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Cafestol

MCE China：Cafestol

Brand：MedChemExpress (MCE)

Cat. No.HY-N6257

CAS：469-83-0

Purity：99.20%

Storage：4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Shipping：Room temperature in continental US; may vary elsewhere.

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.

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].

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].

IC50 & Target：COX-2 NF-κB ERK2

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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]