Art. -Nr.: HY-N6046

Kamebakaurin

1 Cited Publications

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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.

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Reinheit: 99.64%
CAS. Nr.: 73981-34-7
Formel: C₂₀H₃₀O₅
Molecular Weight:350.45

Speicherung:

4°C, protect from light

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

Kamebakaurin Chemical Structure

CAS. Nr.: 73981-34-7

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle NF-κB Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
P388	IC₅₀	0.82 μg/mL Compound: 8	Cytotoxicity against mouse P388 cells Cytotoxicity against mouse P388 cells	[PMID: 15043413]

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.

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.

Chemical Information

CAS. Nr. 73981-34-7
Appearance Solid
Molecular Weight 350.45
Formel C₂₀H₃₀O₅
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
- Terpenoids
- Diterpenoids
Initial Source
- Plants
- Labiatae
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

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

Publications (1)

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Journal Impact Factor

iScience

PTEN acts as a crucial inflammatory checkpoint controlling TLR9/IL-6 axis in B cells. [Abstract]

2024 Jun 26;27(7):110388. PMID: 39092178

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8535 mL

14.2674 mL

28.5347 mL

5 mM

0.5707 mL

2.8535 mL

5.7069 mL

10 mM

0.2853 mL

1.4267 mL

2.8535 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (7.13 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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (294 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lee JH, et al. Kaurane diterpene, kamebakaurin, inhibits NF-kappa B by directly targeting the DNA-binding activity of p50 and blocks the expression of antiapoptotic NF-kappa B target genes. J Biol Chem. 2002 May 24;277(21):18411-20. [Content Brief]

[2]. Wang KS, et al. Kamebakaurin inhibits the expression of hypoxia-inducible factor-1α and its target genes to confer antitumor activity. Oncol Rep. 2016 Apr;35(4):2045-52. [Content Brief]

[3]. Yoshioka H, et al. Suppressive effect of kamebakaurin on acetaminophen-induced hepatotoxicity by inhibiting lipid peroxidation and inflammatory response in mice. Pharmacol Rep. 2017 Oct;69(5):903-907. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Kamebakaurin

1 Cited Publications

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Kamebakaurin

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Publications Citing Use of MedChemExpress (MCE) Kamebakaurin

Alle NF-κB Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Kamebakaurin Related Classifications

HY-N6046 Related Classifications