1. JAK/STAT Signaling Stem Cell/Wnt NF-κB Immunology/Inflammation Metabolic Enzyme/Protease
  2. STAT Keap1-Nrf2 Reactive Oxygen Species
  3. Garcinone D

Garcinone D is an activator of the STAT3/Cyclin D1 and Nrf2/HO-1 pathways, and an inhibitor of CDK2/CyclinE1 (IC50 for CDK2/CyclinE1 is 28.23 μM). Garcinone D promotes neural stem cell proliferation by activating STAT3 phosphorylation and Cyclin D1 expression and enhancing the Nrf2/HO-1 signaling pathway. In addition, Garcinone D blocks the tumor cell cycle by inhibiting CDK2/CyclinE1. Garcinone D can promote the proliferation of C17.2 neural stem cells and inhibit prostate and breast cancer.

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Garcinone D Chemical Structure

Garcinone D Chemical Structure

CAS No. : 107390-08-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 2 publication(s) in Google Scholar

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Description

Garcinone D is an activator of the STAT3/Cyclin D1 and Nrf2/HO-1 pathways, and an inhibitor of CDK2/CyclinE1 (IC50 for CDK2/CyclinE1 is 28.23 μM). Garcinone D promotes neural stem cell proliferation by activating STAT3 phosphorylation and Cyclin D1 expression and enhancing the Nrf2/HO-1 signaling pathway. In addition, Garcinone D blocks the tumor cell cycle by inhibiting CDK2/CyclinE1. Garcinone D can promote the proliferation of C17.2 neural stem cells and inhibit prostate and breast cancer[1][2].

IC50 & Target[1]

p-STAT3

 

Cellular Effect
Cell Line Type Value Description References
HeLa S3 IC50
> 10 μM
Compound: 13
Cytotoxicity in human HeLaS3 cells incubated for 72 hrs by MTT assay
Cytotoxicity in human HeLaS3 cells incubated for 72 hrs by MTT assay
[PMID: 30978023]
HepG2 IC50
> 10 μM
Compound: 13
Cytotoxicity in human HepG2 cells incubated for 72 hrs by MTT assay
Cytotoxicity in human HepG2 cells incubated for 72 hrs by MTT assay
[PMID: 30978023]
HT-29 IC50
> 10 μM
Compound: 13
Cytotoxicity in human HT-29 cells incubated for 72 hrs by MTT assay
Cytotoxicity in human HT-29 cells incubated for 72 hrs by MTT assay
[PMID: 30978023]
KB IC50
> 10 μM
Compound: 13
Cytotoxicity in human KB cells incubated for 72 hrs by MTT assay
Cytotoxicity in human KB cells incubated for 72 hrs by MTT assay
[PMID: 30978023]
MCF7 IC50
> 10 μM
Compound: 13
Cytotoxicity in human MCF7 cells incubated for 72 hrs by MTT assay
Cytotoxicity in human MCF7 cells incubated for 72 hrs by MTT assay
[PMID: 30978023]
In Vitro

Garcinone D (5-400 μM; 24 h) regulates the cell viability of C17.2 neural stem cells. And increases cell viability at 5-10 μM, while significantly reduces cell viability at 20-40 μM[1].
Garcinone D (5 μM; 24 h) promotes the transition of C17.2 neural stem cells in the G1-S phase and arrests the cell cycle in the S phase[1].
Garcinone D (3-10 μM; 6-24 h) increases the levels of p-STAT3, Cyclin D1, Nrf2 and HO-1 proteins in C17.2 neural stem cells in a concentration- and time-dependent manner[1].

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

Cell Viability Assay[1]

Cell Line: C17.2 neural stem cells
Concentration: 5 μM, 10 μM, 20 μM, 40 μM
Incubation Time: 24 h
Result: Significantly increased cell viability at 5 and 10 μM; and significantly decreased cell viability at at 20 and 40 μM.
The percentage of BrdU-positive cells was 1.4-fold higher in the 5 μM group compared with the control, indicating enhanced cell proliferation.
The proportion of cells in the S phase increased from 39.12% to 54.55% after treatment with 5 μM, suggesting promotion of G1-S transition.

Western Blot Analysis[1]

Cell Line: C17.2 neural stem cells
Concentration: 3 μM, 5 μM, 10 μM
Incubation Time: 3 h, 6 h, 12 h, 24 h
Result: Increased the protein levels of p-STAT3, Cyclin D1, Nrf2, and HO-1 in a dose- and time-dependent manner.
Molecular Weight

428.47

Formula

C24H28O7

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C)(O)CCC1=C(OC)C(O)=CC(OC2=CC(O)=C(C/C=C(C)/C)C(O)=C23)=C1C3=O

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 : 50 mg/mL (116.69 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 2.3339 mL 11.6694 mL 23.3389 mL
5 mM 0.4668 mL 2.3339 mL 4.6678 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.83 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 (5.83 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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(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: 99.88%

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 2.3339 mL 11.6694 mL 23.3389 mL 58.3471 mL
5 mM 0.4668 mL 2.3339 mL 4.6678 mL 11.6694 mL
10 mM 0.2334 mL 1.1669 mL 2.3339 mL 5.8347 mL
15 mM 0.1556 mL 0.7780 mL 1.5559 mL 3.8898 mL
20 mM 0.1167 mL 0.5835 mL 1.1669 mL 2.9174 mL
25 mM 0.0934 mL 0.4668 mL 0.9336 mL 2.3339 mL
30 mM 0.0778 mL 0.3890 mL 0.7780 mL 1.9449 mL
40 mM 0.0583 mL 0.2917 mL 0.5835 mL 1.4587 mL
50 mM 0.0467 mL 0.2334 mL 0.4668 mL 1.1669 mL
60 mM 0.0389 mL 0.1945 mL 0.3890 mL 0.9725 mL
80 mM 0.0292 mL 0.1459 mL 0.2917 mL 0.7293 mL
100 mM 0.0233 mL 0.1167 mL 0.2334 mL 0.5835 mL
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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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