Caffeic acid phenethyl ester [104594-70-9]

Référence HY-N0274-100mg

Conditionnement : 100mg

Marque : MedChemExpress

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Description

Caffeic acid phenethyl ester is a NF-κB inhibitor.

IC50 & Target[1]

NF-κB

 

Cellular Effect
Cell Line Type Value Description References
786-0 IC50
26.8 μM
Compound: 2; CAPE
Cytotoxicity against VHL-deficient human 786-0 cells assessed as reduction in cell viability incubated for 4 days by XTT assay
Cytotoxicity against VHL-deficient human 786-0 cells assessed as reduction in cell viability incubated for 4 days by XTT assay
[PMID: 31260889]
786-0 IC50
43.8 μM
Compound: 2; CAPE
Cytotoxicity against VHL-positive human 786-0 cells assessed as reduction in cell viability incubated for 4 days by XTT assay
Cytotoxicity against VHL-positive human 786-0 cells assessed as reduction in cell viability incubated for 4 days by XTT assay
[PMID: 31260889]
A2780 EC50
3.5 μM
Compound: 17; CAPE
Cytotoxicity against human A2780 cells measured after 96 hrs by SRB assay
Cytotoxicity against human A2780 cells measured after 96 hrs by SRB assay
[PMID: 31158743]
A549 EC50
27.9 μM
Compound: 14
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
[PMID: 12027739]
A549 IC50
10 μM
Compound: CAPE
Growth inhibition of human A549 cells
Growth inhibition of human A549 cells
[PMID: 28814374]
A549 IC50
26.8 μM
Compound: 1, CAPE
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
[PMID: 20673727]
A549 IC50
80 μM
Compound: 2; CAPE
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 33210536]
A549 IC50
83.6 μM
Compound: III-19
Cytotoxicity against human A549 cells by MTT assay
Cytotoxicity against human A549 cells by MTT assay
[PMID: 18952420]
A549 IC50
9.72 μM
Compound: CAPE
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
[PMID: 26638042]
B16-BL6 EC50
6.79 μM
Compound: 14
Antiproliferative activity against mouse B16-BL6 cells after 72 hrs by MTT assay
Antiproliferative activity against mouse B16-BL6 cells after 72 hrs by MTT assay
[PMID: 12027739]
B16-F10 IC50
10.68 μM
Compound: CAPE
Antiproliferative activity against mouse B16F10 cells after 72 hrs by MTT assay
Antiproliferative activity against mouse B16F10 cells after 72 hrs by MTT assay
[PMID: 26638042]
Bel-7402 IC50
5.5 μM
Compound: III-19
Cytotoxicity against human Bel7402 cells by MTT assay
Cytotoxicity against human Bel7402 cells by MTT assay
[PMID: 18952420]
BEL-7404 tumor cell line IC50
14.5 μM
Compound: 1, CAPE
Cytotoxicity against human Bel7404 cells after 72 hrs by MTT assay
Cytotoxicity against human Bel7404 cells after 72 hrs by MTT assay
[PMID: 20673727]
BeWo IC50
2.96 μM
Compound: I-18
Antitumor activity against human Bewo cells assessed as inhibition of cell growth by MTT assay
Antitumor activity against human Bewo cells assessed as inhibition of cell growth by MTT assay
[PMID: 25160837]
BGC-823 IC50
19.3 μM
Compound: 1, CAPE
Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay
Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay
[PMID: 20673727]
BV-2 IC50
6.4 μM
Compound: 1, CAPE
Antineuroinflammatory activity in mouse BV2 cells assessed as reduction of LPS-induced nitric oxide production treated 3 hrs before LPS addition measured after 24 hrs by Griess assay
Antineuroinflammatory activity in mouse BV2 cells assessed as reduction of LPS-induced nitric oxide production treated 3 hrs before LPS addition measured after 24 hrs by Griess assay
[PMID: 23726032]
BV-2 IC50
6.4 μM
Compound: 1, CAPE
Inhibition of nitric oxide production in LPS-stimulated mouse BV2 cells treated 3 hrs before LPS addition measured after 24 hrs by Griess assay
Inhibition of nitric oxide production in LPS-stimulated mouse BV2 cells treated 3 hrs before LPS addition measured after 24 hrs by Griess assay
[PMID: 23870700]
BV-2 IC50
6.4 μM
Compound: 1, CAPE
Antineuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 3 hrs followed by LPS challenge measured after 24 hrs by Griess assay
Antineuroinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 3 hrs followed by LPS challenge measured after 24 hrs by Griess assay
[PMID: 24697335]
Caco-2 IC50
11.35 μM
Compound: CAPE
Antiproliferative activity against human Caco2 cells after 72 hrs by MTT assay
Antiproliferative activity against human Caco2 cells after 72 hrs by MTT assay
[PMID: 26638042]
CNE IC50
54 μM
Compound: 1, CAPE
Cytotoxicity against human CNE cells after 72 hrs by MTT assay
Cytotoxicity against human CNE cells after 72 hrs by MTT assay
[PMID: 20673727]
DU-145 IC50
16 μM
Compound: CAPE
Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay
Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay
[PMID: 27979593]
ECa-109 cell line IC50
42.6 μM
Compound: 1, CAPE
Cytotoxicity against human ECA109 cells after 72 hrs by MTT assay
Cytotoxicity against human ECA109 cells after 72 hrs by MTT assay
[PMID: 20673727]
ECa-109 cell line IC50
47.5 μM
Compound: CAPE
