Home NF-κB NF-κB inhibitor Caffeic Acid Phenethyl Ester For research use only.

Caffeic Acid Phenethyl Ester

Synonyms: CAPE, Phenylethyl Caffeate

Caffeic acid phenethyl ester (CAPE, Phenylethyl Caffeate) is a potent and specific inhibitor of NF-κB activation, and also displays antioxidant, immunomodulatory and antiinflammatory activities.

Caffeic Acid Phenethyl Ester Chemical Structure

Caffeic Acid Phenethyl Ester Chemical Structure

CAS No. 104594-70-9

Purity & Quality Control

Caffeic Acid Phenethyl Ester Related Products

Signaling Pathway

NF-κB Signaling Pathways

NF-κB Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse RAW264.7 cells Function assay 24 h Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells assessed as nitrite accumulation administered 1 hr before LPS challenge and measured after 24 hrs by Griess reagent assay, EC50=0.193 μM 18667320
mouse 26-L5 cells Proliferation assay 72 h Antiproliferative activity against mouse 26-L5 cells after 72 hrs by MTT assay, EC50=0.3 μM 12027739
human HeLa cells Proliferation assay 72 h Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay, EC50=2.36 μM 12027739
human Bewo cells Function assay Antitumor activity against human Bewo cells assessed as inhibition of cell growth by MTT assay, IC50=2.96 μM 25160837
mouse J774.1 cells Function assay 24 h Inhibition of LPS-induced NO production in mouse J774.1 cells after 24 hrs by Griess reagent assay, IC50=4.8 μM 15974608
human Bel7402 cells Cytotoxic assay Cytotoxicity against human Bel7402 cells by MTT assay, IC50=5.5 μM 18952420
human LNCAP cells Function assay 24 h Antiandrogenic activity in human LNCAP cells assessed as reduction in DHT-stimulated PSA release after 24 hrs by ELISA, IC50=6.2 nM 24080105
mouse BV2 cells Function assay 24 h Inhibition of nitric oxide production in LPS-stimulated mouse BV2 cells treated 3 hrs before LPS addition measured after 24 hrs by Griess assay, IC50=6.4 μM 23870700
mouse B16-BL6 cells Proliferation assay 72 h Antiproliferative activity against mouse B16-BL6 cells after 72 hrs by MTT assay, EC50=6.79 μM 12027739
HUVEC cells Cytotoxic assay 18 h Cytoprotective activity against H2O2-induced oxidative stress in HUVEC cells after 18 hrs by Cell-Titer Blue assay 20598894
human HT1080 cells Proliferation assay 72 h Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay, EC50=9.5 μM 12027739
human HL60 cells Cytotoxic assay 72 h Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=9.8 μM 20673727
human LS 174T cells Cytotoxic assay 72 h Cytotoxicity against human LS 174T cells after 72 hrs by MTT assay, IC60=9.9 μM 20673727
human SGC7901 cells Function assay Antitumor activity against human SGC7901 cells assessed as inhibition of cell growth by MTT assay, IC50=14.26 μM 25160837
human Bel7404 cells Cytotoxic assay 72 h Cytotoxicity against human Bel7404 cells after 72 hrs by MTT assay, IC50=14.5 μM 20673727
human BGC823 cells Cytotoxic assay 72 h Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay, IC50=19.3 μM 20673727
human HO8910 cells Cytotoxic assay 72 h Cytotoxicity against human HO8910 cells after 72 hrs by MTT assay, IC50=25.5 μM 20673727
human MCF7 cells Cytotoxic assay Cytotoxicity against human MCF7 cells by MTT assay, IC50=26.7 μM 18952420
human A549 cells Cytotoxic assay 72 h Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=26.8 μM 20673727
human LNCAP cells Cytotoxic assay 24 h Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 24 hrs by WST-1 assay, IC50=33.7 μM 24080105
human HeLa cells Function assay Antitumor activity against human HeLa cells assessed as inhibition of cell growth by MTT assay, IC50=37.98 μM 25160837
human HepG2 cells Function assay Antitumor activity against human HepG2 cells assessed as inhibition of cell growth by MTT assay, IC50=40.87 μM 25160837
human ECA109 cells Cytotoxic assay 72 h Cytotoxicity against human ECA109 cells after 72 hrs by MTT assay, IC50=42.6 μM 20673727
human BCG823 cells Cytotoxic assay Cytotoxicity against human BCG823 cells by MTT assay, IC50=44.6 μM 18952420
human KB cells Cytotoxic assay 72 h Cytotoxicity against human KB cells after 72 hrs by MTT assay, IC50=45.2 μM 20673727
human K562 cells Cytotoxic assay 72 h Cytotoxicity against human K562 cells after 72 hrs by MTT assay, IC50=46 μM 20673727
rat VSMC Function assay 5 μM 30 mins Decrease in intracellular ROS level in PDGF-stimulated rat VSMC at 5 uM pretreated with compound for 30 mins measured after up to 23 hrs of post stimulation using H2DCF by flow cytometric analysis 21265554
rat PC12 cells Function assay 2.5 μM 3 h Neuroprotective activity against H2O2-induced damage in rat PC12 cells assessed as cell viability at 2.5 uM preincubated for 3 hrs followed by H2O2 challenge measured after 5 hrs by MTT assay 24697335
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Biological Activity

