(-)-Securinine
Based on 2 publication(s) in Google Scholar
(-)-Securinine is plant-derived alkaloid and also a GABAA receptor antagonist.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 5610-40-2
- Formula: C13H15NO2
- Molecular Weight:217.27
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) (-)-Securinine
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Biological Activity
GABAA receptor[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
6.1 μM
Compound: 1
|
Cytotoxicity against human A375 cells assessed as growth inhibition after 72 hrs by ATPlite assay
Cytotoxicity against human A375 cells assessed as growth inhibition after 72 hrs by ATPlite assay
|
[PMID: 26793989] |
| A-375 | IC50 |
6.1 μM
Compound: 1
|
Antiproliferative activity against human A375 cells assessed as reduction in cell viability after 72 hrs by ATPlite assay
Antiproliferative activity against human A375 cells assessed as reduction in cell viability after 72 hrs by ATPlite assay
|
[PMID: 27096049] |
| A549 | IC50 |
>10 μM
Compound: 1
|
Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by ATPlite assay
Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by ATPlite assay
|
[PMID: 26793989] |
| A549 | IC50 |
>10 μM
Compound: 1
|
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by ATPlite assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by ATPlite assay
|
[PMID: 27096049] |
| A549 | IC50 |
>10 μM
Compound: 12
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Cytotoxicity against human A549 cells after 48 hrs by SRB assay
Cytotoxicity against human A549 cells after 48 hrs by SRB assay
|
[PMID: 31082231] |
| A549 | IC50 |
23.59 μM
Compound: Securinine
|
Growth inhibition of human A549 cells after 72 hrs by MTT assay
Growth inhibition of human A549 cells after 72 hrs by MTT assay
|
[PMID: 27344492] |
| A549 | IC50 |
25 μM
Compound: 1
|
Cytotoxicity against human A549 cells after 72 hrs by Coulter counter analysis
Cytotoxicity against human A549 cells after 72 hrs by Coulter counter analysis
|
[PMID: 26793989] |
| A549 | IC50 |
25 μM
Compound: 1
|
Antiproliferative activity against human A549 cells
Antiproliferative activity against human A549 cells
|
[PMID: 27096049] |
| BV-2 | IC50 |
1.1 μM
Compound: 12
|
Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitrite production after 24 hrs by Griess assay
Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitrite production after 24 hrs by Griess assay
|
[PMID: 31082231] |
| HCT-116 | IC50 |
>10 μM
Compound: 1
|
Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by ATPlite assay
Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by ATPlite assay
|
[PMID: 26793989] |
| HCT-116 | IC50 |
>10 μM
Compound: 1
|
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by ATPlite assay
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by ATPlite assay
|
[PMID: 27096049] |
| HCT-116 | IC50 |
8.6 μM
Compound: 1
|
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability
|
[PMID: 35183880] |
| HCT-15 | IC50 |
>10 μM
Compound: 12
|
Cytotoxicity against human HCT15 cells after 48 hrs by SRB assay
Cytotoxicity against human HCT15 cells after 48 hrs by SRB assay
|
[PMID: 31082231] |
| HeLa | IC50 |
50.23 μM
Compound: Securinine
|
Growth inhibition of human HeLa cells after 72 hrs by MTT assay
Growth inhibition of human HeLa cells after 72 hrs by MTT assay
|
[PMID: 27344492] |
| HepG2 | IC50 |
36.87 μM
Compound: Securinine
|
Growth inhibition of human HepG2 cells after 72 hrs by MTT assay
Growth inhibition of human HepG2 cells after 72 hrs by MTT assay
|
[PMID: 27344492] |
| HL-60 | IC50 |
>10 μM
Compound: 1
|
Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by ATPlite assay
Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by ATPlite assay
|
[PMID: 26793989] |
| HL-60 | IC50 |
>10 μM
Compound: 1
|
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 72 hrs by ATPlite assay
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 72 hrs by ATPlite assay
|
[PMID: 27096049] |
| HL-60 | IC50 |
0.1 μM
Compound: 1
|
Cytotoxicity against human HL-60 cells assessed as reduction in cell viability
Cytotoxicity against human HL-60 cells assessed as reduction in cell viability
|
[PMID: 35183880] |
| KB | IC50 |
2.2 μg/mL
Compound: 6
|
Cytotoxicity against human KB cells
Cytotoxicity against human KB cells
|
[PMID: 18052029] |
| L1210 | IC50 |
1.9 μg/mL
Compound: 6
|
Cytotoxicity against mouse L1210 cells
Cytotoxicity against mouse L1210 cells
|
[PMID: 18052029] |
| MCF7 | IC50 |
25 μM
Compound: 1
|
Cytotoxicity against human MCF7 cells assessed as growth inhibition by CCK8 assay
Cytotoxicity against human MCF7 cells assessed as growth inhibition by CCK8 assay
|
[PMID: 26793989] |
| MCF7 | IC50 |
25 μM
Compound: 1
|
Antiproliferative activity against human MCF7 cells by CCK8 assay
Antiproliferative activity against human MCF7 cells by CCK8 assay
|
[PMID: 27096049] |
| SH-SY5Y | IC50 |
78.9 μM
Compound: Securinine
|
Growth inhibition of human SH-SY5Y cells after 72 hrs by MTT assay
Growth inhibition of human SH-SY5Y cells after 72 hrs by MTT assay
|
[PMID: 27344492] |
| SK-MEL-2 | IC50 |
>10 μM
Compound: 12
|
Cytotoxicity against human SK-MEL-2 cells after 48 hrs by SRB assay
Cytotoxicity against human SK-MEL-2 cells after 48 hrs by SRB assay
|
[PMID: 31082231] |
| SK-OV-3 | IC50 |
>10 μM
Compound: 12
|
Cytotoxicity against human SKOV3 cells after 48 hrs by SRB assay