Antiproliferative activity against human ECA109 cells after 48 hrs by MTT assay
Antiproliferative activity against human ECA109 cells after 48 hrs by MTT assay
[PMID: 27979593]
FaDu EC50
12.1 μM
Compound: 17; CAPE
Cytotoxicity against human FADU cells measured after 96 hrs by SRB assay
Cytotoxicity against human FADU cells measured after 96 hrs by SRB assay
[PMID: 31158743]
HeLa EC50
2.36 μM
Compound: 14
Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
[PMID: 12027739]
HeLa IC50
0.068 μg/mL
Compound: 9
Antiallergic activity in Ca(2+)-stimulated differentiated human HeLa cells assessed as inhibition of cys-leukotriene release after 6 days by ELISA
Antiallergic activity in Ca(2+)-stimulated differentiated human HeLa cells assessed as inhibition of cys-leukotriene release after 6 days by ELISA
[PMID: 19942440]
HeLa IC50
33 μM
Compound: CAPE
Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
[PMID: 27979593]
HeLa IC50
37.98 μM
Compound: I-18
Antitumor activity against human HeLa cells assessed as inhibition of cell growth by MTT assay
Antitumor activity against human HeLa cells assessed as inhibition of cell growth by MTT assay
[PMID: 25160837]
HeLa IC50
8.8 μM
Compound: 1, CAPE
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
[PMID: 20673727]
HepG2 IC50
40.87 μM
Compound: I-18
Antitumor activity against human HepG2 cells assessed as inhibition of cell growth by MTT assay
Antitumor activity against human HepG2 cells assessed as inhibition of cell growth by MTT assay
[PMID: 25160837]
HL-60 IC50
16.65 μM
Compound: I-18
Antitumor activity against human HL60 cells assessed as inhibition of cell growth by MTT assay
Antitumor activity against human HL60 cells assessed as inhibition of cell growth by MTT assay
[PMID: 25160837]
HL-60 IC50
9.8 μM
Compound: 1, CAPE
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
[PMID: 20673727]
HT-1080 EC50
9.5 μM
Compound: 14
Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay
Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay
[PMID: 12027739]
HT-29 EC50
>30 μM
Compound: 17; CAPE
Cytotoxicity against human HT-29 cells measured after 96 hrs by SRB assay
Cytotoxicity against human HT-29 cells measured after 96 hrs by SRB assay
[PMID: 31158743]
HUVEC EC50
8 μM
Compound: CAPE
Cytoprotective activity against H2O2-induced oxidative stress in HUVEC cells after 18 hrs by Cell-Titer Blue assay
Cytoprotective activity against H2O2-induced oxidative stress in HUVEC cells after 18 hrs by Cell-Titer Blue assay
[PMID: 20598894]
IMR-32 IC50
5 μM
Compound: 2; CAPE
Cytotoxicity against human IMR-32 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human IMR-32 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 33210536]
J774.1 IC50
4.8 μM
Compound: CAPE
Inhibition of LPS-induced NO production in mouse J774.1 cells after 24 hrs by Griess reagent assay
Inhibition of LPS-induced NO production in mouse J774.1 cells after 24 hrs by Griess reagent assay
[PMID: 15974608]
JJN-3 IC50
30 μM
Compound: 2; CAPE
Growth inhibition of human JJN-3 cells after 48 hrs by PrestoBlue cell viability assay
Growth inhibition of human JJN-3 cells after 48 hrs by PrestoBlue cell viability assay
[PMID: 33210536]
K562 IC50
46 μM
Compound: 1, CAPE
Cytotoxicity against human K562 cells after 72 hrs by MTT assay
Cytotoxicity against human K562 cells after 72 hrs by MTT assay
[PMID: 20673727]
KB IC50
45.2 μM
Compound: 1, CAPE
Cytotoxicity against human KB cells after 72 hrs by MTT assay
Cytotoxicity against human KB cells after 72 hrs by MTT assay
[PMID: 20673727]
KMM-1 IC50
37.5 μM
Compound: 2; CAPE
Growth inhibition of human KMM-1 cells after 48 hrs by PrestoBlue cell viability assay
Growth inhibition of human KMM-1 cells after 48 hrs by PrestoBlue cell viability assay
[PMID: 33210536]
LNCaP IC50
33.7 μM
Compound: 2, CAPE
Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 24 hrs by WST-1 assay
Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 24 hrs by WST-1 assay
[PMID: 24080105]
LNCaP IC50
6.2 μM
Compound: 2, CAPE
Antiandrogenic activity in human LNCAP cells assessed as reduction in DHT-stimulated PSA release after 24 hrs by ELISA
Antiandrogenic activity in human LNCAP cells assessed as reduction in DHT-stimulated PSA release after 24 hrs by ELISA
[PMID: 24080105]
LS174T IC50
9.9 μM
Compound: 1, CAPE
Cytotoxicity against human LS 174T cells after 72 hrs by MTT assay
Cytotoxicity against human LS 174T cells after 72 hrs by MTT assay
[PMID: 20673727]
Macrophage IC50
15 μM
Compound: CAPE
Inhibition of LPS-induced NO production in ddY mouse macrophages after 20 hrs by Griess reagent assay
Inhibition of LPS-induced NO production in ddY mouse macrophages after 20 hrs by Griess reagent assay
[PMID: 15270564]
MCF7 EC50
12.1 μM
Compound: 17; CAPE
Cytotoxicity against human MCF7 cells measured after 96 hrs by SRB assay
Cytotoxicity against human MCF7 cells measured after 96 hrs by SRB assay
[PMID: 31158743]
MCF7 IC50
26.7 μM
Compound: III-19