Description Caffeic acid phenethyl ester (CAPE, Phenylethyl Caffeate) is a potent and specific inhibitor of NF-κB activation, and also displays antioxidant, immunomodulatory and antiinflammatory activities.
Targets
NF-κB [1]
In vitro
In vitro Caffeic acid phenethyl ester blocks NF-κB activation induced by phorbol ester, ceramide, okadaic acid, and hydrogen peroxide by preventing the translocation of the p65 subunit of NF-κB to the nucleus. [1] In a series of tumor cell lines, Caffeic acid phenethyl ester shows promising antiproliferative activity with EC50 of 1.76, 3.16, 13.7, and 44.0 μM against murine colon 26-L5, murine B16-BL6 melanoma, human HT-1080 fibrosarcoma and human lung A549 adenocarcinoma cell lines, respectively. [2] Caffeic acid phenethyl ester, as a potent antioxidant, exerts its anti-apoptotic effect in cerebellar granule cells by blocking ROS formation and inhibiting caspase activity. [3] Moreover, Caffeic acid phenethyl ester attenuates the pro-inflammatory phenotype of LPS-stimulated HSCs, and LPS-induced sensitization of HSCs to fibrogenic cytokines by inhibiting NF-κB signaling. [4]
Cell Research Cell lines Murine colon 26-L5, murine B16-BL6 melanoma, human HT-1080 fibrosarcoma and human lung A549 adenocarcinoma cell lines
Concentrations ~200 μM
Incubation Time 3 days
Method

Human HT-1080 fibrosarcoma, human lung A549 adenocarcinoma and murine B16-BL6 melanoma cell lines are maintained in EMEM medium supplemented with 10% FCS, 0.1% sodium bicarbonate and 2 mM glutamine. Murine colon 26-L5 carcinoma cell line, on the other hand, is maintained in RPMI medium containing the same supplements as in EMEM. These are all highly metastatic cell lines except for A-549 carcinoma. Cellular viability is determined using the standard MTT assay. In brief, exponentially growing cells are harvested and 100 μl of cell suspension containing 2000 cells is plated in 96-well microtiter plates. After 24 h of incubation to allow for cell attachment, the cells are treated with varying concentrations of test samples in medium (100 μl) and incubated for 72 h at 37°C under 5% CO2. Three hours after the addition of MTT, the amount of formazan formed is measured spectrophotometrically at 550 nm with a Perkin Elmer HTS-7000 plate reader. The test samples are first dissolved in DMSO and then diluted with medium; the final concentration of DMSO is less than 0.25%. Normal also had the same extent of DMSO. 5-Fluorouracil (5-FU) and doxorubicin HCl are used as positive controls, and EC50 values are calculated from the mean values of data from 4 wells.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-p65 / CDH6 / RUNX2 / E-cadherin / N-cadherin / Vimentin / Slug / Snail Nrf2 AKT / AKT1 / AKT2 / AKT3 / p-AKT / FOXO1 / FOXO3a / p-FOXO1 / p-FOXO3a / Skp2 / p27(Kip) / Cyclin D1 / Rb / p-Rb 29284791
Immunofluorescence NF-κB 29284791
Growth inhibition assay Cell number 23615471
In Vivo
In vivo In vivo, Caffeic acid phenethyl ester (10 mg/kg, i.p.) inhibits the growth and angiogenesis of primary tumors in C57BL/6 and BALB/c mice inoculated with Lewis lung carcinoma, colon carcinoma, and melanoma cells. [5] Caffeic acid phenethyl ester (5, 10, 20 mg/kg) also shows immunomodulatory effects in vivo by decreasing thymus weight and/or cellularity of thymus and spleen. [6]
Animal Research Animal Models C57BL/6 and BALB/c mice inoculated with Lewis lung carcinoma, colon carcinoma, and melanoma cells
Dosages ~10 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05726708 Recruiting
Autism Spectrum Disorder
Centre Hospitalier Universitaire Vaudois
 October 24 2023 Not Applicable
NCT05934019 Recruiting
Mental Health Issue|Transdiagnostic Mechanisms|Adolescent Psychology|Prevention|Online Intervention|Psychological Intervention|Mental Disorder in Adolescence Subclinical
University of Bern
 June 9 2023 Not Applicable

Chemical Information & Solubility

Molecular Weight 284.31 Formula

C17H16O4
CAS No. 104594-70-9 SDF Download Caffeic Acid Phenethyl Ester SDF
Smiles C1=CC=C(C=C1)CCOC(=O)C=CC2=CC(=C(C=C2)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 56 mg/mL ( (196.96 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 56 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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