1. Metabolic Enzyme/Protease
    Immunology/Inflammation
    NF-κB
    Apoptosis
    Autophagy
  2. RAR/RXR
    Reactive Oxygen Species
    Apoptosis
    Autophagy
  3. Bigelovin

Bigelovin 

Cat. No.: HY-116506 Purity: 99.81%
Handling Instructions

Bigelovin, a sesquiterpene lactone isolated from Inula helianthus-aquatica, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.

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

Bigelovin Chemical Structure

Bigelovin Chemical Structure

CAS No. : 3668-14-2

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5 mg USD 280 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Bigelovin, a sesquiterpene lactone isolated from Inula helianthus-aquatica, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation[1].

In Vitro

Bigelovin (0-20 μM, 24-72 h) significantly inhibits cell viability of liver cancer cells and induces apoptosis and autophagy[1].
Bigelovin causes a significant increase of p62, LC3B-II, Beclin-1 and a corresponding decrease of p62 levels in a time-dependent manner[1].
Bigelovin induces cell death involves the suppression of mTOR pathway regulated by ROS production[1].

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

Cell Viability Assay[1]

Cell Line: HepG2 and SMMC-7721 cells.
Concentration: 0-20 μM.
Incubation Time: 24, 48, 72 h.
Result: Significantly reduced the cell viability of HepG2 and SMMC-7721 cells in a dose- and time dependent manner.
No significant difference observed in cell viability of normal liver cell lines, LO2 and LX2, after BigV treatment for 24, 48 or 72 h.

Western Blot Analysis[1]

Cell Line: HepG2 and SMMC-7721 cells.
Concentration: 0-10 μM.
Incubation Time: 24 h.
Result: The expression of Bcl-2 was decreased, whereas Bax was increased after treatment with BigV. Moreover, Caspase-9, -3 and PARP cleavage were activated significantly after BigV treatment.
In Vivo

Bigelovin (BigV, 5, 10, 20 mg/kg) exerts anti-tumor activity in HepG2 xenograft tumor model[1].

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

Animal Model: HepG2 xenograft model based on the male athymic BALB/c nude mice (5-6 weeks old, 18-22 g)[1].
Dosage: 5, 10, 20 mg/kg.
Administration: Intravenous injection every 2 days.
Result: The tumor growth rate was significantly slower in BigV treated groups in a dose-dependent manner, along with the reduced tumor weight.
No significant alteration of body weight and hepatic enzyme levels (AST, ALT and LDH) in serum was observed after BigV administration.
Western blot findings of tumor tissues indicated the activation of apoptosis and autophagy characterized by the increase of cleaved Caspase-3 and PARP, as well as LC3BII levels.
The inactivation of mTOR was also observed in tumor tissues isolated from BigV-treated mice.
Molecular Weight

304.34

Formula

C₁₇H₂₀O₅

CAS No.
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 (328.58 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2858 mL 16.4290 mL 32.8580 mL
5 mM 0.6572 mL 3.2858 mL 6.5716 mL
10 mM 0.3286 mL 1.6429 mL 3.2858 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (8.21 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (8.21 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.21 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.81%

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Bigelovin
Cat. No.:
HY-116506
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