Cephaeline
Based on 2 publication(s) in Google Scholar
Cephaeline ((-)-Cephaeline), a desmethyl analog of Emetine, is a phenolic alkaloid in Indian Ipecac roots isolated from the Cephaelis ipecacuanha. Cephaeline exhibits potent inhibition of both Zika virus (ZIKV) and Ebola virus (EBOV) infections. Cephaeline is an inductor of histone H3 acetylation and an inhibitor of mucoepidermoid carcinoma cancer stem cells (MEC), which promotes ferroptosis by inhibiting NRF2 to exert anti-lung cancer efficacy.
For research use only. We do not sell to patients.
- Purity: 99.77%
- CAS No.: 483-17-0
- Formula: C28H38N2O4
- Molecular Weight:466.61
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) Cephaeline
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
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WB
Biological Activity
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EBOV |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
3 μM
Compound: 9
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Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 31513408] |
| BT-549 | IC50 |
0.86 μg/mL
Compound: 3
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Cytotoxicity against human BT549 cells
Cytotoxicity against human BT549 cells
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[PMID: 12880315] |
| HEK-293T | CC50 |
2 μM
Compound: 97
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Cytotoxicity against human HEK293T cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human HEK293T cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
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[PMID: 37597436] |
| HeLa | IC50 |
>10 μg/mL
Compound: 3
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Inhibition of LFA1:CD11a/CD18/ICAM1-mediated human HL60 cell adhesion to human HeLa cells expressing ICAM1 by fluorescence analysis
Inhibition of LFA1:CD11a/CD18/ICAM1-mediated human HL60 cell adhesion to human HeLa cells expressing ICAM1 by fluorescence analysis
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[PMID: 12880315] |
| HeLa | IC50 |
7.6 μM
Compound: 9
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Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 31513408] |
| HL-60 | IC50 |
14.9 μg/mL
Compound: 3
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Cytotoxicity against human HL60 cells by XTT assay
Cytotoxicity against human HL60 cells by XTT assay
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[PMID: 12880315] |
| Huh-7 | CC50 |
3.03 μM
Compound: 97
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Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 37597436] |
| KB | IC50 |
0.33 μg/mL
Compound: 3
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Cytotoxicity against human KB cells
Cytotoxicity against human KB cells
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[PMID: 12880315] |
| SK-MEL | IC50 |
0.25 μg/mL
Compound: 3
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Cytotoxicity against human SK-MEL cells
Cytotoxicity against human SK-MEL cells
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[PMID: 12880315] |
| SK-OV-3 | IC50 |
0.1 μM
Compound: 9
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Cytotoxicity against human SKOV3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human SKOV3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 31513408] |
| SK-OV-3 | IC50 |
0.18 μg/mL
Compound: 3
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Cytotoxicity against human SKOV3 cells
Cytotoxicity against human SKOV3 cells
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[PMID: 12880315] |
| Vero | CC50 |
46.327 μM
Compound: 97
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Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by MTS assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by MTS assay
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[PMID: 37597436] |
| Vero | IC50 |
5.3 μg/mL
Compound: 3
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Cytotoxicity against african green monkey Vero cells
Cytotoxicity against african green monkey Vero cells
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[PMID: 12880315] |
Cephaeline (1-1000 nM, 1 h) inhibits ZIKV NS5 RdRp in the polymerase activity assay with an IC50 value of 976 nM in HEK293 cells[2].
Cephaeline (0.1-1000 μM, 72 h) shows the inhibition effect on Ebola VLP entry with an IC50 value of 3.27 μM in HeLa cells and infection of Ebola live virus with an IC50 value of 22.18 nM in Vero E6 cells[2].
Cephaeline (0-32 μM, 72 h) inhibits cellular viability, growth and migration in mucoepidermoid carcinoma (MEC) cell lines[3].
Cephaeline (5-400 nM, 24, 48 and 72h) induces lung cancer cell death in lung cancer cell line H460 and A549[4].
Cephaeline (0.16, 2.08 and 0.02 μM, 24 h and 48 h) progressively increases histone acetylation in MEC cell lines[3].
Cephaeline (0-100 nM, 24 h) induces ferroptosis in lung cancer cells by targeting NRF2[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells
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Concentration:1-1000 nM
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Incubation Time:1 h
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Result:Showed the inhibition effect on the RNA polymerase activity of recombinant Zika NS5 enzyme in HEK293 cells.
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Cell Line:Vero E6 cells
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Concentration:0-2 μM
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Incubation Time:72 h
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Result:Inhibited EBOV entry and replication in Vero E6 cells.
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Cell Line:Mucoepidermoid carcinoma (MEC) cell lines
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Concentration:0-32 μM
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Incubation Time:72 h
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Result:Inhibited the cell viability of UM-HMC-1, UM-HMC-2 and UM-HMC-3A with IC50 values of 0.16 μM, 2.08 μM and 0.02 μM, respectively.
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Cell Line:MEC cell lines
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Concentration:0.16 μM, 2.08 μM and 0.02 μM
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Incubation Time:0-60 h
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Result:Significantly inhibited tumor migration at 48 and 60h time points in MEC cell lines.
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Cell Line:MEC cell lines
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Concentration:0.16 μM, 2.08 μM and 0.02 μM
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Incubation Time:24 h and 48 h
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Result:Resulted in significant acetylation of histone H3 at lys9 as early as 24h after administration in MEC cell lines.
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Cell Line:Lung cancer cell line H460 and A549
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Concentration:5-400 nM
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Incubation Time:24, 48 and 72h
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Result:Showed a significant inhibitory effect on lung cancer cells.
