2. Anti-infection NF-κB Metabolic Enzyme/Protease Apoptosis
  3. Influenza Virus NF-κB 5 alpha Reductase Keap1-Nrf2 Lactate Dehydrogenase Apoptosis
  4. Germacrone

Germacrone is a sesquiterpene compound with multiple biological activities. Germacrone inhibits the H1N1 and H3N2 influenza A virus and the influenza B virus. Germacrone blocks the progressionof arthritis by regulating Th1/Th2 balance and inhibiting NF-κB signaling. Germacrone can arrest the cell cycle at G0/G1 and G2/M phases and induce apoptosis in breast cancer cells. Germacrone inhibits 5α-reductase and has anti-androgenic effect. Germacrone has neuroprotective functions and can be used for the study of traumatic brain injury (TBI). Germacrone also has antioxidant activity.

For research use only. We do not sell to patients.

Germacrone Chemical Structure

Germacrone Chemical Structure

CAS No. : 6902-91-6

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ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Other Forms of Germacrone:

Germacrone Related Antibodies

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1 Publications Citing Use of MCE Germacrone

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Germacrone is a sesquiterpene compound with multiple biological activities. Germacrone inhibits the H1N1 and H3N2 influenza A virus and the influenza B virus. Germacrone blocks the progressionof arthritis by regulating Th1/Th2 balance and inhibiting NF-κB signaling. Germacrone can arrest the cell cycle at G0/G1 and G2/M phases and induce apoptosis in breast cancer cells. Germacrone inhibits 5α-reductase and has anti-androgenic effect. Germacrone has neuroprotective functions and can be used for the study of traumatic brain injury (TBI). Germacrone also has antioxidant activity[1][2][3][4][5].

IC50 & Target

Influenza virus[1]
In Vitro

Germacrone (0-2.0 μM, 48 h) inhibits the neuraminidase activity of A/PR/8/34(H1N1) (EC50: 6.03/2.66 μM), A/human/Hubei/1/2009(H1N1) (EC50: 5.59/2.9 μM), A/human/Hubei/3/2005(H3N2) (EC50: 3.82/2.15 μM), Influenza B virus (EC50: 6.30/2.33 μM), and A/WSN/33/S31N(H1N1) (EC50: 7.12/4.78 μM) virus strains in MDCK cells and A549 cells[1].
Germacrone (0-400 μM, 24-72 h) inhibits the proliferation of breast cancer cell lines MDA-MB-231 cells and MCF-7 cells in a dose-dependent manner[2].
Germacrone (0-400 μM, 24 h) increases the release of LDH (66.85%; 72.76%) but decreases the mitochondrial membrane potential (ΔΨm) in MDA-MB-231 cells and MCF-7 cells[2].
Germacrone (0-200 μM, 24 h) induces cell cycle arrest in G0/G1 phase (71.24%; 77.08%) and G2/M phase (15.89%; 12.36%) in MDA-MB-231 cells and MCF-7 cells in a dose-dependent manner[2].
Germacrone (0-200 μM, 24 h) induces apoptosis in MDA-MB-231 cells[2].
Germacrone (0-200 μM, 24 h) increases the release of mitochondrial cytochrome c and activates the caspases pathway[2].
Germacrone (0.5 mg/mL, 30 min) inhibits the activity of rat liver 5α-reductase (65.7%, IC50: 0.42 mg/mL)[5].
Germacrone (0.01-10 μM, 96 h) inhibits testosterone-induced LNCaP cell growth in a concentration-dependent manner[5].

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

Germacrone Related Antibodies

Cell Viability Assay[2]

Cell Line: MDA-MB-231 and MCF-7 cells
Concentration: 0, 25, 50, 100, 200, 400 μM
Incubation Time: 24, 48, 72 h
Result: Inhibited cell proliferation.

Apoptosis Analysis[2]

Cell Line: MDA-MB-231 cells
Concentration: 0, 50, 100, 200 μM
Incubation Time: 24 h
Result: Increased the TUNEL-positive cell population of MDA-MB-231 cells undergoing apoptosis (45.13%).

Western Blot Analysis[2]

Cell Line: MDA-MB-231 cells
Concentration: 0, 50, 100, 200 μM
Incubation Time: 24 h
Result: Down-regulated the expression of phosphorylated ATR (Ser428), phosphorylated cdc2 (Tyr15), phosphorylated Rb (Ser795) and cdc2 proteins.
Up-regulated the expression of Bok, caspase 3, 7 and 9, and PARP proteins.

