Caffeic Acid Phenethyl Ester

Catalog No.S7414 Batch:S741402

Technical Data

Formula	C₁₇H₁₆O₄
Molecular Weight	284.31	CAS No.	104594-70-9
Solubility (25°C)*	In vitro	DMSO	57 mg/mL (200.48 mM)
		Ethanol	57 mg/mL (200.48 mM)
		Water	Insoluble
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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 (from reference)

Cell Assay:^{^[2]}	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.
Animal Study:^{^[5]}	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.

Cell Assay:^{^[2]}

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.

Animal Study:^{^[5]}

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.

References

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Customer Product Validation

: Data from [Data independently produced by , , Oncotarget, 2014, 5(23): 12189-202 ]

: Data from [Data independently produced by , , Sci Rep, 2015, 5: 12580]

: Data from [Data independently produced by , , Carbohydr Polym, 2018, 202:134-142]

: Data from [Data independently produced by , , Oncotarget, 2016, 7(25):38539-38550]

Selleck's Caffeic Acid Phenethyl Ester has been cited by 52 publications

Osteopontin deficiency promotes cartilaginous endplate degeneration by enhancing the NF-κB signaling to recruit macrophages and activate the NLRP3 inflammasome [ Bone Res, 2024, 12(1):53]	PubMed: 39242551
Calpain-2 mediates SARS-CoV-2 entry via regulating ACE2 levels [ mBio, 2024, e0228723.]	PubMed: 38349185
Clarithromycin Modulates Neutrophilic Inflammation Induced by Prevotella intermedia in Human Airway Epithelial Cells [ Antibiotics (Basel), 2024, 13(9)909]	PubMed: 39335081
Caffeic acid phenethyl ester restores mitochondrial homeostasis against peritoneal fibrosis induced by peritoneal dialysis through the AMPK/SIRT1 pathway [ Ren Fail, 2024, 46(1):2350235]	PubMed: 38721924
Caffeic Acid Phenethyl Ester Suppresses Oxidative Stress and Regulates M1/M2 Microglia Polarization via Sirt6/Nrf2 Pathway to Mitigate Cognitive Impairment in Aged Mice following Anesthesia and Surgery [ Antioxidants (Basel), 2023, 12(3)714]	PubMed: 36978961
Caffeic acid phenethyl ester suppresses metastasis of breast cancer cells by inactivating FGFR1 via MD2 [ PLoS One, 2023, 18(7):e0289031]	PubMed: 37490511
Androgen Receptor Regulation in Prostate Stroma [ THE UNIVERSITY OF ARIZONA, 2023, ]	PubMed: none
Chronic Inflammation Pathway NF-κB Cooperates with Epigenetic Reprogramming to Drive the Malignant Progression of Glioblastoma [ Int J Biol Sci, 2022, 18(15):5770-5786]	PubMed: 36263173
Cancer-associated fibroblast-induced lncRNA UPK1A-AS1 confers platinum resistance in pancreatic cancer via efficient double-strand break repair [ Oncogene, 2022, 10.1038/s41388-022-02253-6]	PubMed: 35264742
Comprehensive drug response profiling and pan-omic analysis identified therapeutic candidates and prognostic biomarkers for Asian cholangiocarcinoma [ iScience, 2022, 25(10):105182]	PubMed: 36248745

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SHIPPING AND STORAGE
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