Arenobufagin

SKU: orb1301359

Description

Arenobufagin is a bufadienolide compound isolated from toad venom. It exhibits potent antineoplastic activity against hepatocellular carcinoma HepG2 cells and their multidrug-resistant HepG2/ADM counterparts in vitro. This natural product is a valuable research tool for studying cancer cell apoptosis and overcoming drug resistance mechanisms.

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology, Protein Biochemistry, Signal Transduction

Key Properties

• CAS Number: 464-74-4
• MW: 416.51
• Purity: 99.92% (May vary between batches)
• Formula: C₂₄H₃₂O₆
• SMILES: C[C@@]12[C@H](CC[C@]1(O)[C@@H]1CC[C@@H]3C[C@@H](O)CC[C@]3(C)[C@H]1[C@H](O)C2=O)c1ccc(=O)oc1
• Target: Others,mTOR,ATG,Akt,PARP,PI3K,Apoptosis,Caspase,Autophagy
• Solubility: DMSO:250 mg/mL (600.23 mM);Ethanol:10 mg/mL (24.01 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (12 mM)

Bioactivity

• In Vivo:
  Arenobufagin inhibited the growth of HepG2/ADM xenograft tumors, which were associated with poly (ADP-ribose) polymerase cleavage, light chain 3-II activation and mTOR inhibition . Arenobufagin also suppressed sprouting formation from VEGF-treated aortic rings in an ex vivo model .
• In Vitro:
  Arenobufagin induced mitochondria-mediated apoptosis in HCC cells, with decreasing mitochondrial potential, as well as increasing Bax/Bcl-2 expression ratio, Bax translocation from cytosol to mitochondria. Arenobufagin also induced autophagy in HepG2/ADM cells. Autophagy-specific inhibitors (3-methyladenine, chloroquine and bafilomycin A1) or Beclin1 and Atg 5 small interfering RNAs (siRNAs) enhanced arenobufagin-induced apoptosis, indicating that arenobufagin-mediated autophagy may protect HepG2/ADM cells from undergoing apoptotic cell death . arenobufagin inhibited vascular endothelial growth factor (VEGF)-induced viability, migration, invasion and tube formation in human umbilical vein endothelial cells (HUVECs) in vitro . Arenobufagin blocked the Na+/K+ pump current in a dose-dependent manner with a half-maximal concentration of 0.29 microM and a Hill coefficient of 1.1 .

Storage & Handling

• Storage: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, Arenobufagin

Compound Identifiers

PubChem CID

12305198