Cytotoxicity against human MCF7 cells by MTT assay
Cytotoxicity against human MCF7 cells by MTT assay
[PMID: 18952420]
MCF7 IC50
28.8 μM
Compound: CAPE
Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
[PMID: 27979593]
NIH3T3 EC50
21.4 μM
Compound: 17; CAPE
Cytotoxicity against mouse NIH/3T3 cells measured after 96 hrs by SRB assay
Cytotoxicity against mouse NIH/3T3 cells measured after 96 hrs by SRB assay
[PMID: 31158743]
PC-12 IC50
2 μM
Compound: CAPE
Neuroprotection activity in rat PC12 cells assessed as reduction in H2O2-induced cell death preincubated for 3 hrs followed by H2O2 addition and measured after 3 hrs by MTS assay
Neuroprotection activity in rat PC12 cells assessed as reduction in H2O2-induced cell death preincubated for 3 hrs followed by H2O2 addition and measured after 3 hrs by MTS assay
[PMID: 30928712]
PC-3 IC50
10.15 μM
Compound: CAPE
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
[PMID: 26638042]
PC-3 IC50
51.4 μM
Compound: 2, CAPE
Antiproliferative activity against human PC3 cells after 72 hrs by trypan blue assay
Antiproliferative activity against human PC3 cells after 72 hrs by trypan blue assay
[PMID: 24080105]
PC-3 IC50
91 μM
Compound: 1, CAPE
Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
[PMID: 20673727]
Peritoneal macrophage IC50
4.31 μM
Compound: 5; CAPE
Anti-inflammatory activity in ICR mouse peritoneal macrophages assessed inhibition of LPS-induced TNF-alpha production preincubated for 30 to 60 mins followed by LPS stimulation measured after 24 hrs by ELISA
Anti-inflammatory activity in ICR mouse peritoneal macrophages assessed inhibition of LPS-induced TNF-alpha production preincubated for 30 to 60 mins followed by LPS stimulation measured after 24 hrs by ELISA
[PMID: 29202400]
Peritoneal macrophage cell IC50
11 μM
Compound: CAPE
Hepatoprotective activity in ddY mouse peritoneal macrophages assessed as inhibition of LPS-induced nitric oxide production after 20 hrs by Griess method relative to untreated control
Hepatoprotective activity in ddY mouse peritoneal macrophages assessed as inhibition of LPS-induced nitric oxide production after 20 hrs by Griess method relative to untreated control
[PMID: 19775895]
RAW264.7 EC50
0.193 μM
Compound: Table 1, R23C1
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
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
[PMID: 18667320]
RAW264.7 EC50
4.518 μM
Compound: Table 1, R23C1
Cytotoxicity against mouse RAW264.7 cells assessed as cell survival after 24 hrs by MTT assay
Cytotoxicity against mouse RAW264.7 cells assessed as cell survival after 24 hrs by MTT assay
[PMID: 18667320]
RAW264.7 IC50
0.39 μM
Compound: CAPE
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of NO production pretreated for 1 hr followed by LPS addition and measured after 24 hrs by griess reagent based assay
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of NO production pretreated for 1 hr followed by LPS addition and measured after 24 hrs by griess reagent based assay
[PMID: 37976711]
RAW264.7 IC50
3.8 μM
Compound: CAPE
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 10 mins prior to LPS-challenge measured after 18 hrs by Griess method
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 10 mins prior to LPS-challenge measured after 18 hrs by Griess method
[PMID: 22831798]
RAW264.7 IC50
9.3 μM
Compound: CAPE
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production by measuring nitrite accumulation by Griess method
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production by measuring nitrite accumulation by Griess method
[PMID: 28561586]
RCC4 IC50
14 μM
Compound: 2; CAPE
Cytotoxicity against VHL-deficient human RCC4 cells assessed as reduction in cell viability incubated for 4 days by XTT assay
Cytotoxicity against VHL-deficient human RCC4 cells assessed as reduction in cell viability incubated for 4 days by XTT assay
[PMID: 31260889]
RCC4/VHL IC50
29.1 μM
Compound: 2; CAPE
Cytotoxicity against VHL-positive human RCC4/VHL cells assessed as reduction in cell viability incubated for 4 days by XTT assay
Cytotoxicity against VHL-positive human RCC4/VHL cells assessed as reduction in cell viability incubated for 4 days by XTT assay
[PMID: 31260889]
SGC-7901 IC50
14.26 μM
Compound: I-18
Antitumor activity against human SGC7901 cells assessed as inhibition of cell growth by MTT assay
Antitumor activity against human SGC7901 cells assessed as inhibition of cell growth by MTT assay
[PMID: 25160837]
SiHa IC50
66.92 μM
Compound: I-18
Antitumor activity against human SiHa cells assessed as inhibition of cell growth by MTT assay
Antitumor activity against human SiHa cells assessed as inhibition of cell growth by MTT assay
[PMID: 25160837]
SW-1736 EC50
4.7 μM
Compound: 17; CAPE
Cytotoxicity against human SW1736 cells measured after 96 hrs by SRB assay
Cytotoxicity against human SW1736 cells measured after 96 hrs by SRB assay
[PMID: 31158743]
In Vitro