Cell Proliferation Assay[5]

Cell Line: LNCaP cells
Concentration: 0.01, 0.5, 5, 10 μM
Incubation Time: 96 h
Result: Inhibited cell proliferation.
In Vivo

Germacrone (50-100 mg/kg, i.v., once a day for 6 days) inhibits viral activity in 5 LD50 influenza virus (A/Puerto Rico/8/34) infected mice[1].
Germacrone (20 mg/kg, p.o., once a day for 3 weeks) reduces the levels of Th1 cytokines (TNF-α and IFN-γ) and increases Th2 cytokines (IL-4) in serum, synovial tissue and spleen of mice in collagen-induced arthritis (CIA) model[3].
Germacrone (20 mg/kg, p.o., once a day for 3 weeks) inhibits NF-κB activation in synovial tissue of mice in CIA model[3].
Germacrone (5-20 mg/kg, i.p.) improves neurological dysfunction and neurological injury in controlled cortical impact (CCI) model mice; inhibits the activity of microglia, the expression of proinflammatory factors TNF-α, IL-1β, IL-6 and oxidative stress in CCI mice; also inhibits NF-κB and induces Nrf2 pathway to exert anti-inflammatory and antioxidant effects[4].
Germacrone (3-100 μg, topical administration, 4 weeks) inhibits testosterone-stimulated lumbar gland growth in castrated male rats (79-82%)[5].

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

Animal Model: BALB/c mice intranasally infected with 5 LD50 influenza virus (A/Puerto Rico/8/34) (18-20 g)[1]
Dosage: 50, 100 mg/kg
Administration: Intravenous injection (i.v.), once every day for 6 d
Result: Reduced virus titer.
Increased mice survival rate.
Delayed in the mortality time in mice.
Animal Model: CIA mouse model (male DBA/1 J mice, 6 weeks old)[3]
Dosage: 20 mg/kg
Administration: Oral gavage (p.o.), once per day for 3 weeks
Result: Reduced the expression of TNF-α and IFN-γ, but increased the expression of IL-4.
Increased the expression of IκB and decreased the phosphorylation level of NF-κB p65.
Animal Model: CCI mouse model (male DBA/1 J mice, 6 weeks old)[4]
Dosage: 5, 10 and 20  mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Reversed the pathological changes.
Reduced expression of CD16 and CD11b.
Reduced the expression of TNF-α, IL-1β and IL-6.
Reduced MPO and MDA, increased SOD expression.
Inhibitd NF-κB and induced Nrf2 expression.
Animal Model: 8-week-old castrated male mice[5]
Dosage: 3, 30 and 100 μg
Administration: Topical Administration, 4 weeks
Result: Inhibited the growth of flank gland.
Molecular Weight

218.33

Formula

C15H22O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C/C(C)=C/CC/C(C)=C/C/C1=C(C)\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 (458.02 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 4.5802 mL 22.9011 mL 45.8022 mL
5 mM 0.9160 mL 4.5802 mL 9.1604 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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (11.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (11.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
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: 99.76%

SDS (393 KB)

COA (257 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
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 4.5802 mL 22.9011 mL 45.8022 mL 114.5056 mL
5 mM 0.9160 mL 4.5802 mL 9.1604 mL 22.9011 mL
10 mM 0.4580 mL 2.2901 mL 4.5802 mL 11.4506 mL
15 mM 0.3053 mL 1.5267 mL 3.0535 mL 7.6337 mL
20 mM 0.2290 mL 1.1451 mL 2.2901 mL 5.7253 mL
25 mM 0.1832 mL 0.9160 mL 1.8321 mL 4.5802 mL
30 mM 0.1527 mL 0.7634 mL 1.5267 mL 3.8169 mL
40 mM 0.1145 mL 0.5725 mL 1.1451 mL 2.8626 mL
50 mM 0.0916 mL 0.4580 mL 0.9160 mL 2.2901 mL
60 mM 0.0763 mL 0.3817 mL 0.7634 mL 1.9084 mL
80 mM 0.0573 mL 0.2863 mL 0.5725 mL 1.4313 mL
100 mM 0.0458 mL 0.2290 mL 0.4580 mL 1.1451 mL
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Germacrone Related Classifications

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.

Keywords:

Germacrone6902-91-6Influenza VirusNF-κB5 alpha ReductaseKeap1-Nrf2Lactate DehydrogenaseApoptosisNuclear factor-κBNuclear factor-kappaB5α-reductaseLDHAnti-viralanticancerinflammatoryMDA-MB-231MCF-7LNCaP5 LD50 infected modelCIA modelCCI modelInhibitorinhibitorinhibit

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