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

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).

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Eurycomalactone Chemical Structure

Eurycomalactone Chemical Structure

CAS No. : 23062-24-0

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Description

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]

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].

MedChemExpress (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.
Molecular Weight

348.39

Formula

C19H24O6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@]12[C@@]([C@H]([C@@](O3)([H])[C@@](C)([H])[C@]2([H])C3=O)O)([H])[C@]([C@@](C(C)=CC4=O)([H])CC1=O)([C@@H]4O)C

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (287.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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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Eurycomalactone Related Classifications

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  • 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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