1. NF-κB
  2. NF-κB
  3. Ginsenoside Rk3

Ginsenoside Rk3 is present in the roots Panax ginseng herbs. Ginsenoside Rk3 significantly inhibits TNF-α-induced NF-κB transcriptional activity, with an IC50 of 14.24±1.30 μM in HepG2 cells.

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Ginsenoside Rk3 Chemical Structure

Ginsenoside Rk3 Chemical Structure

CAS No. : 364779-15-7

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5 mg USD 220 In-stock
10 mg USD 370 In-stock
25 mg USD 620 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Ginsenoside Rk3 is present in the roots Panax ginseng herbs. Ginsenoside Rk3 significantly inhibits TNF-α-induced NF-κB transcriptional activity, with an IC50 of 14.24±1.30 μM in HepG2 cells.

IC50 & Target[1]

NF-κB

14.24 μM (IC50, in HepG2 cells)

NF-κB

15.32 μM (IC50, in SK-Hep1 cell)

In Vitro

Ginsenoside Rk3 exerts the strong activity inhibiting NF-κB in a dose-dependent manner. HepG2 cells are pre-treated with different ginsenosides at concentrations ranging from 0.01 to 10 μM for 1 h, and induced with TNF-α for 20 h. Ginsenoside Rk3 significantly inhibits TNF-α-induced NF-κB transcriptional activity, with an IC50 of 14.24±1.30 μM. Ginsenoside Rk3 significantly inhibits TNF-α-induced NF-κB transcriptional activity, with an IC50 of 15.32±0.29 μM in SK-Hep1 cells, consistent with the data from HepG2 cells. Consistent with the inhibition of NF-κB, Ginsenoside Rk3 inhibits the induction of IL8, CXCL1, iNOS, and ICAM1 mRNA significantly in a dose-dependent manner[1].

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

In Vivo

The inhibitory effects of Ginsenoside Rk3 (Rk3) on tumor progression are studied in vivo using a H460 xenograft model in nude mice. Compared with the control group, a significant inhibition of tumor growth (volume) is observed in the Ginsenoside Rk3-treated group. Twenty-one days after treatment initiation, tumor growth is significantly inhibited by approximately 62.99% in the mice receiving 20 mg/kg Ginsenoside Rk3, similar to the inhibitory effect observed in the 20 mg/kg Gefitinib-treated group (57.21%). Compared with the control group, tumor growth is moderately inhibited in the mice receiving 10 and 5 mg/kg Ginsenoside Rk3, with inhibition rates of 32.54% and 11.84%, respectively[2].

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

Molecular Weight

620.86

Formula

C36H60O8

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]([C@@]12C)(C[C@H](O[C@]([C@@H]([C@@H](O)[C@@H]3O)O)([H])O[C@@H]3CO)[C@@]4([H])C5(C)C)[C@@](C[C@@H](O)[C@]1([H])[C@@H](C(CC/C=C(C)/C)=C)CC2)([H])[C@]4(CC[C@@H]5O)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 (161.07 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 1.6107 mL 8.0533 mL 16.1067 mL
5 mM 0.3221 mL 1.6107 mL 3.2213 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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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 (4.03 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 (4.03 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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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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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
References
Cell Assay
[1]

HepG2 and SK-Hep1 cells are maintained in Dulbecco’s modified Eagle’s medium containing 10% heat-inactivated fetal bovine serum, 100 units/mL Penicillin, and 10 μg/mL Streptomycin, at 37°C and 5% CO2. Cell-Counting Kit (CCK)-8 is used to analyze the effect of compounds (e.g., Ginsenoside Rk3; 0.01, 0.1, 1 and 10 uM) on cell toxicity. Cells are cultured overnight in 96-well plate (~1×104 cells/well). Cell toxicity is assessed after the addition of compounds on dose-dependent manner. After 24 h of treatment, 10 μL of the CCK-8 solution is added to triplicate wells, and incubated for 1 h. Absorbance is measured at 450 nm to determine viable cell numbers in wells[1].

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

Animal Administration
[2]

Mice[2]
Four- to 5-week-old male nude mice are selected and housed under aseptic conditions. The animals are exposed to a phase shift of the light/dark cycle for one week and allowed free access to a normal diet. All animal handling is performed under a laminar flow hood. The H460 xenograft model is established. Cell suspensions at a density of 4-5×106 cells are subcutaneously implanted into the left axilla of each mouse. Tumor engraftment is considered successful when the tumors are clearly visible, which occurs after one to two weeks. The tumor-bearing mice are randomly divided into the following 5 groups (5 mice per group) according to tumor size and body weight: control group (0.9% saline solution), Ginsenoside Rk3-treated group (5/10/20 mg/kg), and Gefitinib-treated group (20 mg/kg). The indicated doses (5-20 mg/kg) of Ginsenoside Rk3 are safe for mice as determined by preliminary acute oral toxicity tests. The dose of Gefitinib is based on the results from another study. Mice are intragastrically treated daily for 21 days. The tumor volumes are estimated. The body weights and tumor volumes of the mice in each group are measured twice per week. After 21 days, all animals are euthanized, and all tumor tissues are removed, weighed, and collected.

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

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 1.6107 mL 8.0533 mL 16.1067 mL 40.2667 mL
5 mM 0.3221 mL 1.6107 mL 3.2213 mL 8.0533 mL
10 mM 0.1611 mL 0.8053 mL 1.6107 mL 4.0267 mL
15 mM 0.1074 mL 0.5369 mL 1.0738 mL 2.6844 mL
20 mM 0.0805 mL 0.4027 mL 0.8053 mL 2.0133 mL
25 mM 0.0644 mL 0.3221 mL 0.6443 mL 1.6107 mL
30 mM 0.0537 mL 0.2684 mL 0.5369 mL 1.3422 mL
40 mM 0.0403 mL 0.2013 mL 0.4027 mL 1.0067 mL
50 mM 0.0322 mL 0.1611 mL 0.3221 mL 0.8053 mL
60 mM 0.0268 mL 0.1342 mL 0.2684 mL 0.6711 mL
80 mM 0.0201 mL 0.1007 mL 0.2013 mL 0.5033 mL
100 mM 0.0161 mL 0.0805 mL 0.1611 mL 0.4027 mL
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