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Furanodiene

SKU: orb1684599

Description

Furanodiene is a sesquiterpenoid natural product that acts as a P-glycoprotein (Pgp) inhibitor, reducing both its function and expression. Its anticancer mechanisms, studied in vitro, include anti-angiogenesis, induction of reactive oxygen species (ROS), DNA damage, and apoptosis.

Research Area

Cell Biology, Epigenetics & Chromatin, Immunology & Inflammation, Metabolism Research, Molecular Biology, Neuroscience, Pharmacology & Drug Discovery, Protein Biochemistry, Signal Transduction

Images & Validation

Key Properties

CAS Number19912-61-9
MW216.32
Purity98.00% (May vary between batches)
FormulaC15H20O
SMILESCC=1C2=C(OC1)C\C(\C)=C/CC/C(/C)=C\C2
TargetCDK|||Apoptosis|||PARP|||Caspase|||Reactive Oxygen Species|||P-gp
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (9.25 mM);DMSO:10 mM

Bioactivity

In Vitro
The in vitro effects of Furanodiene were examined on two human breast cancer cell lines, MCF-7 and MDA-MB-231 cells. Assays of proliferation, LDH release, mitochondrial membrane potential (ΔΨm), cell cycle distribution, apoptosis and relevant signaling pathways were performed. The in vivo effect was determined with MCF7 tumor xenograft model in nude mice. Furanodiene significantly inhibited the proliferation and increased the LDH release in both cell lines in a dose-dependent manner. ΔΨm depolarization, chromatin condensation, and DNA fragmentation were also observed after Furanodiene treatment. Furanodiene dose-dependently induced cell cycle arrest at the G0/G1 phase. The protein expressions of p-cyclin D1, total cyclin D1, p-CDK2, total CDK2, p-Rb, total Rb, Bcl-xL, and Akt were significantly inhibited by Furanodiene, whereas the protein expressions of Bad and Bax, and the proteolytic cleavage of caspase-9, caspase-7, and poly-ADP-ribose polymerase (PARP) were dramatically increased. Furthermore, the z-VAD-fmk markedly reversed the Furanodiene-induced cell cytotoxicity, the proteolytic cleavage of caspase-9, and DNA fragmentation but did not affect the proteolytic cleavage of PARP, whereas the Akt inhibitor VIII increased the Furanodiene-induced cytotoxicity and PARP cleavage. In addition, Furanodiene dose-dependently suppressed the tumor growth in vivo, achieving 32% and 54% inhibition rates after intraperitoneal injection of 15 mg/kg and 30 mg/kg, respectively

Storage & Handling

Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

ReactiveOxygenSpecies, Reactive Oxygen Species, P-glycoprotein, Pgp, P-gp (P-glycoprotein), P-gp, Multidrug resistance protein 1, inhibit, PARP, Inhibitor, MDR1, Furanodiene, Apoptosis, ABCB1, CDK, Cluster of differentiation 243, CD243, Caspase

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Key Properties

No computed properties available.

Protocol Information

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1 mg
$ 100.00
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