1. Anti-infection Apoptosis
  2. EBV HSV Apoptosis
  3. Ferruginol

Ferruginol ((+)-Ferruginol), a natural diterpenoid, is an inhibitor of the activation of Epstein-Barr virus early antigen (EBV-EA). Ferruginol inhibits the growth of thyroid cancer cells through the induction of mitochondrial apoptosis. Ferruginol has antitumor, cardioprotective, antioxidant, gastroprotective, and neuroprotective activities.

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Ferruginol

Ferruginol Chemical Structure

CAS No. : 514-62-5

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Description

Ferruginol ((+)-Ferruginol), a natural diterpenoid, is an inhibitor of the activation of Epstein-Barr virus early antigen (EBV-EA). Ferruginol inhibits the growth of thyroid cancer cells through the induction of mitochondrial apoptosis. Ferruginol has antitumor, cardioprotective, antioxidant, gastroprotective, and neuroprotective activities[1][2][3].

Cellular Effect
Cell Line Type Value Description References
A549 ED50
6.47 μg/mL
Compound: ferruginol
Cytotoxicity against human A549 cells after 7 days by MTT assay
Cytotoxicity against human A549 cells after 7 days by MTT assay
[PMID: 9014350]
A549 GI50
<50 μg/mL
Compound: 2
Inhibitory activity against human A549 lung tumor cell proliferation
Inhibitory activity against human A549 lung tumor cell proliferation
[PMID: 15808460]
A549 GI50
30.67 μM
Compound: 14
Cytotoxicity against human A549 cells assessed as growth inhibition by WST-8 assay
Cytotoxicity against human A549 cells assessed as growth inhibition by WST-8 assay
[PMID: 24210499]
A549 IC50
>40 μM
Compound: 25
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
[PMID: 23691952]
AGS IC50
18 μM
Compound: 3
Cytotoxicity against human AGS cells
Cytotoxicity against human AGS cells
[PMID: 25440884]
BJ EC50
19.57 μM
Compound: 1
Cytotoxicity against human BJ cells
Cytotoxicity against human BJ cells
[PMID: 25316317]
BXPC-3 GI50
21.14 μM
Compound: 14
Cytotoxicity against human BxPC3 cells assessed as growth inhibition by WST-8 assay
Cytotoxicity against human BxPC3 cells assessed as growth inhibition by WST-8 assay
[PMID: 24210499]
HCT-116 GI50
<50 μg/mL
Compound: 2
Growth inhibitory activity against human HCT116 colon tumor cell line
Growth inhibitory activity against human HCT116 colon tumor cell line
[PMID: 15808460]
HEK293 EC50
>25 μM
Compound: 1
Cytotoxicity against HEK293 cells
Cytotoxicity against HEK293 cells
[PMID: 25316317]
HeLa IC50
64.9 μM
Compound: 1
Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 48 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 48 hrs by MTT assay
[PMID: 26638041]
HepG2 EC50
>25 μM
Compound: 1
Cytotoxicity against human HepG2 cells
Cytotoxicity against human HepG2 cells
[PMID: 25316317]
HepG2 IC50
>40 μM
Compound: 19
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
[PMID: 20402524]
HL-60 GI50
27.33 μM
Compound: 14
Cytotoxicity against human HL60 cells assessed as growth inhibition by WST-8 assay
Cytotoxicity against human HL60 cells assessed as growth inhibition by WST-8 assay
[PMID: 24210499]
HL-60 IC50
>40 μM
Compound: 19
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
[PMID: 20402524]
HL-60 IC50
>40 μM
Compound: 25
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
[PMID: 23691952]
HT-29 ED50
6.43 μg/mL
Compound: ferruginol
Cytotoxicity against human HT-29 cells after 7 days by MTT assay
Cytotoxicity against human HT-29 cells after 7 days by MTT assay
[PMID: 9014350]
HT-29 IC50
39.4 μM
Compound: 12
Cytotoxicity against human HT-29 cells after 72 hrs by SRB assay
Cytotoxicity against human HT-29 cells after 72 hrs by SRB assay
[PMID: 26905523]
Jurkat IC50
35.1 μM
Compound: 19
Cytotoxicity against human Jurkat cells after 48 hrs by MTT assay