Caffeic acid phenethyl ester is a NF-κB inhibitor. Cell survival and proliferation of CRPC cell lines are all significantly suppressed by Caffeic acid phenethyl ester (CAPE) treatment dose-dependently. The growth inhibitory effect of Caffeic acid phenethyl ester is evident within 24 hours of treatment but the suppressive effect accumulates over time. The IC50 of 24, 48, 72, and 96 h Caffeic acid phenethyl ester treatment on LNCaP 104-R1 cells is 64.0, 30.5, 20.5, and 18.0 μM, respectively. Colony formation assay reveals that treatment with 10 μM Caffeic acid phenethyl ester reduces colony formation of LNCaP 104-R1 cells by 90% while treatment with 20 μM Caffeic acid phenethyl ester completely blocks the formation of LNCaP 104-R1 colonies. Flow cytometric analysis reveals a reduction of cells in the S phase and G2/M phase but an increase of cells in the G1 phase population in LNCaP 104-R1 cells under Caffeic acid phenethyl ester treatment. Caffeic acid phenethyl ester treatment also significantly decreases protein levels of fatty acid synthase (FAS), retinoblastoma protein (Rb), phospho-Rb Ser807/811, c-Myc, p70S6kinase, phospho-p70S6kinase Thr421/Ser424, Skp2, p90RSK, and NF-κB p65[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (351.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5173 mL 17.5864 mL 35.1729 mL
5 mM 0.7035 mL 3.5173 mL 7.0346 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 20 mg/mL (70.35 mM); Clear solution; Need ultrasonic

Pureté et documentation
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