2. MAPK/ERK Pathway Stem Cell/Wnt Immunology/Inflammation NF-κB Apoptosis Autophagy Protein Tyrosine Kinase/RTK
  3. ERK PGE synthase COX NF-κB Apoptosis Autophagy AP-1 FAK
  4. Cafestol

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.

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

Cafestol Chemical Structure

Cafestol Chemical Structure

CAS No. : 469-83-0

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Cafestol:

Cafestol Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Cafestol

View All ERK Isoform Specific Products:

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ERK ERK1 ERK2 ERK5 ERK8

View All COX Isoform Specific Products:

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COX COX-1 COX-2 COX-3

View All NF-κB Isoform Specific Products:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

View All AP-1 Isoform Specific Products:

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c-Fos c-Jun

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3][4].

IC50 & Target[1]

COX-2

 

NF-κB

 

ERK2

 

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.

Cafestol Related Antibodies

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.
Clinical Trial
Molecular Weight

316.43

Formula

C20H28O3
CAS No.
Appearance

Solid

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
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 (316.03 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 3.1603 mL 15.8013 mL 31.6026 mL
5 mM 0.6321 mL 3.1603 mL 6.3205 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)

Mass
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Volume
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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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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    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.

    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.
  • 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

mg/kg

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(per animal)

g

Dosing volume
(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

Purity: 99.91%

SDS (252 KB)

COA (249 KB) HNMR (187 KB) RP-HPLC (100 KB)

Handling Instructions (2659 KB)
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 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
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Cafestol Related Classifications

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.

Keywords:

Cafestol469-83-0ERKPGE synthaseCOXNF-κBApoptosisAutophagyAP-1FAKExtracellular signal regulated kinasesProstaglandin E synthaseCyclooxygenaseNuclear factor-κBNuclear factor-kappaBActivator Protein 1PTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseMacrophagesHuman umbilical vein endothelial cellsHCT116 cellsColon cancer modelKKAy miceInhibitorinhibitorinhibit

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