Cytotoxicity against human SKOV3 cells after 48 hrs by SRB assay
|
[PMID: 31082231] |
| SW480 | IC50 |
25.855 μM
Compound: Securinine
|
Antiproliferative activity against human SW480 cells after 48 hrs by MTT assay
Antiproliferative activity against human SW480 cells after 48 hrs by MTT assay
|
[PMID: 27344492] |
(-)-Securinine is a major plant-derived alkaloid and also a GABAA receptor antagonist. (-)-Securinine is significantly potent on HeLa cells growth inhibition with IC50 values of 7.02±0.52 μg/mL (32.3 μM). (-)-Securinine induces apoptosis in a dose-dependent manner in the tested cells, increases the percentage of ROS positive cells and depolarized cells as well as stimulates the activity of ERK1/2, caspase-9 and -3/7. (-)-Securinine also induces cell cycle arrest in S phase. Real-time PCR analysis shows high expression of tumor necrosis factor receptor superfamily (TNFRSF) genes in the cells stimulated with (-)-Securinine[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 5610-40-2
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Appearance Solid
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Molecular Weight 217.27
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Formula C13H15NO2
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Color Light yellow to yellow
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SMILES
O=C(O1)C=C2[C@@]13[C@](CCCC4)([H])N4[C@](C3)([H])C=C2
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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
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
Intraovarian injection of securinine stimulates the growth of small ovarian follicles by reducing stromal suppression. [Abstract]2026 Apr 13;17(1):5061. PMID: 41974717 -
Cell Death Dis
Single-cell transcriptome profiles the heterogeneity of tumor cells and microenvironments for different pathological endometrial cancer and identifies specific sensitive drugs. [Abstract]2024 Aug 7;15(8):571. PMID: 39112478
Solvent & Solubility
DMSO : 50 mg/mL (230.13 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (11.51 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 (11.51 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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-
-
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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.
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.
Protocol
The cells are seeded in 12-well plates (1×105/well) and treated with (-)-Securinine at concentrations of 1.0 to 50.0 μg/mL. The control cells are exposed to DMSO at a concentration of 0.5% (v/v). After 6 h and 24 h of exposure, the activity of caspase-9 is measured by Caspase-Glo 9 Assay Kit and Glomax Multi+ Detection System, according to the manufacturer’s instruction. The activity of caspase-3/7 is assessed after 24 h of exposure the cells to (-)-Securinine. Then the cells are harvested and prepared using Muse Caspase-3/7 Assay Kit according with the manufacturer’s protocol. The stained cells are analyzed by Muse Cell Analyzer. The experiments are performed at least in three independent repeats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
The viability of the cells is determined by MTT assay. HeLa cells are seeded in 96-well plates at a density of 5×103 cells/well and treated for 24 h with (-)-Securinine in the concentration range of 1.0 to 20.0 μg/mL. The maximal concentrations of the solvents used in all the MTT experiments are 5.0% (v/v) and 1.0% (v/v) for methanol and DMSO, respectively. The absorption of the obtained formazan solution is measured with a plate reader. The viability results are presented as IC50 mean values of at least three independent experiments[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
6 week old female nude mice are used and injected bilaterally s.c. with 10×106 HL-60 cells. (-)-Securinine treatment is started 10 days after tumor cell injection. Palpable tumors are present for the established tumor model prior to initiating drug treatment. 15 mg/kg of (-)-Securinine or vehicle (30 µL of DMSO and 70 µL of water) are injected i.p. 2 or 3 times a day for 5 days followed by once a day for two days. This injection schedule is repeated for two additional weeks[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Stefanowicz-Hajduk J, et al. Securinine from Phyllanthus glaucus Induces Cell Cycle Arrest and Apoptosis in Human Cervical Cancer HeLa Cells. PLoS One. 2016 Oct 28;11(10):e0165372. [Content Brief]
[2]. Kalpana Gupta, et al. Securinine, a Myeloid Differentiation Agent with Therapeutic Potential for AML. PLoS One. 2011; 6(6): e21203. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.6026 mL | 23.0128 mL | 46.0257 mL | 115.0642 mL |
| 5 mM | 0.9205 mL | 4.6026 mL | 9.2051 mL | 23.0128 mL | |
| 10 mM | 0.4603 mL | 2.3013 mL | 4.6026 mL | 11.5064 mL | |
| 15 mM | 0.3068 mL | 1.5342 mL | 3.0684 mL | 7.6709 mL | |
| 20 mM | 0.2301 mL | 1.1506 mL | 2.3013 mL | 5.7532 mL | |
| 25 mM | 0.1841 mL | 0.9205 mL | 1.8410 mL | 4.6026 mL | |
| 30 mM | 0.1534 mL | 0.7671 mL | 1.5342 mL | 3.8355 mL | |
| 40 mM | 0.1151 mL | 0.5753 mL | 1.1506 mL | 2.8766 mL | |
| 50 mM | 0.0921 mL | 0.4603 mL | 0.9205 mL | 2.3013 mL | |
| 60 mM | 0.0767 mL | 0.3835 mL | 0.7671 mL | 1.9177 mL | |
| 80 mM | 0.0575 mL | 0.2877 mL | 0.5753 mL | 1.4383 mL | |
| 100 mM | 0.0460 mL | 0.2301 mL | 0.4603 mL | 1.1506 mL |