Caffeic Acid Phenethyl Ester

Catalog No.S7414 Synonyms: CAPE, Phenylethyl Caffeate

Caffeic Acid Phenethyl Ester Chemical Structure

Molecular Weight(MW): 284.31

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

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2 Customer Reviews

  • The protein expression alteration of p-NF-κB, NF-κB, PD-L1 in NP-69-LMP1 or NP-69 cell lines treated with 0, 0.5, and 1.0 μM Caffeic Acid Phenethyl Ester (CAPE) for 72 hours. β-actin was used to verify equal loading.

    Oncotarget, 2014, 5(23): 12189-202 . Caffeic Acid Phenethyl Ester purchased from Selleck.

    Representative apoptosis assay of LPS141 cells. Summary of apoptosis assay results. Data represent % apoptotic cells ± standard deviation (SD, error bars).

    Sci Rep, 2015, 5: 12580. Caffeic Acid Phenethyl Ester purchased from Selleck.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Caffeic acid phenethyl ester is a potent and specific inhibitor of NF-κB activation, and also displays antioxidant, immunomodulatory and antiinflammatory activities.
Targets
NF-κB [1]
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]

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]

Protocol

Cell Research
+ Expand
  • 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.


    (Only for Reference)
Animal Research
+ Expand
  • Animal Models: C57BL/6 and BALB/c mice inoculated with Lewis lung carcinoma, colon carcinoma, and melanoma cells
  • Formulation: PBS
  • Dosages: ~10 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 57 mg/mL (200.48 mM)
Ethanol 57 mg/mL (200.48 mM)
Water <1 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 284.31
Formula

C17H16O4

CAS No. 104594-70-9
Storage powder
in solvent
Synonyms CAPE, Phenylethyl Caffeate

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02767752 Not yet recruiting Pancreatic Cancer Herlev Hospital|GENIS September 2016 Phase 2
NCT00960544 Not yet recruiting Breast Cancer M.D. Anderson Cancer Center|Myriad Genetic Laboratories, Inc. September 2016 Phase 2
NCT02831179 Not yet recruiting Functional Pancreatic Neuroendocrine Tumor|Malignant Somatostatinoma|Merkel Cell Carcinoma|Metastatic Adrenal Gland Pheochromocytoma|Metastatic Carcinoid Tumor|Multiple Endocrine Neoplasia Type 1|Multiple Endocrine Neoplasia Type 2A|Multiple Endocrine Neoplasia Type 2B|Neuroendocrine Neoplasm|Non-Functional Pancreatic Neuroendocrine Tumor|Pancreatic Glucagonoma|Pancreatic Insulinoma|Recurrent Adrenal Cortex Carcinoma|Recurrent Adrenal Gland Pheochromocytoma|Recurrent Merkel Cell Carcinoma|Somatostatin-Producing Neuroendocrine Tumor|Stage III Adrenal Cortex Carcinoma|Stage III Thyroid Gland Medullary Carcinoma|Stage IIIA Merkel Cell Carcinoma|Stage IIIB Merkel Cell Carcinoma|Stage IV Adrenal Cortex Carcinoma|Stage IV Merkel Cell Carcinoma|Stage IVA Thyroid Gland Medullary Carcinoma|Stage IVB Thyroid Gland Medullary Carcinoma|Stage IVC Thyroid Gland Medullary Carcinoma|Thymic Carcinoid Tumor|VIP-Producing Neuroendocrine Tumor|Well Differentiated Adrenal Cortex Carcinoma|Zollinger Ellison Syndrome Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) August 2016 Phase 1
NCT02795988 Not yet recruiting Gastrointestinal Neoplasms|Adenocarcinoma Imugene Limited August 2016 Phase 1|Phase 2
NCT02574455 Not yet recruiting Breast Cancer Immunomedics, Inc. July 2016 Phase 3
NCT02830139 Not yet recruiting Malignant Neoplasm of Colorectum Wuhan University July 2016 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID