313984-77-9 | PU-02; PU02
英文名称
6-[(1-NaphthalenylMethyl)thio]-9H-purine
分子式
C16H12N4S
分子量
292.36
结构式
中文别名
英文别名
| 属性 | 值 |
|---|---|
| 形态 | 粉末 |
| 颜色 | White to off-white |
| 溶解度 | Soluble to 100 mM in DMSO |
| 储存条件 | Sealed in dry,2-8°C |
| 标题 | 内容 |
|---|---|
| 靶点 | 5-HT 3A Receptor 0.36 μM (IC 50 ) 5-HT 3 AB 0.73 μM (IC 50 ) |
| 体外研究 | PU02 (NMMP) (0-200 μM) leads to a steady decrease in cell viability of HepG2 cells (IC 50 =48.585 μM). PU02 (NMMP) shows less toxicity on L02 cells than did 6-MP after 48 h of treatment. PU02 (NMMP) at 6.25 or 25 μM exhibits inhibitory effects on the viability of the tested cell lines, including SMMC-7721, MDA-MB-231, RKO and HCT-8 cells. PU02 (NMMP) induces cell cycle arrest at the G2/M phase. PU02 (NMMP) downregulats the expression of cyclin B1/D1 and CDK4 in a time-dependent manner in HepG2 cells,but the expression of cyclin E is not affected. PU02 (NMMP)-treated cells exhibits a significant increase in caspase-3 cleavage, suggesting enhanced apoptotic activity. Apoptosis Analysis Cell Line: HepG2 cells. Concentration: 6.26, 12.5, 25, 50 μM. Incubation Time: 6, 12, 24, 36 h. Result: Induced mitochondria-dependent apoptosis. |
| 生物活性 | PU02 是 6-MP (HY-13677) 的一个衍生物，是 5-HT3 受体的负变构调节剂，其在 HEK293 细胞测得的转染 5-HT3A 和 5-HT3AB 受体后的 IC50 值分别为 0.36 和 0.73 μM。 |