Cytotoxicity against human Jurkat cells after 48 hrs by MTT assay
[PMID: 20402524]
Jurkat IC50
48.2 μM
Compound: 1
Cytotoxicity against human Jurkat cells assessed as cell growth inhibition after 48 hrs by MTT assay
Cytotoxicity against human Jurkat cells assessed as cell growth inhibition after 48 hrs by MTT assay
[PMID: 26638041]
MCF7 ED50
23.42 μg/mL
Compound: ferruginol
Cytotoxicity against human MCF7 cells after 7 days by MTT assay
Cytotoxicity against human MCF7 cells after 7 days by MTT assay
[PMID: 9014350]
MCF7 IC50
>40 μM
Compound: 25
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
[PMID: 23691952]
MDA-MB-231 GI50
<50 μg/mL
Compound: 2
Growth inhibitory activity against human MDA-MB-231 breast tumor cell line
Growth inhibitory activity against human MDA-MB-231 breast tumor cell line
[PMID: 15808460]
MIA PaCa-2 IC50
25.9 μM
Compound: 20
Cytotoxicity against human MIAPaCa2 cells after 24 hrs by MTT assay
Cytotoxicity against human MIAPaCa2 cells after 24 hrs by MTT assay
[PMID: 21775156]
MRC5 GI50
40.01 μM
Compound: 14
Cytotoxicity against human MRC5 cells assessed as growth inhibition by WST-8 assay
Cytotoxicity against human MRC5 cells assessed as growth inhibition by WST-8 assay
[PMID: 24210499]
MRC5 IC50
19 μM
Compound: 3
Cytotoxicity against human MRC5 cells
Cytotoxicity against human MRC5 cells
[PMID: 25440884]
NCI-H23 GI50
<50 μg/mL
Compound: 2
Growth inhibitory activity against human NCI-H23 lung tumor cell line
Growth inhibitory activity against human NCI-H23 lung tumor cell line
[PMID: 15808460]
PANC-1 GI50
41.13 μM
Compound: 14
Cytotoxicity against human PANC1 cells assessed as growth inhibition by WST-8 assay
Cytotoxicity against human PANC1 cells assessed as growth inhibition by WST-8 assay
[PMID: 24210499]
PC-3 GI50
56.45 μM
Compound: 14
Cytotoxicity against human PC3 cells assessed as growth inhibition by WST-8 assay
Cytotoxicity against human PC3 cells assessed as growth inhibition by WST-8 assay
[PMID: 24210499]
Raji EC50
11.49 μM
Compound: 1
Cytotoxicity against human Raji cells
Cytotoxicity against human Raji cells
[PMID: 25316317]
SMMC-7721 IC50
>40 μM
Compound: 25
Cytotoxicity against human SMMC7721 cells after 48 hrs by MTT assay
Cytotoxicity against human SMMC7721 cells after 48 hrs by MTT assay
[PMID: 23691952]
SW480 IC50
>40 μM
Compound: 25
Cytotoxicity against human SW480 cells after 48 hrs by MTT assay
Cytotoxicity against human SW480 cells after 48 hrs by MTT assay
[PMID: 23691952]
SW-620 GI50
<50 μg/mL
Compound: 2
Growth inhibitory activity against human SW620 colon tumor cell line
Growth inhibitory activity against human SW620 colon tumor cell line
[PMID: 15808460]
U-937 IC50
19.7 μM
Compound: 19
Cytotoxicity against human U937 cells after 48 hrs by MTT assay
Cytotoxicity against human U937 cells after 48 hrs by MTT assay
[PMID: 20402524]
U-937 IC50
21.3 μM
Compound: 1
Cytotoxicity against human U937 cells assessed as cell growth inhibition after 48 hrs by MTT assay
Cytotoxicity against human U937 cells assessed as cell growth inhibition after 48 hrs by MTT assay
[PMID: 26638041]
Vero CC50
80.4 μM
Compound: 1
Cytotoxicity against Vero E6 cells by MTT assay
Cytotoxicity against Vero E6 cells by MTT assay
[PMID: 17663539]
Vero EC50
1.39 μM
Compound: 1
Antiviral activity against SARS coronavirus in Vero E6 cells assessed as inhibition of viral replication by ELISA
Antiviral activity against SARS coronavirus in Vero E6 cells assessed as inhibition of viral replication by ELISA
[PMID: 17663539]
Vero IC50
90.4 μM
Compound: 1
Cytotoxicity against African green monkey Vero cells assessed as cell growth inhibition after 48 hrs by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as cell growth inhibition after 48 hrs by MTT assay
[PMID: 26638041]
In Vitro

