Cafestol
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.
For research use only. We do not sell to patients.
- Purity : 99.20%
- CAS No.: 469-83-0
- Formula: C20H28O3
- Molecular Weight:316.43
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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HY-N6258
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OlaparibPARP Inhibitor -
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GSK126EZH2 Inhibitor -
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3,4-Dicaffeoylquinic acidAntioxidant -
HY-N0056
Isochlorogenic acid AAntioxidant -
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Cryptochlorogenic acidphenolic Acid Compound -
HY-N0058
4,5-Dicaffeoylquinic acidAntioxidant -
HY-N0722
Neochlorogenic acidCOX Inhibitor -
HY-N0414
TrigonellineNrf2 Inhibitor -
HY-N6257R
Cafestol (Standard)ERK2 Inhibitor
Publications Citing Use of MedChemExpress (MCE) Cafestol
MoreAll AP-1 Isoforms
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Biological Activity
Description
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. Further protocols information, click here.
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Cell Line:LPS (HY-D1056) treated RAW264.7 cells
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Concentration:100 μM
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Incubation Time:6 h
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Result:Significantly reduced the level of COX-2 mRNA.
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Cell Line:HUVECs
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Concentration:2.5, 5, 10 and 20 μM
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Incubation Time:1.5 h
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Result:Inhibited the phosphorylation of FAK and Akt in a dose-dependent manner.
In Vivo
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.
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Animal Model:HCT116 cells treated BALB/C null mice[3]
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Dosage:40 and 80 mg/kg
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Administration:Oral gavage (i.g.); 20 days
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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.
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Animal Model:Male KKAy mice[4]
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Dosage:0.4 and 1.1 mg/day
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Administration:Feed administration; 10 weeks
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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
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 469-83-0
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Appearance Solid
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Molecular Weight 316.43
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Formula C20H28O3
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Color White to off-white
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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
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Structure Classification
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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
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Most Recent
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J Ethnopharmacol
Xihuang pill suppressed primary liver cancer growth by downregulation of AFP and YAP signaling. [Abstract]2025 May 28:348:119891. 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
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Autophagy
Autophagy is a process in which eukaryotic cells use lysosomes to degrade their own cytoplasmic proteins and damaged organelles under the regulation of autophagy related gene (Atg). Microtubule-associated proteins light chain 3 (LC3) is recognized as autophagy marker, which transfers from cytoplasmic LC3 (LC3-I) to membrane type (LC3-II). LC3-II/I ratio could be detected by Western Blot and fluorescence microscopy.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Lysosome and acidic-vesicle live-cell staining
Lysosome and acidic-vesicle live-cell staining detects acidic intracellular compartments by using membrane-permeant acidotropic probes that accumulate in low-pH vesicles, including lysosomes, late endosomes, autolysosomes, and acidic phagosomes. LysoTracker staining is commonly used as an intensity-based readout of acidic lysosomal compartment abundance or enlargement, while acridine orange produces green fluorescence in less concentrated compartments and red fluorescence after concentration-dependent accumulation in acidic vesicular organelles. Loss or reduction of acridine-orange red signal can be used as a readout of lysosomal membrane permeabilization or reduced acidic-vesicle integrity. This protocol is designed for live cultured cells and can be adapted for fluorescence microscopy, high-content imaging, plate-reader readout, or flow cytometry when the selected literature supports the readout. Because these dyes report acidotropic accumulation rather than lysosome identity alone,
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Macroautophagy Solutions
Macroautophagy is a conserved lysosome-dependent degradation pathway in which cytoplasmic material is sequestered into double-membrane autophagosomes and delivered to lysosomes for degradation and recycling. The pathway supports cellular homeostasis during nutrient limitation, organelle stress, protein-aggregate accumulation, infection, differentiation, and tissue remodeling by coupling cargo sequestration, autophagosome maturation, lysosomal fusion, and degradation of cargo-derived macromolecules. The core molecular sequence includes initiation by nutrient- and stress-regulated autophagy machinery, autophagosome nucleation, LC3/ATG8-family conjugation to autophagosomal membranes, cargo selection through receptors such as SQSTM1/p62, autophagosome-lysosome fusion, and lysosomal degradation. LC3 was identified as a mammalian homolog of yeast Atg8 that localizes to autophagosomal membranes after processing, and p62/SQSTM1 was shown to connect ubiquitinated cargo with autophagic degradati
Purity & Documentation
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Data Sheet (280 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
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 |
Cafestol Related Classifications
HY-N6257 Related Classifications
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