2. NF-κB Apoptosis Metabolic Enzyme/Protease
  3. NF-κB Apoptosis Caspase HIF/HIF Prolyl-Hydroxylase
  4. Kamebakaurin

Kamebakaurin is an orally active diterpenoid compound that can be isolated from Isodon excia (Maxin.). Kamebakaurin can inhibit NF-κB activation by directly targeting the DNA-binding activity of p50. Kamebakaurin can induce apoptosis and cell cycle arrest in tumor cells. Kamebakaurin has anti-inflammatory and anti-tumor activities.

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

Kamebakaurin Chemical Structure

Kamebakaurin Chemical Structure

CAS No. : 73981-34-7

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Kamebakaurin Related Antibodies

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HIF-1α HIF

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Description

Kamebakaurin is an orally active diterpenoid compound that can be isolated from Isodon excia (Maxin.). Kamebakaurin can inhibit NF-κB activation by directly targeting the DNA-binding activity of p50. Kamebakaurin can induce apoptosis and cell cycle arrest in tumor cells. Kamebakaurin has anti-inflammatory and anti-tumor activities[1][2][3].

In Vitro

Kamebakaurin (0-10 μg/mL; 8.5 h) can inhibit the expression of NF-κB reporter genes and DNA-binding activities induced by TNF-α, Phorbol 12-myristate 13-acetate (HY-18739), and LPS (HY-D1056) in a dose-dependent manner in various cells such as Jurkat and THP-1[1].
Kamebakaurin (0-10 μg/mL; 3.5-48 h) can inhibit the expression of TNF-α-induced NF-κB target genes and induce apoptosis, significantly enhancing caspase-8 activity in MCF-7 cells[1].
Kamebakaurin (0-30 μM; 12 h) can significantly inhibit the accumulation of hypoxia-induced HIF-1α protein in the cell nucleus of HCT116 cells, as well as inhibit the expression of HIF-1α target genes VEGF and EPO, and can induce cell cycle arrest[2].

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

Kamebakaurin Related Antibodies

Immunofluorescence[2]

Cell Line: HCT116 cells were cultured under hypoxia conditions
Concentration: 30 μM
Incubation Time: 12 h
Result: Decreased the staining of HIF-1α in the cell nucleus.

Western Blot Analysis[2]

Cell Line: HCT116 cells were cultured under hypoxia conditions
Concentration: 0, 3, 10 and 30 μM
Incubation Time: 12 h
Result: Inhibited the VEGF and GLUT-1 protein level.
Inhibited the cyclin D1 and c-Myc protein level.
In Vivo

Kamebakaurin (15-50 mg/kg; oral administration; every other day; 40 days) exhibits anti-tumor activity in a mouse model of colon cancer[2].
Kamebakaurin (100 mg/kg; oral administration; 7 days) can inhibit Acetaminophen (APAP) (HY-66005)-induced hepatotoxicity when used for pretreatment in C57BL/6J mice[3].

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

Animal Model: Crj:BALB/c nu/nu female athymic nude mice aged six weeks old treated HCT116 cells[2]
Dosage: 15 and 50 mg/kg
Administration: Oral administration; every other day for 40 days
Result: Significantly inhibited the growth of HCT116 cells in the xenograft tumor model at a dose of 50 mg/kg.
Significantly decreased the protein levels of HIF-1α in the tumors, while having no significant effect on Topo-I levels
Significantly decreased the serum VEGF levels in a dose-dependent manner.
Animal Model: Female C57BL/6J mice aged 6 weeks old treated APAP(HY-66005)[2]
Dosage: 100 mg/kg
Administration: Oral administration; 7 days
Result: Significantly reduced the increases in plasma levels of hepatic injury markers (ALT and AST) induced by APAP.
Eliminated the APAP-induced upregulation of hepatic MDA levels and significantly decreased the GSH depletion caused by APAP.
Attenuated the APAP-induced increase in hepatic and plasma TNFα levels, and there was a tendency for a decrease in IL-6 mRNA levels.
Showed antioxidant capacity, with its total antioxidant power increasing in a dose-dependent manner, although its radical scavenging activity was relatively small
Did not significantly change the expression of hepatic CYP2e1 and CYP1a2 mRNA.
Molecular Weight

350.45

Formula

C20H30O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]1[C@@]23[C@](CC[C@@]1([H])C(C3=O)=C)([H])[C@]4([C@](C(C)(CC[C@@H]4O)C)([H])C[C@H]2O)CO
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 (285.35 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 2.8535 mL 14.2674 mL 28.5347 mL
5 mM 0.5707 mL 2.8535 mL 5.7069 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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 (7.13 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 (7.13 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)

μL

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
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 2.8535 mL 14.2674 mL 28.5347 mL 71.3369 mL
5 mM 0.5707 mL 2.8535 mL 5.7069 mL 14.2674 mL
10 mM 0.2853 mL 1.4267 mL 2.8535 mL 7.1337 mL
15 mM 0.1902 mL 0.9512 mL 1.9023 mL 4.7558 mL
20 mM 0.1427 mL 0.7134 mL 1.4267 mL 3.5668 mL
25 mM 0.1141 mL 0.5707 mL 1.1414 mL 2.8535 mL
30 mM 0.0951 mL 0.4756 mL 0.9512 mL 2.3779 mL
40 mM 0.0713 mL 0.3567 mL 0.7134 mL 1.7834 mL
50 mM 0.0571 mL 0.2853 mL 0.5707 mL 1.4267 mL
60 mM 0.0476 mL 0.2378 mL 0.4756 mL 1.1889 mL
80 mM 0.0357 mL 0.1783 mL 0.3567 mL 0.8917 mL
100 mM 0.0285 mL 0.1427 mL 0.2853 mL 0.7134 mL
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Kamebakaurin 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.

Keywords:

Kamebakaurin73981-34-7NF-κBApoptosisCaspaseHIF/HIF Prolyl-HydroxylaseNuclear factor-κBNuclear factor-kappaBHypoxia-inducible factorsHIFsHIF-PHcolon cancer modelJurkatTHP-1MCF-7HCT116Inhibitorinhibitorinhibit

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