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Caffeic Acid Phenethyl Ester

Name: Caffeic Acid Phenethyl Ester
Brand: Selleck Chemicals
SKU: S7414
Rating: 5 (54 reviews)

Synonyms: CAPE, Phenylethyl Caffeate

Catalog No.S7414 Purity:99.99%

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

CAS No. 104594-70-9

Purity & Quality Control

Batch: Purity: 99.99%

99.99

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Signaling Pathway

NF-κB Signaling Pathway

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	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
Click to View More Cell Line Experimental Data

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

References

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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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.800mg/ml (9.85mM)	Taking the 1 mL working solution as an example, add 50 μL of 56 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.700mg/ml (2.46mM)	Taking the 1 mL working solution as an example, add 50 μL of 14 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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.

Handling Instructions

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