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CAFESTOL

Catalog No. T5727   CAS 469-83-0

CAFESTOL is a ERK inhibitor for AP-1-targeted activity against PGE2 production and the mRNA expression of cyclooxygenase (COX)-2 in LPS-activated RAW264.7 cells. Cafestol has strong inhibitory activity on PGE2 production by suppressing the NF-kB activation pathway.

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CAFESTOL Chemical Structure
CAFESTOL, CAS 469-83-0
Pack Size Availability Price/USD Quantity
2 mg In stock $ 32.00
5 mg In stock $ 52.00
10 mg In stock $ 85.00
25 mg In stock $ 162.00
50 mg In stock $ 238.00
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Purity: 99.84%
Purity: 99.08%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CAFESTOL is a ERK inhibitor for AP-1-targeted activity against PGE2 production and the mRNA expression of cyclooxygenase (COX)-2 in LPS-activated RAW264.7 cells. Cafestol has strong inhibitory activity on PGE2 production by suppressing the NF-kB activation pathway.
In vitro The precise molecular mechanism of the antiinflammatory activity of cafestol in terms of prostaglandin E(2) (PGE(2)) production, a critical factor involved in inflammatory responses. Cafestol inhibited both PGE(2) production and the mRNA expression of cyclooxygenase (COX)-2 from lipopolysaccharide (LPS)-treated RAW264.7 cells. This compound strongly decreased the translocation of c-Jun into the nucleus and AP-1 mediated luciferase activity. In kinase assays using purified extracellular signal-regulated kinase 2 (ERK2) or immunoprecipitated ERK prepared from LPS-treated cells in the presence or absence of cafestol, it was found that this compound can act as an inhibitor of ERK2 but not of ERK1 and mitogen-activated protein kinase kinase 1 (MEK 1). Suggest that cafestol may be a novel ERK inhibitor with AP-1-targeted inhibitory activity against PGE(2) production in LPS-activated RAW264.7 cells[1].
In vivo CAFESTOL possesses antidiabetic properties in KKAy mice. Consequently, cafestol may contribute to the reduced risk of developing T2D in coffee consumers and has a potential role as an antidiabetic drug[2].
Animal Research Cafestol can postpone development of T2D in KKAy mice. Forty-seven male KKAy mice were randomized to consume chow supplemented daily with either 1.1 (high), 0.4 (low), or 0 (control) mg of cafestol for 10 weeks. Collected blood samples for fasting glucose, glucagon, and insulin as well as liver, muscle, and fat tissues for gene expression analysis. Isolated islets of Langerhans and measured insulin secretory capacity. After 10 weeks of intervention, fasting plasma glucose was 28-30% lower in cafestol groups compared with the control group (p < 0.01). Fasting glucagon was 20% lower and insulin sensitivity improved by 42% in the high-cafestol group (p < 0.05). Cafestol increased insulin secretion from isolated islets by 75-87% compared to the control group (p < 0.001)[2].
Source
Molecular Weight 316.43
Formula C20H28O3
CAS No. 469-83-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5 mg/mL (15.8 mM)

TargetMolReferences and Literature

1. Shen T , Lee J , Lee E , 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[J]. Biological & Pharmaceutical Bulletin, 2010, 33(1):128-132. 2. Mellbye F B , Jeppesen P B , Shokouh P , et al. Cafestol, a Bioactive Substance in Coffee, Has Antidiabetic Properties in KKAy Mice[J]. Journal of Natural Products, 2017:acs.jnatprod.7b00395.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Inhibitor Library Traditional Chinese Medicine Monomer Library Natural Product Library Natural Product Library for HTS Kinase Inhibitor Library Antioxidant Compound Library Anti-Obesity Compound Library Human Metabolite Library MAPK Inhibitor Library

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Keywords

CAFESTOL 469-83-0 Immunology/Inflammation MAPK Neuroscience NF-Κb NF-κB ERK COX PGE Synthase Inhibitor Nuclear factor-kappaB Cyclooxygenase PGE synthase Nuclear factor-κB Prostaglandin E synthase inhibit Extracellular signal regulated kinases inhibitor

 

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