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Cell Line:Lung cancer cell line H460 and A549
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Concentration:25, 50, 100 nM
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Incubation Time:24 h
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Result:The inhibitory effects of cephaeline on lung cancer cells were significantly reversed after administration of the ferroptosis inhibitors in H460 and A549 cells.
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Cell Line:Lung cancer cell line H460 and A549
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Concentration:25, 50, 100 nM
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Incubation Time:24 h
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Result:Significantly downregulated the key antioxidant genes GPX4, SLC7A11 and inhibited the expression of the key antioxidant regulatory protein NRF2 in lung cancer cells.
Cephaeline (5 mg/kg, i.p.,daily for 7 days) effectively suppressed EBOV infection in EBOV mouse models[3].
Cephaeline (5, 10 mg/kg, i.p., a single dose for 12 days) plays an anti-lung cancer role by inducing ferroptosis in tumor xenograft mouse model[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Ifnar1−/− mice infected with ZIKV (8-9 week old, male and female)[2]
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Dosage:2 mg/kg
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Administration:i.p.,daily for 3 days
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Result:Significantly lowered the serum viral load of ZIKV infected Ifnar1−/− mice and decreased the NS1 protein and ZIKV RNA in serum and liver of mice, respectively.
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Animal Model:EBOV mouse model[3]
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Dosage:5 mg/kg
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Administration:i.p., daily for 7 days
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Result:Achieved 67% survival in EBOV infection to death in EBOV mouse model.
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Animal Model:Tumor xenograft mouse model injected with the lung cancer H460 cell line[4]
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Dosage:5, 10 mg/kg
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Administration:i.p., a single dose for 12 days
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Result:Showed significant antitumour effects in tumor xenograft mouse model.
Chemical Information
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CAS No. 483-17-0
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Appearance Solid
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Molecular Weight 466.61
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Formula C28H38N2O4
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Color Off-white to light yellow
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SMILES
OC1=CC2=C([C@@H](C[C@@H]3[C@@H](CC)CN4CCC5=CC(OC)=C(OC)C=C5[C@]4([H])C3)NCC2)C=C1OC
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Synonyms
(-)-Cephaeline; NSC 32944 free base
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (2)
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Journal Impact Factor
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Most Recent
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J Cancer Res Clin Oncol
Prognostic value of amino acid metabolism-related gene expression in invasive breast carcinoma. [Abstract]2023 Oct;149(13):11117-11133. PMID: 37340191
Cephaeline purchased from MedChemExpress. Usage Cited in: J Cancer Res Clin Oncol. 2023 Oct;149(13):11117-11133. [Abstract]
MDA-MB-231 and MCF-7 cells were treated with different dose of Cephaeline (0.1, 0.5, 1, 5, 10 μM) and cell viability were calculated by Cell Counting Kit-8.
Cephaeline purchased from MedChemExpress. Usage Cited in: J Cancer Res Clin Oncol. 2023 Oct;149(13):11117-11133. [Abstract]
Representative images of cell scratch-wound healing test taken by a microscope at × 100 magnification treated with Cephaeline (0.2, 0.4 μM).
Cephaeline purchased from MedChemExpress. Usage Cited in: J Cancer Res Clin Oncol. 2023 Oct;149(13):11117-11133. [Abstract]
Representative western blots for PI3K/AKT signal pathway and HIF-1α under different doses of Cephaeline (0.1, 0.2, 0.3, 0.4, 0.5 μM).
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Daru
2026 Jun 19;34(2):38. PMID: 42319734
Solvent & Solubility
DMSO : 100 mg/mL (214.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 33.33 mg/mL (71.43 mM; Need ultrasonic)
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.36 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.36 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (284 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
[2]. Yang S, et al. Emetine inhibits Zika and Ebola virus infections through two molecular mechanisms: inhibiting viral replication and decreasing viral entry. Cell Discov. 2018 Jun 5;4:31. [Content Brief]
[3]. Silva LC, et al. Cephaeline is an inductor of histone H3 acetylation and inhibitor of mucoepidermoid carcinoma cancer stem cells. J Oral Pathol Med. 2022 Jul;51(6):553-562. [Content Brief]
[4]. Chen P, et al. Cephaeline promotes ferroptosis by targeting NRF2 to exert anti-lung cancer efficacy. Pharm Biol. 2024 Dec;62(1):195-206. [Content Brief]
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 2.1431 mL | 10.7156 mL | 21.4312 mL | 53.5779 mL |
| 5 mM | 0.4286 mL | 2.1431 mL | 4.2862 mL | 10.7156 mL | |
| 10 mM | 0.2143 mL | 1.0716 mL | 2.1431 mL | 5.3578 mL | |
| 15 mM | 0.1429 mL | 0.7144 mL | 1.4287 mL | 3.5719 mL | |
| 20 mM | 0.1072 mL | 0.5358 mL | 1.0716 mL | 2.6789 mL | |
| 25 mM | 0.0857 mL | 0.4286 mL | 0.8572 mL | 2.1431 mL | |
| 30 mM | 0.0714 mL | 0.3572 mL | 0.7144 mL | 1.7859 mL | |
| 40 mM | 0.0536 mL | 0.2679 mL | 0.5358 mL | 1.3394 mL | |
| 50 mM | 0.0429 mL | 0.2143 mL | 0.4286 mL | 1.0716 mL | |
| 60 mM | 0.0357 mL | 0.1786 mL | 0.3572 mL | 0.8930 mL | |
| DMSO | 80 mM | 0.0268 mL | 0.1339 mL | 0.2679 mL | 0.6697 mL |
| 100 mM | 0.0214 mL | 0.1072 mL | 0.2143 mL | 0.5358 mL |