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%
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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

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 GI50
4.2 μM
Compound: 5
Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by WST-1 assay
Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by WST-1 assay
[PMID: 24767850]
Daudi GI50
10.6 μM
Compound: 5
Cytotoxicity against human Daudi cells assessed as growth inhibition after 72 hrs by WST-1 assay
Cytotoxicity against human Daudi cells assessed as growth inhibition after 72 hrs by WST-1 assay
[PMID: 24767850]
PC-3 GI50
4 μM
Compound: 5
Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by WST-1 assay
Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by WST-1 assay
[PMID: 24767850]
Pfeiffer GI50
1.5 μM
Compound: 5
Cytotoxicity against human Pfeiffer cells expressing EZH2 A667G mutant assessed as growth inhibition after 72 hrs by WST-1 assay
Cytotoxicity against human Pfeiffer cells expressing EZH2 A667G mutant assessed as growth inhibition after 72 hrs by WST-1 assay
[PMID: 24767850]
T98G GI50
6 μM
Compound: 5
Cytotoxicity against human T98G cells assessed as growth inhibition after 72 hrs by WST-1 assay
Cytotoxicity against human T98G cells assessed as growth inhibition after 72 hrs by WST-1 assay
[PMID: 24767850]
U2932 GI50
9.5 μM
Compound: 5
Cytotoxicity against human U2932 cells assessed as growth inhibition after 72 hrs by WST-1 assay
Cytotoxicity against human U2932 cells assessed as growth inhibition after 72 hrs by WST-1 assay
[PMID: 24767850]
U-87MG ATCC GI50
5.7 μM
Compound: 5
Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by WST-1 assay
Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by WST-1 assay
[PMID: 24767850]
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)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 25 mg/mL (80.05 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2018 mL 16.0092 mL 32.0184 mL
5 mM 0.6404 mL 3.2018 mL 6.4037 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2018 mL 16.0092 mL 32.0184 mL 80.0461 mL
5 mM 0.6404 mL 3.2018 mL 6.4037 mL 16.0092 mL
10 mM 0.3202 mL 1.6009 mL 3.2018 mL 8.0046 mL
15 mM 0.2135 mL 1.0673 mL 2.1346 mL 5.3364 mL
20 mM 0.1601 mL 0.8005 mL 1.6009 mL 4.0023 mL
25 mM 0.1281 mL 0.6404 mL 1.2807 mL 3.2018 mL
30 mM 0.1067 mL 0.5336 mL 1.0673 mL 2.6682 mL
40 mM 0.0800 mL 0.4002 mL 0.8005 mL 2.0012 mL
50 mM 0.0640 mL 0.3202 mL 0.6404 mL 1.6009 mL
60 mM 0.0534 mL 0.2668 mL 0.5336 mL 1.3341 mL
80 mM 0.0400 mL 0.2001 mL 0.4002 mL 1.0006 mL
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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产品名称:
Tanshindiol C
目录号:
HY-122936
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