1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor
  3. (-)-Securinine

(-)-Securinine 

Cat. No.: HY-N2079 Purity: ≥98.0%
Handling Instructions

(-)-Securinine is plant-derived alkaloid and also a GABAA receptor antagonist.

For research use only. We do not sell to patients.

(-)-Securinine Chemical Structure

(-)-Securinine Chemical Structure

CAS No. : 5610-40-2

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Based on 1 publication(s) in Google Scholar

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Description

(-)-Securinine is plant-derived alkaloid and also a GABAA receptor antagonist.

IC50 & Target

GABAA receptor[1]

In Vitro

(-)-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].

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

In Vivo

In this tumor model, tumor growth is significantly impaired with (-)-Securinine treatment indicating that (-)-Securinine has potential as an Acute Myeloid Leukemia (AML) therapeutic. (-)-Securinine treated mice (n=5 mice, bilateral tumors), exhibit an average of more than 75% smaller tumors than vehicle treated mice at the end of the study period[2].

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

Molecular Weight

217.26

Formula

C₁₃H₁₅NO₂

CAS No.
SMILES

O=C(O1)C=C2[[email protected]@]13[[email protected]](CCCC4)([H])N4[[email protected]](C3)([H])C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 2 mg/mL (9.21 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.6028 mL 23.0139 mL 46.0278 mL
5 mM 0.9206 mL 4.6028 mL 9.2056 mL
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

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].

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

Cell Assay
[1]

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].

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

Animal Administration
[2]

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].

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

References
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Keywords:

(-)-SecurinineGABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorInhibitorinhibitorinhibit

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