Cat. No.: HY-N6257

Cafestol

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

Cafestol is an orally active diterpenoid and an inhibitor of ERK2. Cafestol has elevated blood lipids, anti-inflammatory, anti-angiogenic and anti-diabetic activities. In addition, Cafestol induces tumor cell apoptosis and autophagy, which can be used in the study of cancer.

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Pureté: 99.20%
CAS No.: 469-83-0
Formule: C₂₀H₂₈O₃
Masse moléculaire:316.43

Stockage:

4°C, protect from light

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

Cafestol Chemical Structure

CAS No.: 469-83-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

COX-2

NF-κB

ERK2

Voir tous les produits spécifiques à Isoform ERK :

Voir tous les produits spécifiques à Isoform COX :

Voir tous les produits spécifiques à Isoform NF-κB :

Voir tous les produits spécifiques à Isoform AP-1 :

In Vitro

Cafestol (0-100 μM; 6-24 h) inhibits PGE₂ production in a dose-dependent manner, with an IC₅₀ of 45.7 μM, and decreases COX-2 mRNA levels in LPS (HY-D1056) treated macrophages^[1].
Cafestol (0-100 μM; 1 h) inhibits AP-1 activation and ERK2 activity in LPS (HY-D1056) treated macrophages^[1].
Cafestol (0-80 μM; 6-24 h) inhibits the proliferation, migration and lumen formation of human umbilical vein endothelial cells by inhibiting the phosphorylation of FAK, Akt and the production of NO^[2].
Cafestol (20-80 μM; 24-72 h) inhibits the proliferation of HCT116 cells and induces autophagy through LKB1/AMPK/ULK1 pathway^[3].

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

RT-PCR^[1]

Cell Line:

LPS (HY-D1056) treated RAW264.7 cells
Concentration:

100 μM
Incubation Time:

6 h
Result:

Significantly reduced the level of COX-2 mRNA.

Western Blot Analysis^[2]

Cell Line:

HUVECs
Concentration:

2.5, 5, 10 and 20 μM
Incubation Time:

1.5 h
Result:

Inhibited the phosphorylation of FAK and Akt in a dose-dependent manner.

In Vivo

Cafestol (40-80 mg/kg; oral gavage ; 20 days) has antitumor effect in xenografted mouse model of colon cancer^[3].
Cafestol (0.4-1.1 mg/day; feed administration; 10 weeks) shows antidiabetic activity in KKAy mice^[4].

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

Animal Model:

HCT116 cells treated BALB/C null mice^[3]
Dosage:

40 and 80 mg/kg
Administration:

Oral gavage (i.g.); 20 days
Result:

Increased the body weight, tumor suppression rate and decreased the tumor weight.
Did not change the colonic morphology.
Increased the richness and diversity of intestinal flora in tumor-bearing mice.
Stimulated autophagy in the colon tumors.

Animal Model:

Male KKAy mice^[4]
Dosage:

0.4 and 1.1 mg/day
Administration:

Feed administration; 10 weeks
Result:

Reduced fasting plasma glucose and increased insulin secretion.
Reduced fasting glucagon was 20% lower and insulin sensitivity improved by 42% at dose of 1.1 mg.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 469-83-0
Appearance Solid
Masse moléculaire 316.43
Formule C₂₀H₂₈O₃
Color White to off-white
SMILES

C[C@]12[C@@]3([H])[C@@]4(CC[C@]1([H])C5=C(OC=C5)CC2)C[C@@]([C@](CO)(O)C4)([H])CC3
Structure Classification
- Terpenoids
- Diterpenoids
Initial Source
- Plants
- Rubiaceae
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

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

Publications (2)

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Journal Impact Factor

J Ethnopharmacol

Xihuang pill suppressed primary liver cancer growth by downregulation of AFP and YAP signaling. [Abstract]

2025 Apr 26:348:119891. PMID: 40294663
bioRxiv

An efficient behavioral screening platform classifies natural products and other chemical cues according to their chemosensory valence in C. elegans. [Abstract]

2024 Apr 3:2023.06.02.542933. PMID: 37333363

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (316.03 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

3.1603 mL

15.8013 mL

31.6026 mL

5 mM

0.6321 mL

3.1603 mL

6.3205 mL

10 mM

0.3160 mL

1.5801 mL

3.1603 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.90 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 2

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

Solubility: ≥ 2.5 mg/mL (7.90 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (252 KB)
- English - EN (252 KB)
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- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
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- 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)
Instruction de manipulation (2659 KB)

Références

[1]. Shen T, et al. Cafestol, a coffee-specific diterpene, is a novel extracellular signal-regulated kinase inhibitor with AP-1-targeted inhibition of prostaglandin E2 production in lipopolysaccharide-activated macrophages. Biol Pharm Bull. 2010;33(1):128-32. [Content Brief]

[2]. Wang S, et al. Antiangiogenic properties of cafestol, a coffee diterpene, in human umbilical vein endothelial cells. Biochem Biophys Res Commun. 2012 May 11;421(3):567-71. [Content Brief]

[3]. Feng Y, et al. Cafestol inhibits colon cancer cell proliferation and tumor growth in xenograft mice by activating LKB1/AMPK/ULK1-dependent autophagy. J Nutr Biochem. 2024 Jul;129:109623. [Content Brief]

[4]. Mellbye FB, et al. Cafestol, a Bioactive Substance in Coffee, Has Antidiabetic Properties in KKAy Mice. J Nat Prod. 2017 Aug 25;80(8):2353-2359. [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	3.1603 mL	15.8013 mL	31.6026 mL	79.0064 mL
	5 mM	0.6321 mL	3.1603 mL	6.3205 mL	15.8013 mL
	10 mM	0.3160 mL	1.5801 mL	3.1603 mL	7.9006 mL
	15 mM	0.2107 mL	1.0534 mL	2.1068 mL	5.2671 mL
	20 mM	0.1580 mL	0.7901 mL	1.5801 mL	3.9503 mL
	25 mM	0.1264 mL	0.6321 mL	1.2641 mL	3.1603 mL
	30 mM	0.1053 mL	0.5267 mL	1.0534 mL	2.6335 mL
	40 mM	0.0790 mL	0.3950 mL	0.7901 mL	1.9752 mL
	50 mM	0.0632 mL	0.3160 mL	0.6321 mL	1.5801 mL
	60 mM	0.0527 mL	0.2634 mL	0.5267 mL	1.3168 mL
	80 mM	0.0395 mL	0.1975 mL	0.3950 mL	0.9876 mL
	100 mM	0.0316 mL	0.1580 mL	0.3160 mL	0.7901 mL

Keywords

Cafestol

2 Cited Publications

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Cafestol

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Publications Citing Use of MedChemExpress (MCE) Cafestol

Voir tous les produits spécifiques à Isoform ERK

Voir tous les produits spécifiques à Isoform COX

Voir tous les produits spécifiques à Isoform NF-κB

Voir tous les produits spécifiques à Isoform AP-1

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation