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  1. NF-κB Apoptosis PI3K/Akt/mTOR
  2. NF-κB Apoptosis Akt Bcl-2 Family
  3. Eurycomalactone

Eurycomalactone  (Synonyms: 東革內(nèi)酯)

目錄號: HY-N4327 純度: 98.99%
COA 產(chǎn)品使用指南 技術(shù)支持

Eurycomalactone 是一種可以從 Eurycoma longifolia Jack 中分離得到的活性擬松類化合物。Eurycomalactone 是一種有效的NF-κB 抑制劑,其 IC50 值為 0.5 μM。Eurycomalactone 可抑制蛋白合成,降低 cyclin D1 蛋白水平。Eurycomalactone 通過阻滯細胞周期于G2/M 期和延遲 DNA 雙鏈斷裂修復來提高放射敏感性。Eurycomalactone 抑制 AKT/NF-κB 信號通路的激活,誘導細胞凋亡并增強對 Cisplatin (HY-17394) 的化療敏感性。

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Eurycomalactone Chemical Structure

Eurycomalactone Chemical Structure

CAS No. : 23062-24-0

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

Eurycomalactone is an active quassinoid could be isolated from Eurycoma longifolia Jack. Eurycomalactone is a potent NF-κB inhibitor with an IC50 value of 0.5 μM. Eurycomalactone inhibits protein synthesis and depletes cyclin D1. Eurycomalactone enhances radiosensitivity through arrest cell cycle at G2/M phase and delayed DNA double-strand break repair. Eurycomalactone inhibits the activation of AKT/NF-κB signaling, induces apoptosis and enhances chemosensitivity to Cisplatin (HY-17394)[1][2][3].

IC50 & Target

IC50: 0.5 μM (NF-κB)[1]

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
HT-1080 IC50
0.98 μM
Compound: 11
Cytotoxicity against human HT1080 cells after 72 hrs by MTT assay
Cytotoxicity against human HT1080 cells after 72 hrs by MTT assay
[PMID: 19919052]
體外研究
(In Vitro)

Eurycomalactone (24, 48 and 72 h) selectively inhibits the viability of A549 and COR-L23 cells Eurycomalactone inhibits the viability of A549 cells with IC50 values of 20.17, 3.77, and 1.90 μM for 24, 48 and 72 hours, respectively. Eurycomalactone inhibits the viability of COR-L23 cells with IC50 values of 25.02, 2.74, and 1.80 μM for 24, 48 and 72 hours, respectively[1].
Eurycomalactone (2.29-156.3 μM; 24 h; A549 and Calu-1 cells) promotes Non-small cell lung cancer (NSCLC) cells apoptosis[2].
Eurycomalactone (0-25.05 μM; 24 h; A549 and COR-L23 cells) induces cell cycle arrest at the radiosensitive G2/M phase and induces apoptosis in irradiated Non-small cell lung cancer (NSCLC) cells. Eurycomalactone downregulated the key G2/M regulatory proteins in irradiated Non-small cell lung cancer (NSCLC) cells[1].
Eurycomalactone (2.5-25 μM; 24 h; A549 cells) suppressed the repair of radiation-Induced DNA double-strand breaks[1].
Eurycomalactone (2.29-156.3 μM; 24 h; A549 and Calu-1 cells) suppresses AKT/NF-κB activation in Non-small cell lung cancer (NSCLC) cells[2].

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

Apoptosis Analysis[2]

Cell Line: A549 and Calu-1 cells
Concentration: 2.29, 10.14, 12.02, 20.81, 80.77, and 156.3 μM
Incubation Time: 24 hours
Result: Increased the apoptotic rates in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: A549 and COR-L23 cells
Concentration: 1.57, 2.57, 20.17 and 25.05 μM
Incubation Time: 24 hours
Result: Induced cell cycle arrest at G2/M phase in irradiated cells and increased the sub-G1 population. A549 and COR-L23 cells

Western Blot Analysis[2]

Cell Line: A549 and Calu-1 cells
Concentration: 2.29, 10.14, 12.02, 20.81, 80.77, and 156.3 μM
Incubation Time: 24 hours
Result: Induced the expression levels of active caspase-3 and active PARP (cleaved form), while decreased Bcl-xL and surviving.

Western Blot Analysis[1]

Cell Line: A549 and COR-L23 cells
Concentration: 1.57, 2.57, 20.17 and 25.05 μM
Incubation Time: 24 hours
Result: Downregulated the expression of both G2/M regulatory proteins in a dose-dependent manner.

Western Blot Analysis[2]

Cell Line: A549 and COR-L23 cells
Concentration: 2.29, 10.14, 12.02, 20.81, 80.77, and 156.3 μM
Incubation Time: 24 hours
Result: inhibited the expression levels of p(S473)-AKT, total AKT, p(S536)-NF-κB p65 and total NF-κB p65.
分子量

348.39

Formula

C19H24O6

CAS 號
性狀

固體

顏色

White to off-white

中文名稱

東革內(nèi)酯

結(jié)構(gòu)分類
初始來源
運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, protect from light

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

溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : 100 mg/mL (287.03 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.8703 mL 14.3517 mL 28.7035 mL
5 mM 0.5741 mL 2.8703 mL 5.7407 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

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純度 & 產(chǎn)品資料
參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8703 mL 14.3517 mL 28.7035 mL 71.7587 mL
5 mM 0.5741 mL 2.8703 mL 5.7407 mL 14.3517 mL
10 mM 0.2870 mL 1.4352 mL 2.8703 mL 7.1759 mL
15 mM 0.1914 mL 0.9568 mL 1.9136 mL 4.7839 mL
20 mM 0.1435 mL 0.7176 mL 1.4352 mL 3.5879 mL
25 mM 0.1148 mL 0.5741 mL 1.1481 mL 2.8703 mL
30 mM 0.0957 mL 0.4784 mL 0.9568 mL 2.3920 mL
40 mM 0.0718 mL 0.3588 mL 0.7176 mL 1.7940 mL
50 mM 0.0574 mL 0.2870 mL 0.5741 mL 1.4352 mL
60 mM 0.0478 mL 0.2392 mL 0.4784 mL 1.1960 mL
80 mM 0.0359 mL 0.1794 mL 0.3588 mL 0.8970 mL
100 mM 0.0287 mL 0.1435 mL 0.2870 mL 0.7176 mL
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    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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產(chǎn)品名稱:
Eurycomalactone
目錄號:
HY-N4327
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