)-5-(2-imino-6-mercapto-2H-purin-9(3H)-yl)tetrahydrofuran-3-ol |
分子式 | C10H13N5O3S |
分子量 | 283.31 |
溶解度 | ≥ 62.5mg/mL in DMSO |
储存条件 | 4°C, protect from light |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
6-thio-dG is a nucleoside analogue [1], is a telomerase-mediated telomere disrupting compound [2]. It is an anti-cancer inhibitor [1]. Cancer cells were very sensitive to 6-thio-dG with observed IC50 values ranging from 0.7-2.9 μM, depending on cell types [3].
Telomeres are found at the end of eukaryotic linear chromosomes. They are essential for genomic stability and chromosome maintenance [3].
In HCT116 human colon cancer cell line, treatment with 6-thio-dG made progressive telomere shortening independent of telomerase activity inhibition and induced telomere dysfunction. GRN163L is a telomerase inhibitor. In HCT116 cells, treatment with GRN163L and 6-thio-dG together increased telomere shortening. Within 1 week, 6-thio-dG killed most of HCT116 cells and altered cellular morphology. Normal BJ fibroblast cells are telomerase silent. After 1 week, treatment with 6-thio-dG showed no effect on cell morphology. After long-term treatment with 6-thio-dG, no effect on telomere shortening was found [1].
In murine mode with xenograft derived from A549 lung cancer cell line, as compared to controls, intraperitoneal injection with 2 mg/kg of 6-thio-dG every other day completely prevented progressive tumor growth. Ki67 is a biomarker correlating with proliferation levels. Compared to controls, 6-thio-dG decreased Ki67 staining. Treatment with 6-thio-dG through local injection resulted in even more dramatic decrease in the tumor growth rate compared to untreated controls [3].
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标签:6-Thio-dG
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