2. Anti-infection NF-κB Apoptosis Immunology/Inflammation Metabolic Enzyme/Protease
  3. Filovirus Flavivirus Keap1-Nrf2 Ferroptosis Reactive Oxygen Species
  4. Cephaeline

Cephaeline  (Synonyms: (-)-Cephaeline; NSC 32944 free base)

Cat. No.: HY-N4118 Purity: 98.94%
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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.

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Cephaeline Chemical Structure

Cephaeline Chemical Structure

CAS No. : 483-17-0

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Based on 1 publication(s) in Google Scholar

Other Forms of Cephaeline:

Cephaeline Related Antibodies

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1 Publications Citing Use of MCE Cephaeline

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EBOV MARV ZEBOV

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Description

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[1][2][3][4].

IC50 & Target

EBOV

 

Cellular Effect
Cell Line Type Value Description References
A549 IC50
3 μM
Compound: 9
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
[PMID: 31513408]
HeLa IC50
> 10 μg/mL
Compound: 3
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
[PMID: 12880315]
HeLa IC50
7.6 μM
Compound: 9
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
[PMID: 31513408]
HL-60 IC50
14.9 μg/mL
Compound: 3
Cytotoxicity against human HL60 cells by XTT assay
Cytotoxicity against human HL60 cells by XTT assay
[PMID: 12880315]
SK-OV-3 IC50
0.1 μM
Compound: 9
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
[PMID: 31513408]
In Vitro

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.

Cephaeline Related Antibodies

RNA polymerase activity Assay[2]

Cell Line: HEK293 cells
Concentration: 1-1000 nM
Incubation Time: 1 h
Result: Showed the inhibition effect on the RNA polymerase activity of recombinant Zika NS5 enzyme in HEK293 cells.

Immunofluorescence[2]

Cell Line: Vero E6 cells
Concentration: 0-2 μM
Incubation Time: 72 h
Result: Inhibited EBOV entry and replication in Vero E6 cells.

Cell Viability Assay[3]

Cell Line: Mucoepidermoid carcinoma (MEC) cell lines
Concentration: 0-32 μM
Incubation Time: 72 h
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.

Cell Migration Assay [3]

Cell Line: MEC cell lines
Concentration: 0.16 μM, 2.08 μM and 0.02 μM
Incubation Time: 0-60 h
Result: Significantly inhibited tumor migration at 48 and 60h time points in MEC cell lines.

Immunofluorescence[3]

Cell Line: MEC cell lines
Concentration: 0.16 μM, 2.08 μM and 0.02 μM
Incubation Time: 24 h and 48 h
Result: Resulted in significant acetylation of histone H3 at lys9 as early as 24h after administration in MEC cell lines.

Cell Viability Assay[4]

Cell Line: Lung cancer cell line H460 and A549
Concentration: 5-400 nM
Incubation Time: 24, 48 and 72h
Result: Showed a significant inhibitory effect on lung cancer cells.

Immunofluorescence[4]

Cell Line: Lung cancer cell line H460 and A549
Concentration: 25, 50, 100 nM
Incubation Time: 24 h
Result: The inhibitory effects of cephaeline on lung cancer cells were significantly reversed after administration of the ferroptosis inhibitors in H460 and A549 cells.

RT-PCR[4]

Cell Line: Lung cancer cell line H460 and A549
Concentration: 25, 50, 100 nM
Incubation Time: 24 h
Result: Significantly downregulated the key antioxidant genes GPX4, SLC7A11 and inhibited the expression of the key antioxidant regulatory protein NRF2 in lung cancer cells.
In Vivo

Cephaeline (2 mg/kg, i.p.,daily for 3 days) suppresses ZIKV load and decreases the NS1 protein and ZIKV RNA in serum of ZIKV infected Ifnar1−/− mice[2].
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.

Animal Model: Ifnar1−/− mice infected with ZIKV (8-9 week old, male and female)[2]
Dosage: 2 mg/kg
Administration: i.p.,daily for 3 days
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.
Animal Model: EBOV mouse model[3]
Dosage: 5 mg/kg
Administration: i.p., daily for 7 days
Result: Achieved 67% survival in EBOV infection to death in EBOV mouse model.
Animal Model: Tumor xenograft mouse model injected with the lung cancer H460 cell line[4]
Dosage: 5, 10 mg/kg
Administration: i.p., a single dose for 12 days
Result: Showed significant antitumour effects in tumor xenograft mouse model.
Molecular Weight

466.61

Formula

C28H38N2O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1431 mL 10.7156 mL 21.4312 mL
5 mM 0.4286 mL 2.1431 mL 4.2862 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, 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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 (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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 98.94%

SDS (480 KB)

COA (248 KB) HNMR (291 KB) LCMS (87 KB)

Handling Instructions (2659 KB)
References

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
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Cephaeline Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cephaeline483-17-0(-)-CephaelineNSC 32944NSC32944NSC-32944FilovirusFlavivirusKeap1-Nrf2FerroptosisReactive Oxygen Speciesphenolic alkaloidZIKVEBOVhistone H3 acetylationMECanti-cancerferroptosisNRF2Inhibitorinhibitorinhibit

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