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Bigelovin

Catalog No. TN6735 CAS 3668-14-2

Bigelovin 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.It is also known as a potent cytotoxic sesquiterpene lactone from Inula sp.

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Bigelovin, CAS 3668-14-2

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Purity: 98%

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Storage & Solubility Information

Description	Bigelovin 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.It is also known as a potent cytotoxic sesquiterpene lactone from Inula sp.
In vitro	BigV exhibited potential anti-tumor activities against human liver cancer in vitro and in vivo.?BigV reduced the cell proliferation and colony formation.?BigV induced apoptosis through improving the cleavage of Caspase-3 and poly (ADP-ribose) polymerase 1 (PARP-1).?The process was along with the activation of autophagy, as proved by the enhanced accumulation of autophagosomes, the microtubule-associated light chain 3B-II (LC3B-II) and Beclin-1, and p62 decrease.?Further, the autophagy blockage markedly sensitized BigV-induced cell death, indicating the cytoprotective function of autophagy in liver cancer cell lines.?In addition, BigV treatment inactivated the pathway of protein kinase B (AKT)/mammalian target of rapamycin (mTOR)/ribosomal protein S6 kinase (p70S6K).?Of note, BigV-induced cell death was abolished by over-expressing the phosphorylation of mTOR.?Intriguingly, the induction of apoptosis and autophagy were eliminated by the pretreatment of reactive oxygen species (ROS) scavenger N-acetyl-l-cysteine (NAC), suggesting that ROS played an important role in the regulation of BigV-induced cell death.
In vivo	In vivo studies demonstrated that BigV significantly suppressed the growth of HepG2 cancer xenograft tumors through the activation of apoptosis and autophagy in a dose-dependent manner with low systemic toxicity.?Revealed that BigV had significant antitumor effects against human liver cancer and it may potentially be used as a novel antitumor agent for the prevention of liver cancer.

Molecular Weight	304.34
Formula	C17H20O5
CAS No.	3668-14-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 60 mg/ml (197.15 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Bei Wang, et al. Bigelovin, a sesquiterpene lactone, suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation in liver cancer. Biochem Biophys Res Commun. 2018 May 5;499(2):156-163.

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Keywords

Bigelovin 3668-14-2 Apoptosis Autophagy Immunology/Inflammation Metabolism NF-Κb RAR/RXR Reactive Oxygen Species Retinoid Receptor inhibit Inhibitor Retinoic acid receptors Retinoid X receptors RAR/RXR inhibitor

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