Ferruginol (0-160 μM; 24 hours) exerts potent antiproliferative action against thyroid cancer cells, and an IC50 of 12 μM for the MDA-T32 cell line. The toxic effects of Ferruginol are less pronounced against normal cells[1].
Ferruginol (0-24 μM; 24 hours) induces apoptotic cell death of MDA-T32 cells. Ferruginol increases Bax expression and decreases Bcl-2 expression dose-dependently[1].
Ferruginol (0-24 μM; 24 hours) inhibits the MAPK and PI3K/AKT signaling pathway of MDA-T32 cells[1].
Ferruginol (0-24 μM; 24 hours) also causes ROS mediated alterations in the MMP of MDA-T32 cells[1].

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

Cell Viability Assay[1]

Cell Line: MDA-T32 cells
Concentration: 0-160 μM
Incubation Time: 24 hours
Result: Exerted potent antiproliferative action against thyroid cancer cells.

Apoptosis Analysis[1]

Cell Line: MDA-T32 cells
Concentration: 0 μM, 6 μM, 12 μM, and 24 μM
Incubation Time: 24 hours
Result: Induced apoptotic cell death of MDA-T32 cells

Western Blot Analysis[1]

Cell Line: MDA-T32 cells
Concentration: 0 μM, 6 μM, 12 μM, and 24 μM
Incubation Time: 24 hours
Result: Blocked the MAPK and PI3K/AKT signaling pathway.
In Vivo

Ferruginol (20 mg/kg; p.o.; daily; for 4 weeks) exerts cardioprotection manifested as enhanced cardiac function and reduced structural damage and apoptosis. The transcriptome and other results revealed that Ferruginol facilitates PGC-1α-mediated mitochondrial biogenesis and fatty acid oxidation (MB and FAO) by increasing the expression of PGC-1α and concurrently promoting the expression of SIRT1-enhancing deacetylase SIRT1 deacetylating and activating PGC-1α[3].

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

Animal Model: Male C57BL/6 mice (20 g, 8-10 weeks old) with Doxorubicin (DOX)-induced cardiotoxicity (DIC)[3].
Dosage: 20 mg/kg
Administration: Administered intragastrically; daily; for 4 weeks
Result: Relieved Doxorubicin-induced cardiac structural and functional lesion.
Molecular Weight

286.45

Formula

C20H30O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

[H][C@]1(CCC2=C3)C(C)(C)CCC[C@]1(C)C2=CC(O)=C3C(C)C

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°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 (349.10 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 3.4910 mL 17.4551 mL 34.9101 mL
5 mM 0.6982 mL 3.4910 mL 6.9820 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.

  • Molarity Calculator

  • Dilution Calculator

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

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (8.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 96.91%

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 3.4910 mL 17.4551 mL 34.9101 mL 87.2753 mL
5 mM 0.6982 mL 3.4910 mL 6.9820 mL 17.4551 mL
10 mM 0.3491 mL 1.7455 mL 3.4910 mL 8.7275 mL
15 mM 0.2327 mL 1.1637 mL 2.3273 mL 5.8184 mL
20 mM 0.1746 mL 0.8728 mL 1.7455 mL 4.3638 mL
25 mM 0.1396 mL 0.6982 mL 1.3964 mL 3.4910 mL
30 mM 0.1164 mL 0.5818 mL 1.1637 mL 2.9092 mL
40 mM 0.0873 mL 0.4364 mL 0.8728 mL 2.1819 mL
50 mM 0.0698 mL 0.3491 mL 0.6982 mL 1.7455 mL
60 mM 0.0582 mL 0.2909 mL 0.5818 mL 1.4546 mL
80 mM 0.0436 mL 0.2182 mL 0.4364 mL 1.0909 mL
100 mM 0.0349 mL 0.1746 mL 0.3491 mL 0.8728 mL
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Ferruginol
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