1. Epigenetics NF-κB Cell Cycle/DNA Damage
  2. Histone Methyltransferase Keap1-Nrf2 Sirtuin
  3. Tanshindiol C

Tanshindiol C  (Synonyms: 丹参二醇C)

目录号: HY-122936 纯度: 98.47%
COA 产品使用指南

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 Nrf2Sirtuin 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。

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Tanshindiol C Chemical Structure

Tanshindiol C Chemical Structure

CAS No. : 97465-71-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research[1][2].

IC50 & Target[1][2]

EZH2

0.55 μM (IC50)

SIRT1

 

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

312.32

Formula

C18H16O5

CAS 号
性状

固体

颜色

Brown to red

中文名称

丹参二醇C

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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