Tanshindiol C 是一种 S-腺苷甲硫氨酸竞争性EZH2(Histone Methyltransferase) 抑制剂，抑制甲基转移酶活性的IC50为 0.55 μM。Tanshindiol C 也是巨噬细胞中Nrf2和Sirtuin 1 (Sirt1)的激活剂。Tanshindiol C 具有抗癌活性，可用于动脉粥样硬化研究。
| 生物活性 | Tanshindiol C is a S-adenosylmethionine-competitiveEZH2(Histone Methyltransferase) inhibitor with anIC50of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of bothNrf2andSirtuin1 (Sirt1)in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research[1][2]. |
| IC50& Target[1][2] | |
体外研究
(In Vitro) | Tanshindiol C (1-10 μM; for 24 h) 激活 Nrf2 并上调巨噬细胞中的 Prdx1 表达和 mRNA 水平。Tanshindiol C 通过激活 Prdx1/ABCA1 信号通路保护巨噬细胞免受 oxLDL 诱导的泡沫细胞形成[1]。
Tanshindiol C 以相似的效力抑制 EZH2 野生型和 A667G 突变体 (Ki值为 176 nM) 的活性[2]。
Tanshindiol C 抑制 Pfeiffer、U-2932 和 Daudi（淋巴瘤）、PC3（前列腺癌）、T98G 和 U87MG（胶质瘤）以及 A549（肺癌）等细胞系的生长，GI50值分别为 1.5 μM、9.5 μM , 10.6 μM, 4 μM, 6 μM, 5.7 μM 和 4.2 μM[2]。
Tanshindiol C (1-5 μM; 72 hours) 诱导亚 G1 期 Pfeiffer 细胞聚集，表明细胞处于晚期凋亡和坏死[2]。
Tanshindiol C (1-3 μM; 72 hours) 增加细胞中重要的细胞凋亡相关蛋白标志物、cleaved caspase-3、caspase-7 和聚 ADP-核糖聚合酶 (PRAP) 的蛋白水平。Tanshindiol C 显着降低 细胞中的 H3K27me3[2].
RT-PCR[1] | Cell Line: | RAW264.7 cells | | Concentration: | 1 μM, 3 μM, 10 μM | | Incubation Time: | 24 h | | Result: | Upregulated the Nrf2 and Prdx1 mRNA levels. |
Western Blot Analysis[1] | Cell Line: | Mouse peritoneal macrophages | | Concentration: | 1 μM, 3 μM, 10 μM | | Incubation Time: | 24 h | | Result: | Activated Nrf2 and upregulated Prdx1 expression in macrophages. |
Cell Cycle Analysis[2] | Cell Line: | Pfeiffer cells | | Concentration: | 1 μM, 2.5 μM and 5 μM | | Incubation Time: | 72 hours | | Result: | Induced accumulation of Pfeiffer cells in sub-G1 phase. |
Western Blot Analysis[2] | Cell Line: | Pfeiffer cells | | Concentration: | 1 μM, 3 μM | | Incubation Time: | 72 hours | | Result: | The levels of H3K27me3 was significantly decreased in the cells. |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 结构分类 | |
| 来源 | - Plants
- Compositae
- Hemistepta lyrata
|
| 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. |
