Powder: -20°C for 3 years
In solvent: -80°C for 2 years
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.
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 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 60 mg/ml (197.15 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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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